1,389 results on '"Oral retinoid"'
Search Results
2. Hereditary Disorders of Cornification
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Mathes, Erin F., Spring, Shanna, Friedland, Rivka, Paller, Amy S., Teng, Joyce M.C., editor, Marqueling, Ann L., editor, and Benjamin, Latanya T., editor
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- 2017
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3. Non-Oral Drug Delivery in Parkinson’s Disease: Current Applications and Future
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Sinem Yaprak Karavana and Meliha Güneş
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medicine.medical_specialty ,Parkinson's disease ,business.industry ,Pharmacology toxicology ,Pharmaceutical Science ,Molecular Medicine ,Medicine ,Review ,Current (fluid) ,business ,Intensive care medicine ,medicine.disease ,Oral retinoid - Abstract
Parkinson's disease (PD) is a type of movement disorder that affects the ability to perform daily activities. It is considered that 1 million people in the U.S. and more than 10 million people worldwide live with PD. It is a chronic and progressive disease, so symptoms worsen over the time. Patients experience motor symptoms such as tremors, stiffness and slow motion, and non-motor symptoms such as sleep problems, constipation, anxiety, depression and fatigue. Dopaminergic drugs are critical for treating motor symptoms in PD. Levodopa (L-DOPA) is the "gold standard" medication for the control of motor symptoms. Because of the progression of the disease, the effectiveness of oral L-DOPA decreases over time and motor fluctuations such as "delayed ON", "no ON" and unpredictable "ON-OFF" periods appear. These motor fluctuations affect the quality of life of the patient at a high rate and the patient has problems in fulfilling his daily morning routines. Gastrointestinal (GI) problems, as the common non-motor symptom, are the most important cause of motor fluctuations that occur because of inadequate oral treatment with the progression of PD. When oral treatments are not sufficient, non-oral treatments that are not affected by GI problems are required. In this review, the treatment strategies, developed and approved non-oral drug delivery systems in the early and advanced stages of PD are emphasized.
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- 2022
4. The Fearful Patient
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Nguyen, Tien V., Wong, Jillian W., Koo, John, Norman, Robert A., Series editor, Nguyen, Tien V., Wong, Jillian W., and Koo, John
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- 2014
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5. Current and Novel Approaches for Genetic Skin Disorders
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Lai-Cheong, Joey E., Paller, Amy S., and Tom, Wynnis L., editor
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- 2014
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6. Psoriasis and Pityriasis Rubra Pilaris
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Pacha, Omar, Schlichte, Megan J., Hebert, Adelaide A., and Tom, Wynnis L., editor
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- 2014
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7. A 'cluster bomb' oral drug delivery system to sequentially overcome the multiple absorption barriers
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Huirui Wang, Yun Zhang, Lei Wang, Ke Wang, Hao Wang, Junfei Yang, Gao Hui, and Qingling Song
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Drug ,Chemistry ,media_common.quotation_subject ,General Chemistry ,Absorption (skin) ,Receptor-mediated endocytosis ,Clinical therapy ,medicine ,Biophysics ,Doxorubicin ,Delivery system ,Fe3o4 nanoparticles ,Oral retinoid ,medicine.drug ,media_common - Abstract
Oral drugs have been widely used in clinical therapy, but their developments were severely limited by the side effects of drug exposure as well as the multiple biological barriers. In this study, we constructed a “cluster bomb” oral drug delivery system (DOX@PFeL@L100) with core-shell structure to overcome the complex absorption barriers. The inner core termed as “bomb” that contains a lot of ultra-small diameter Fe3O4 nanoparticles (DOX@PFeL NPs) loaded with doxorubicin (DOX) and modified with l -valine, which can efficiently penetrate the epithelial cells via PePT1 receptor mediated endocytosis. The outer shell of this “cluster bomb” is a layer of pH-sensitive polymer (Eudragit®L100) that can be served as a pH-responsive switch and effectively control the “bomb” release in the intestinal microenvironment to improve the antitumor efficiency by the Fenton like reaction of DOX and Fe2+/Fe3+. This study demonstrates that the “cluster comb” oral drug delivery system can sequentially overcome the multiple biological barriers, providing a safe and effective approach for tumor therapy.
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- 2022
8. Jennifer Dressman - 40 years of Oral Drug Absorption
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Bertil Abrahamsson, James Butler, Rodrigo Cristofoletti, Christos Reppas, Edmund Kostewicz, and Christoph Saal
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Chemistry ,Pharmaceutical Science ,Absorption (electromagnetic radiation) ,Oral retinoid ,Nuclear chemistry - Published
- 2022
9. In-Silico Prediction of Oral Drug Bioavailability: A multi-boluses approach
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Marta Menci, Filippo Cacace, Marco Papi, and Vincenzo Piemonte
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Empirical equations ,Study drug ,Computer science ,Intestinal physiology ,In silico ,Biomedical Engineering ,Biophysics ,Administration, Oral ,Reproducibility of Results ,Continuous mode ,Models, Biological ,Bioavailability ,Intestinal Absorption ,Pharmaceutical Preparations ,Solubility ,Computer Simulation ,Biological system ,Oral retinoid ,Reliability (statistics) - Abstract
This work focuses on a new mathematical model able to describe in a simple manner the intestinal physiology, in order to better study drug absorption and bioavailability. The aim of our model is to overcome the limitations of physiological pharmacokinetics models of the literature, introducing a different modelling approach. The core of the new proposed model is a Discrete-Continuous Approach (DCA): a sequence of boluses travels in the investigated portion of the intestine, in counter-current with blood that flows in continuous mode. No empirical equations are implemented in this model. Simulation results show an excellent correlation between the predicted and experimental concentration profile used to validate our model. Our new approach provides a simple tool, with a good reliability, to analyze a very complex phenomenon, using only few parameters.
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- 2021
10. Investigations of personalized and sustainable approach of oral drug delivery systems through additive manufacturing
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R. Durga Prasad Reddy, Haytham Elgazzar, and Vivek Sharma
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Fused deposition modeling ,business.industry ,Computer science ,Mechanical Engineering ,3D printing ,Excipient ,Industrial and Manufacturing Engineering ,law.invention ,Tableting ,law ,medicine ,Drug release ,Taguchi analysis ,Process engineering ,business ,Life-cycle assessment ,Oral retinoid ,medicine.drug - Abstract
Purpose The purpose of this paper is to print a thermolabile drug-containing tablet using the fused deposition modeling (FDM) technique and analyze its mechanical, pharmaceutical and environmental feasibility using a variety of tests. Design/methodology/approach Ascorbic acid (Vitamin C) is the thermally-sensitive drug impregnated into polyvinyl alcohol excipient using ethanol-water mixture and printed by an FDM printer by varying three parameters without using any external stabilizing agent. Afterward, Taguchi analysis has been performed on these parameters to recognize the significant factors and interactions. Besides this, a regression model has been obtained based on the dissolution data. Various thermo-mechanical and pharmaceutical tests have been carried out to confirm the feasibility. Finally, a life cycle assessment (LCA) analysis has been carried out to compare it with the existing tableting method by considering the environmental impacts. Findings The dissolution profile was found to follow the Korsmeyer-Peppas model, where the drug release occurred both by dissolution and erosion. Further, the infill percent has been found as the most significant parameter. The characterization tests and imaging outputs proved the fidelity of this attempt. Finally, the three-dimensional printed method was found to be more environmentally sustainable than the existing conventional tableting process. Originality/value LCA on a printed tablet is a one-of-a-kind attempt. Thus, this research attempt delivered another approach to print personalized tablets at a temperature lower than prescribed temperatures with required release behavior and can contribute toward the quest of sustainable personalized medication.
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- 2021
11. New players in the treatment of hypercholesterolaemia: focus on bempedoic acid and inclisiran
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Alberto Corsini, Nicola Ferri, Cesare Riccardo Sirtori, and Massimiliano Ruscica
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myalgia ,Atherosclerotic cardiovascular disease ,business.industry ,Hypercholesterolemia ,Articles ,Bempedoic acid ,Inclisiran ,Bioinformatics ,Proprotein convertase ,Clinical trial ,Statin side effect ,Kexin ,Medicine ,lipids (amino acids, peptides, and proteins) ,AcademicSubjects/MED00200 ,medicine.symptom ,Cardiology and Cardiovascular Medicine ,business ,Oral retinoid - Abstract
Dyslipidaemias and in particular elevated plasma low-density lipoprotein cholesterol (LDL-C) levels are major risk factors for atherosclerotic cardiovascular disease (ASCVD). Indeed, the more LDL-C is reduced the larger will be the ASCVD risk reduction. Although statins represent the first-line intervention to reduce the atherosclerotic burden driven by raised levels of LDL-C, adherence is not optimal and most patients do not follow guidelines and recommended doses. Thus, to achieve optimal LDL-C goals, especially in very high-risk patients, there is a need for new and safe agents, more tolerable than statins with low risk of myalgia. Thus, the present review will address the most recent clinical trials with bempedoic acid and inclisiran. Bempedoic acid is an oral drug acting at a biochemical step preceding hydroxymethylglutaryl-CoA reductase and not associated with muscular side effects. Inclisiran, the first-in-class small interfering RNA-based approach, has the ability to effectively reduce LDL-C by inhibiting the hepatic synthesis of proprotein convertase subtilisin/kexin type 9, with the advantage of requiring subcutaneous of a single dose on Day 1, Day 90, and every 6 months thereafter.
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- 2021
12. FORMULATION AND EVALUATION OF FLOATING IN SITU GEL OF OMEPRAZOLE MAGNESIUM FOR ORAL DRUG DELIVERY SYSTEM
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Mahesh Kumar Kataria and Ankit Soni
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Pharmacology ,In situ ,Chemistry ,Pharmaceutical Science ,Pharmacology (medical) ,Delivery system ,Omeprazole Magnesium ,Oral retinoid - Abstract
Objective: Omeprazole magnesium is indicated for the treatment of erosive esophagitis associated with gastroesophageal reflux disease. It is one of the highly prescribed proton pump inhibitor in the management of peptic ulcer diseases. The therapeutic concentration of a drug in blood can be maintained for a prolonged period of time by administering it in the form of in situ floating gel dosage form. Omeprazole magnesium undergoes degradation at a low pH of the esophagus and stomach; it is therefore given as in situ gel, so, there is minimum contact with acidic pH. Methods: Omeprazole magnesium suspension prepared using various polymers and floating agents in varying concentrations. Several evaluation tests including dissolution test to ensure the release of the drug from formulation by in vitro technique, color and homogeneity, in vitro floating duration, in vitro gelling capacity, drug content determination, pH of the formulation, and floating lag time were studied. Results: All formulations demonstrated good Fourier-transform infrared compliance and no interaction between drug, polymer, and other excipients. The study’s findings show that the formulation F6 showed the best results. Conclusion: The developed formulation was a viable alternative conventional solution by virtue of its ability to enhance bioavailability through its longer gastric residence time and ability to sustain drug release as well as the advantage of floating and pH which minimize the degradation of omeprazole magnesium which is easily degraded by acidic environment.
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- 2021
13. High compliance and effective treatment of fish endoparasitic infections with oral drug delivery nanobioparticles: Safety of intestinal tissue and blood parameters
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Marcos Tavares-Dias, Anai P. Flores-Gonzales, Omar Mertins, Ana C.M.F. Patta, Carlos A.B. Ramirez, Patrick D. Mathews, Vera L.S. Rigoni, and Rafael R.M. Madrid
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Alginates ,Veterinary (miscellaneous) ,Administration, Oral ,Trematode Infections ,Aquatic Science ,Biology ,Pharmacology ,Praziquantel ,Fish Diseases ,Oral administration ,medicine ,Animals ,Catfishes ,Chitosan ,Drug Carriers ,Intestines ,Compliance (physiology) ,Toxicity ,Drug delivery ,Nanoparticles ,%22">Fish ,Trematoda ,Blood parameters ,Oral retinoid ,medicine.drug - Abstract
Parasite infections in fish require constant surveillance and strategies for efficient treatments which guarantee the fish health, their sale value and the non-propagation of pathogens in new environments. Fish treatments based on nanotechnology become of increasing interest since nanoparticles have been shown as efficient materials for optimizing administration of bioactives. In this study a chitosan derivative, alginate and praziquantel conjugated nanobioparticle of effective action for oral treatment of digenetic trematodes in highly infected Corydoras schwartzi was evaluated in terms of histological and hematological safety. The inherent absence of alterations in intestinal tissue and the reversible blood cells counting during a period up to 35 days showed the safety of the drug delivery nanobioparticles, which thus represent a promising strategy for effective applications in pathogens treatments by oral administration.
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- 2021
14. In vitro and in vivo correlation for lipid-based formulations: Current status and future perspectives
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Zhongjian Chen, Yi Lu, Yanping Huang, Quangang Zhu, Wei Wu, and Qin Yu
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LBF, lipid-based formulation ,Computer science ,Review ,AUC, area under the curve ,SLS, sodium lauryl sulfate ,0302 clinical medicine ,IVIVC ,SIF, simulated intestinal fluid ,SCT, short-chain triglyceride ,General Pharmacology, Toxicology and Pharmaceutics ,SEDDS, self-emulsifying drug delivery system ,In silico prediction ,0303 health sciences ,FDA, US Food and Drug Administration ,DDS, drug delivery system ,GI, gastrointestinal ,SMEDDS, self-microemulsifying drug delivery system ,In vitro and in vivo correlations ,CETP, cholesterol ester transfer protein ,Oral delivery ,030220 oncology & carcinogenesis ,LCT, long-chain triglyceride ,Perspectives ,HLB, hydrophilic–lipophilic balance ,Lipolysis ,MCT, medium-chain triglyceride ,RM1-950 ,Computational biology ,PK, pharmacokinetic ,Absorption ,Gastrointestinal digestion ,03 medical and health sciences ,In vivo ,PBPK, physiologically based pharmacokinetic ,SGF, simulated gastric fluid ,TIM, TNO gastrointestinal model ,030304 developmental biology ,BCS, biopharmaceutics classification system ,IVIVC, in vitro and in vivo correlation ,SNEDDS, self-nanoemulsifying drug delivery system ,ANN, artificial neural network ,TNO, Netherlands Organization for Applied Scientific Research ,IVIVR, in vitro and in vivo relationship ,Therapeutics. Pharmacology ,Cmax, peak plasma concentration ,BE, bioequivalence ,Oral retinoid ,Tmax, time to reach the peak plasma concentration ,Lipid-based formulation ,Model - Abstract
Lipid-based formulations (LBFs) have demonstrated a great potential in enhancing the oral absorption of poorly water-soluble drugs. However, construction of in vitro and in vivo correlations (IVIVCs) for LBFs is quite challenging, owing to a complex in vivo processing of these formulations. In this paper, we start with a brief introduction on the gastrointestinal digestion of lipid/LBFs and its relation to enhanced oral drug absorption; based on the concept of IVIVCs, the current status of in vitro models to establish IVIVCs for LBFs is reviewed, while future perspectives in this field are discussed. In vitro tests, which facilitate the understanding and prediction of the in vivo performance of solid dosage forms, frequently fail to mimic the in vivo processing of LBFs, leading to inconsistent results. In vitro digestion models, which more closely simulate gastrointestinal physiology, are a more promising option. Despite some successes in IVIVC modeling, the accuracy and consistency of these models are yet to be validated, particularly for human data. A reliable IVIVC model can not only reduce the risk, time, and cost of formulation development but can also contribute to the formulation design and optimization, thus promoting the clinical translation of LBFs., Graphical abstract In vitro and in vivo correlations (IVIVCs) are powerful tools for preparation development. Constructing IVIVCs for lipid-based formulations is rather challenging. This article reviews the current status and future perspectives in this field.Image 1
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- 2021
15. An update on oral drug delivery via intestinal lymphatic transport
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Wei Wu, Yi Lu, Zichen Zhang, and Jianping Qi
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Oral ,Drug ,Microfold cell ,media_common.quotation_subject ,RM1-950 ,Bioinformatics ,Systemic circulation ,Chylomicron ,03 medical and health sciences ,Lymphatic transport ,0302 clinical medicine ,Medicine ,General Pharmacology, Toxicology and Pharmaceutics ,Drug absorption ,030304 developmental biology ,media_common ,Drug transport ,0303 health sciences ,business.industry ,Lymphatic system ,030220 oncology & carcinogenesis ,Drug delivery ,Therapeutics. Pharmacology ,business ,Oral retinoid ,Drug metabolism - Abstract
Orally administered drug entities have to survive the harsh gastrointestinal environment, penetrate the enteric epithelia and circumvent hepatic metabolism before reaching the systemic circulation. Whereas the gastrointestinal stability can be well maintained by taking proper measures, hepatic metabolism presents as a formidable barrier to drugs suffering from first-pass metabolism. The pharmaceutical academia and industries are seeking alternative pathways for drug transport to circumvent problems associated with the portal pathway. Intestinal lymphatic transport is emerging as a promising pathway to this end. In this review, we intend to provide an updated overview on the rationale, strategies, factors and applications involved in intestinal lymphatic transport. There are mainly two pathways for peroral lymphatic transport—the chylomicron and the microfold cell pathways. The underlying mechanisms are being unraveled gradually and nowadays witness increasing research input and applications.
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- 2021
16. Revising Pharmacokinetics of Oral Drug Absorption: II Bioavailability-Bioequivalence Considerations
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Pavlos Chryssafidis, Athanasios A. Tsekouras, and Panos Macheras
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Pharmacology ,Absorption (pharmacology) ,Organic Chemistry ,Cmax ,Administration, Oral ,Biological Availability ,Pharmaceutical Science ,Time data ,Bioequivalence ,Models, Biological ,Bioavailability ,Combinatorics ,Intestinal Absorption ,Therapeutic Equivalency ,Pharmacokinetics ,Area Under Curve ,Humans ,Molecular Medicine ,Pharmacology (medical) ,Oral retinoid ,Biotechnology ,Mathematics ,Absolute bioavailability - Abstract
To explore the application of the parameters of the physiologically based finite time pharmacokinetic (PBFTPK) models subdivided in first-order (PBFTPK)1 and zero-order (PBFTPK)0 models to bioavailability and bioequivalence. To develop a methodology for the estimation of absolute bioavailability, F, from oral data exclusively. Simulated concentration time data were generated from the Bateman equation and compared with data generated from the (PBFTPK)1 and (PBFTPK)0 models. The blood concentration Cb(τ) at the end of the absorption process τ, was compared to Cmax; the utility of $$ {(AUC)}_0^{\tau } $$ and $$ {(AUC)}_t^{\infty } $$ in bioequivalence assessment was also explored. Equations for the calculation of F from oral data were derived for the (PBFTPK)1 and (PBFTPK)0 models. An estimate for F was also derived from an areas proportionality using oral data exclusively. The simulated data of the (PBFTPK)0 models exhibit rich dynamics encountered in complex drug absorption phenomena. Both (PBFTPK)1 and (PBFTPK)0 models result either in Cmax = Cb(τ) or Cmax > Cb(τ) for rapidly- and not rapidly-absorbed drugs, respectively; in the latter case, Cb(τ) and τ are meaningful parameters for drug’s rate of exposure. For both (PBFTPK)1 and (PBFTPK)0 models, $$ {(AUC)}_0^{\tau } $$ or portions of it cannot be used as early exposure rate indicators. $$ {(AUC)}_{\tau}^{\infty } $$ is a useful parameter for the assessment of extent of absorption for very rapidly absorbed drugs. An estimate for F for theophylline formulations was found close to unity. The (PBFTPK)1 and (PBFTPK)0 models are more akin to in vivo conditions. Estimates for F can be derived from oral data exclusively.
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- 2021
17. Confluent and Reticulated Papillomatosis
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Jackson-Richards, Diane, Jackson-Richards, Diane, editor, and Pandya, Amit G., editor
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- 2014
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18. Inherited Keratinocyte Diseases (Ichthyosis and Related Disorders)
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Ishida-Yamamoto, Akemi, Krieg, Thomas, editor, Bickers, David R., editor, and Miyachi, Yoshiki, editor
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- 2010
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19. Common Skin Problems
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Rzany, Berthold, Maio, Mauricio, and Rzany, Berthold
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- 2009
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20. Darier’s Disease
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Saez-De-Ocariz, Marimar, Orozco-Covarrubias, Luz, Durán-McKinster, Carola, Ruiz-Maldonado, Ramón, Ruggieri, Martino, editor, Pascual-Castroviejo, Ignacio, editor, and Di Rocco, Concezio, editor
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- 2008
- Full Text
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21. Magnetic Ganoderma Lucidum Spores (mGLS): A Novel Regulatable Targeted Drug Delivery System
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Zhankun Weng, Kaige Qu, Fenguo Zhou, Jingmei Li, Bojian Liang, Zuobin Wang, Bin Han, Yuhan Wu, Xin Zhao, Qinhan Zhang, and Guixia Liu
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Carrier material ,Pharmacokinetics ,Targeted drug delivery ,In vivo ,Chemistry ,Drug delivery ,Biophysics ,Bioengineering ,Pharmacology ,Oral retinoid ,Biotechnology ,Ganoderma lucidum ,Spore - Abstract
In the past decades, many materials have been studied as carriers for targeted drug delivery. However, there is a need for utilizable and selective carrier materials with few side effects. Here, the magnetic Ganoderma Lucidum Spores (mGLS) as a highly efficient targeted drug delivery carrier were explored. Then the regulatable targeted drug delivery system was verified by loading and releasing of the 5-Fluorouracil (5-FU). The results showed that the maximum of the loaded 5-FU reached 250.23 mg·g−1 in the mGLS. The cumulative release of the 5-FU for the drug delivery system could reach 80.11% and 67.14% in the PBS and HCl after 48 h, respectively. In addition, this system showed the good pharmacokinetic properties in vivo. After 12 h, the blood concentration in the 5-FU@mGLS group kept at 5.3 µg·mL−1 and was four times higher than that in the 5-FU group. In summary, the GLS as a natural microscale core-shell structures appears the striking application in carrier material for oral drug delivery.
- Published
- 2021
22. Preparation and optimization of fast disintegrating tablets of isosorbide dinitrate using lyophilization method for oral drug delivery
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Elaheh Nasiri, Mitra Alami-Milani, Mitra Jelvehgari, and Sara Salatin
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Saliva ,Administration, Oral ,Pharmaceutical Science ,02 engineering and technology ,Polyethylene glycol ,Isosorbide Dinitrate ,030226 pharmacology & pharmacy ,03 medical and health sciences ,Freeze-drying ,chemistry.chemical_compound ,Drug Delivery Systems ,0302 clinical medicine ,medicine ,Humans ,Child ,Aged ,Chromatography ,021001 nanoscience & nanotechnology ,Freeze Drying ,Solubility ,chemistry ,Isosorbide dinitrate ,0210 nano-technology ,Oral retinoid ,Tablets ,medicine.drug - Abstract
Background: Orally disintegrating tablets rapidly disintegrate in saliva and then swallowed without the need for water. Materials & methods: The orally disintegrating tablets were prepared by freeze-drying of an aqueous dispersion of isosorbide dinitrate containing a matrix former (gelatin), a cryoprotectant (mannitol), a plasticizer (glycerin) and a dissolution enhancer (Tween/polyethylene glycol). Results: Results demonstrated that the selected formulation, Ft9, disintegrated within 1 min and showed faster dissolution rate compared with the commercial tablet. Conclusion: Having a fast disintegration time, the developed lyophilized tablet does not need to be swallowed as a whole. So, it is a convenient solid oral dosage form for the patients who have difficulty with swallowing such as the pediatric and elderly ones.
- Published
- 2021
23. Synthesis and Characterization of Thiolated Gum Ghatti as a Novel Excipient: Development of Compression-Coated Mucoadhesive Tablets of Domperidone
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Inderbir Singh, Vivek Puri, Kampanart Huanbutta, Ameya Sharma, and Pradeep Kumar
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chemistry.chemical_classification ,Chemistry ,General Chemical Engineering ,Excipient ,General Chemistry ,Polymer ,Article ,Domperidone ,chemistry.chemical_compound ,Gum ghatti ,Drug delivery ,medicine ,Mucoadhesion ,Thioglycolic acid ,QD1-999 ,Oral retinoid ,Nuclear chemistry ,medicine.drug - Abstract
Mucoadhesive polymers represent a major part of site-specific and localized retention strategies in oral drug delivery. The present research was designed to synthesize and characterize a novel mucoadhesive carbohydrate polymer (thiolated gum ghatti; TGG), which was employed to formulate mucoadhesive tablets of domperidone using an industrially viable compression coating technique. Thiolation of gum ghatti was achieved by the ester formation (esterification) between the hydroxyl group and the carboxyl group of gum ghatti and thioglycolic acid. TGG was characterized by various physicochemical techniques such as FTIR, XRD, SEM, and DSC. In rheological studies, the observed viscosities of pure gum mucin were 45.45 and 71.75 mPa·s and those of the thiolated gum were 78.7 and 112.58 mPa·s, respectively, in water and simulated gastric fluid. A significant increase in viscosity for thiolated gum may be attributed to increased macromolecular interactions responsible for enhanced mucoadhesive potential of thiolated gum. In silico studies corroborate the role of mucin gum interaction and energetic stabilization for enhanced mucoadhesion properties of thiolated gum. Ex vivo mucoadhesion strength of gum ghatti- and TGG-coated tablets was found to be ranging between 45.77 ± 1.49 and 88.16 ± 1.75 and 115.32 ± 2.36 and 184.65 ± 2.07 mN, respectively. In an acute oral toxicity study, TGG did not show any toxicity on the vital organs of the Wistar rat and proved to be a safe polymer. TGG may be regarded as a promising polymer for developing different mucoadhesive drug delivery systems.
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- 2021
24. Natural Superdisintegrant: Opportunity in Oral Drug Delivery System
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Angat T. Kotangale, Aparna O. Yadav, Ajita S. Kesharwani, Vishal K. Bisen, Aishwarya A. Jain, Rina G. Maskare, and Nitin H. Indurwade
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Topiramate ,business.industry ,Medicine ,Delivery system ,Pharmacology ,business ,Oral retinoid ,medicine.drug - Abstract
The present work concerned with formulation and evaluation of fast disintegrating tablet of Topiramate by using natural superdisintegrants like Trigonellafoenum graceum (fenugreek) powder, Plantago ovata powder, dehydrated banana powder, soy polysaccharide, linseed powder. Topiramate is an antiepileptic drug and also used in migraine. Preformulation studies like solubility, melting point were studied. Five formulations were prepared using different natural superdisintegrant with same concentrations by using direct compression method. All the formulations were evaluated for precompression parameters and all the parameters were found to be within the pharmacopoeial limits. Post compression parameters like hardness of the tablet, thickness of the tablet, friability test, weight variation, disintegration test, in-vitro dissolution test, drug content were performed. The formulation F-5 containing Trigonellafoenum-graceum (fenugreek) powder shown disintegration time of 12sec. Rapid disintegration of the Trigonellafoenum-graceum due to its rapid water absorbency swells in water to the extent of 200–300% disintegrates rapidly for quick and complete disintegration of the tablet. An accelerated stability study on optimized formulation was performed and it was found to be stable. It can be concluded that Trigonellafoenum-graceum (fenugreek) powder as Superdisintegrant showed better release than soy polysaccharide, plantago ovata powder, dehydrated banana powder and linseed powder.
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- 2021
25. Trifluoromethyl Hydrolysis En Route to Corroles with Increased Druglikeness
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Vinay Kumar Sharma, Mahmoud Majdoub, Amit Kumar, Yael Diskin-Posner, Atif Mahammed, Natalia Fridman, Pinky Yadav, Zeev Gross, Anil Kumar, and Sally Khoury
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Trifluoromethyl ,Hydrocarbons, Fluorinated ,Molecular Structure ,010405 organic chemistry ,Hydrolysis ,General Chemistry ,General Medicine ,010402 general chemistry ,Druglikeness ,01 natural sciences ,Combinatorial chemistry ,Catalysis ,0104 chemical sciences ,chemistry.chemical_compound ,Water soluble ,chemistry ,Coordination Complexes ,Corrole ,Oral retinoid - Abstract
Heme-like metal-chelating macrocycles, including expanded and contracted porphyrins, are of everlasting interest as drug candidates for numerous diseases. Still, all reported corrole derivatives (and most other heme analogues) do not fulfill the most basic standards expected for oral drug administration: a combination of low molecular weight and reasonable water solubility. We now disclose a very straightforward synthetic method that relies on surprisingly facile trifluoromethyl hydrolysis for gaining access to a new class of corroles that do satisfy all druglikeness criteria. The relevance is briefly exemplified for the iron corroles by demonstrating the ability to affect their association with plasma proteins and their performance for catalase-like decomposition of hydrogen peroxide.
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- 2021
26. Oral Retinoids for Hidradenitis Suppurativa
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Boer, Jurr, Jemec, Gregor B. E., editor, Revuz, Jean, editor, and Leyden, James J., editor
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- 2006
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27. A REVIEW ON CURRENT TRENDS IN ORAL DRUG DELIVERY-FAST DISSOLVING TABLETS
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Ahmed Akif Khan and Afra Azeem
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medicine.medical_specialty ,business.industry ,medicine ,Current (fluid) ,Intensive care medicine ,business ,Oral retinoid - Abstract
Medication conveyance systems are getting progressively complex as drug researchers gain a superior comprehension of the physicochemical and biochemical parameters appropriate to their performance. In the course of recent many years, Fast Dissolving Tablets (FDTs) have acquired a lot of consideration as a preferred option in contrast to regular oral dose structures like tablets and containers. FDTs are strong unit dosage forms containing therapeutic substances which break down or disintegrate quickly for the most part surprisingly fast, when they interact with saliva, in this manner obviating the prerequisite of water during the administration. Hence, these dosage forms have attracted the market for a specific segment of the patient populace which incorporates dysphagic, incapacitated, mystic, geriatric and pediatric patients. This has supported both the scholarly community and industry to produce new orally breaking down formulations and innovative methodologies in this field. This article centers around the different plan angles, disintegrates utilized and innovations produced for FDTs, alongside different excipients, assessment tests, promoted definitions, future possibilities, and medications investigated in this field.
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- 2021
28. X-ray Imaging for Gastrointestinal Tracking of Microscale Oral Drug Delivery Devices
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Carsten Gundlach, Anette Müllertz, Maja Nørgaard Kristensen, Anja Boisen, Rolf Bech Kjeldsen, Thomas Rades, Kinga Zor, Line Hagner Nielsen, and Lasse Højlund Thamdrup
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0206 medical engineering ,Biomedical Engineering ,Administration, Oral ,Computed tomography ,02 engineering and technology ,Barium sulfate ,Biomaterials ,Drug Delivery Systems ,Animals ,Medicine ,Microscale chemistry ,medicine.diagnostic_test ,business.industry ,X-Rays ,Gastrointestinal transit ,Computed tomography scanning ,021001 nanoscience & nanotechnology ,020601 biomedical engineering ,Rats ,Gastrointestinal Tract ,Microcontainers ,Pharmaceutical Preparations ,Delivery system ,Planar X-ray imaging ,Tomography, X-Ray Computed ,0210 nano-technology ,business ,Oral retinoid ,Biomedical engineering - Abstract
Microscale devices are promising tools to overcome specific challenges within oral drug delivery. Despite the availability of advanced high-quality imaging techniques, visualization and tracking of microscale devices in the gastrointestinal (GI) tract is still a challenge. This work explores the possibilities of applying planar X-ray imaging and computed tomography (CT) scanning for visualization and tracking of microscale devices in the GI tract of rats. Microcontainers (MCs) are an example of microscale devices that have shown great potential as an oral drug delivery system. Barium sulfate (BaSO4) loaded into the cavity of the MCs increases their overall X-ray contrast, which allows them to be easily tracked. The BaSO4-loaded MCs are quantitatively tracked throughout the entire GI tract of rats by planar X-ray imaging and visualized in 3D by CT scanning. The majority of the BaSO4-loaded MCs are observed to retain in the stomach for 0.5-2 h, enter the cecum after 3-4 h, and leave the cecum and colon 8-10 h post-administration. The imaging approaches can be adopted and used with other types of microscale devices when investigating GI behavior in, for example, preclinical trials and potential clinical studies.
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- 2021
29. Cross-reactive hypersensitivity to NSAIDs: Experience of a Tunisian allergology center
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L. Ben Mahmoud, R. Sahnoun, Najla Bahloul, H. Ghozzi, H. Khmekhem, Ahmed Hakim, K. Zeghal, and Samy Kammoun
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musculoskeletal diseases ,Drug ,Allergy ,medicine.medical_specialty ,media_common.quotation_subject ,Provocation test ,Center (group theory) ,digestive system ,Atopy ,03 medical and health sciences ,0302 clinical medicine ,Internal medicine ,medicine ,Immunology and Allergy ,In patient ,030212 general & internal medicine ,skin and connective tissue diseases ,media_common ,business.industry ,medicine.disease ,digestive system diseases ,030228 respiratory system ,Celecoxib ,business ,Oral retinoid ,medicine.drug - Abstract
Background The accurate diagnosis of cross-reactive reactions (CRR) to nonsteroidal anti-inflammatory drugs (NSAIDs) depends on a careful history and oral drug challenge. In this study, we report the result of a new procedure implemented in Tunisian allergology center to explore CRR to NASIDs in patients with immediate hypersensitivity (IHS) to NSAIDs. Methods Our structured protocol using oral provocation tests (OPTs) was based on the latest advances in the literature. This protocol was tested in patients with a clinical history of IHS reactions to one or more NSAIDs and referred to the pharmacology department of Sfax (Tunisia) between 2012 and 2018. Patients were classified into 5 subgroups: an ASA subgroup, a multiple NSAIDs subgroup, a single non-selective NSAID subgroup, a paracetamol subgroup, and a celecoxib subgroup. Results A total of 34 patients were enrolled. Personal history of atopy was found in 26 (76.5%). A diagnosis of CRR to NSAIDs was made in 24 patients (70.6%): 6 patients in the ASA subgroup, 12 patients in the multiple NSAIDs subgroup, 4 patients in the single non-selective NSAID subgroup, 1 patient in the paracetamol subgroup and 1 patient in the celecoxib subgroup. Regarding safe alternatives in patients with CRR to NSAIDs (n = 24), prevalence of cross-reactivity to paracetamol or celecoxib was found in 20% and 27.3% of patients with confirmed CRR to NSAIDs, respectively. Conclusion Our structured protocol based on standardized oral provocation tests helps physicians to prescribe a suitable drug in patients with a history of IHS reactions to NSAIDs.
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- 2021
30. A concise review on preparation methods used for the development of solid lipid nanoparticles
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Vasu Deva Reddy Matta
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Drug ,Chemistry ,media_common.quotation_subject ,Nanoparticle ,Nanotechnology ,02 engineering and technology ,021001 nanoscience & nanotechnology ,030226 pharmacology & pharmacy ,Bioavailability ,body regions ,Preparation method ,03 medical and health sciences ,0302 clinical medicine ,Controlled delivery ,Solid lipid nanoparticle ,Drug delivery ,0210 nano-technology ,Oral retinoid ,media_common - Abstract
Solid lipid nanoparticles (SLNs) are in submicron size range nanoparticles and are made of biocompatible and biodegradable materials (mainly composed of lipids and surfactants) capable of incorporating both lipophilic and hydrophilic drugs. SLNs are also considered as substitute to other colloidal drug systems, also used as controlled systems and targeted delivery. SLNs can be considered as an alternative for oral drug delivery vehicle to improve the oral bioavailability of drugs, associated reduction of drug toxicity and stability of drug in both GIT and plasma. There are different techniques used for the preparation of SLNs. Generally, the preparation of SLNs and any other nanoparticle system necessitates a dispersed system as precursor; otherwise particles are produced through the use of a particular instrumentation. This review provides the summary on the techniques or methods used for the development of SLNs of poorly water soluble drugs for improved drug delivery. Keywords: Solid lipid nanoparticles, controlled delivery, precursor, techniques.
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- 2021
31. FLOATING DRUG DELIVERY SYSTEM: A REVIEW
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Satyawan Singh, Arpita Singh, Amresh Gupta, and Archana Tomar
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medicine.medical_specialty ,Gastric emptying ,Mechanism (biology) ,business.industry ,Drug delivery ,medicine ,General Medicine ,Pharmacology ,Intensive care medicine ,business ,Dosage form ,Oral retinoid ,System a - Abstract
The main motto of working on that article on floating drug delivery systems (FDDS) is to make a compiled report on the recent studies and research with special consideration on the principle mechanism of flotation to achieve gastric retention. The scientific and technological advancements were made in the last few years in the research and development of rate-controlled oral drug delivery systems by overcoming physiological difficulties, like short gastric residence times (GRT) and unpredictable gastric emptying times (GET). This review also epitomized the in-vitro procedure, in-vivo to assess the pursuance and implementation of floating systems, and applications of these systems. These methods are useful to various queries experienced during the development of a pharmaceutical dosage form.
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- 2021
32. Current approaches in lipid-based nanocarriers for oral drug delivery
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Manuel J. Santander-Ortega, María Victoria Lozano, and M. Plaza-Oliver
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Solid-lipid nanoparticle ,Drug ,Nanocapsule ,media_common.quotation_subject ,Administration, Oral ,Biological Availability ,Pharmaceutical Science ,Nanotechnology ,02 engineering and technology ,030226 pharmacology & pharmacy ,03 medical and health sciences ,Drug Delivery Systems ,0302 clinical medicine ,Nanoemulsion ,Solid lipid nanoparticle ,Oral route ,Medicine ,media_common ,Drug Carriers ,Liposome ,Intestinal mucus ,Low toxicity ,business.industry ,021001 nanoscience & nanotechnology ,Lipids ,Oral delivery ,Nanoparticles ,Original Article ,Nanocarriers ,0210 nano-technology ,business ,Self-emulsifying system ,Oral retinoid - Abstract
Graphical abstract Lipid-based nanocarriers have gained much interest as carriers of drugs with poor oral bioavailability because of their remarkable advantages like low toxicity, affordable scale-up manufacture, strong biocompatibility or high drug loading efficiency. The potential of these nanocarriers lies in their ability to improve the gastrointestinal stability, solubility and permeability of their cargo drugs. However, achieving efficient oral drug delivery through lipid-based nanocarriers is a challenging task, since they encounter multiple physicochemical barriers along the gastrointestinal tract, e.g. the gastric acidic content, the intestinal mucus layer or the enzymatic degradation, that they must surmount to reach their target. These limitations may be turned into opportunities through a rational design of lipid-based nanocarriers. For that purpose, this review focuses on the main challenges of the oral route indicating the strategies undertaken for lipid-based nanocarriers in order to overcome them. Understanding their shortcomings and identifying their strengths will determine the future clinical success of lipid-based nanocarriers.
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- 2021
33. Oral biopharmaceutics tools: recent progress from partnership through the Pharmaceutical Education and Research with Regulatory Links collaboration
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Laura J. Henze, Christos Reppas, Jennifer B. Dressman, Marina Statelova, Chara Litou, Christina Pentafragka, Patrick J O'Dwyer, Karl J. Box, Brendan T. Griffin, Maria Vertzoni, and Publica
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Drug ,Physiologically based pharmacokinetic modelling ,Swine ,Computer science ,Drug Compounding ,Food Effect Study ,media_common.quotation_subject ,Pharmaceutical Research ,Administration, Oral ,Biological Availability ,Pharmaceutical Science ,02 engineering and technology ,Models, Biological ,030226 pharmacology & pharmacy ,Biopharmaceutics ,Bio-enabling drug products ,Food-Drug Interactions ,03 medical and health sciences ,0302 clinical medicine ,Drug Development ,Pharmacokinetics ,Animals ,Humans ,Intersectoral Collaboration ,media_common ,Pharmacology ,Paediatrics ,Pig model ,Food effect ,021001 nanoscience & nanotechnology ,Bioavailability ,Gastrointestinal Tract ,In vitro testing ,Education, Pharmacy ,PBPK modelling ,Biorelevant ,Biochemical engineering ,0210 nano-technology ,Oral retinoid - Abstract
ObjectivesTo summarise key contributions of the Pharmaceutical Education and Research with Regulatory Links (PEARRL) project (2016–2020) to the optimisation of existing and the development of new biopharmaceutics tools for evaluating the in vivo performance of oral drug products during the development of new drugs and at the regulatory level.Key findingsOptimised biopharmaceutics tools: Based on new clinical data, the composition of biorelevant media for simulating the fed state conditions in the stomach was simplified. Strategies on how to incorporate biorelevant in vitro data of bio-enabling drug products into physiologically based pharmacokinetic (PBPK) modelling were proposed. Novel in vitro biopharmaceutics tools: Small-scale two-stage biphasic dissolution and dissolution-permeation setups were developed to facilitate understanding of the supersaturation effects and precipitation risks of orally administered drugs. A porcine fasted state simulated intestinal fluid was developed to improve predictions and interpretation of preclinical results using in vitro dissolution studies. Based on new clinical data, recommendations on the design of in vitro methodologies for evaluating the GI drug transfer process in the fed state were suggested. The optimized design of in vivo studies for investigating food effects: A food effect study protocol in the pig model was established which successfully predicted the food-dependent bioavailability of two model compounds. The effect of simulated infant fed state conditions in healthy adults on the oral absorption of model drugs was evaluated versus the fasted state and the fed state conditions, as defined by regulatory agencies for adults. Using PBPK modelling, the extrapolated fasted and infant fed conditions data appeared to be more useful to describe early drug exposure in infants, while extrapolation of data collected under fed state conditions, as defined by regulators for adults, failed to capture in vivo infant drug absorption.SummarySubstantial progress has been made in developing an advanced suite of biopharmaceutics tools for streamlining drug formulation screening and supporting regulatory applications. These advances in biopharmaceutics were achieved through networking opportunities and research collaborations provided under the H2020 funded PEARRL project.
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- 2021
34. Improving Nursing Students’ Medication Safety Knowledge and Skills on Using the 4C/ID Learning Model
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Fitri Haryanti, Lisa Musharyanti, and Mora Claramita
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Instructional design ,Journal of Multidisciplinary Healthcare ,medication-safety ,030503 health policy & services ,education ,nursing students’ education and training ,Safety knowledge ,Drug administration ,General Medicine ,03 medical and health sciences ,Patient safety ,0302 clinical medicine ,Nursing ,Intervention (counseling) ,Observational study ,030212 general & internal medicine ,4C/ID model ,0305 other medical science ,Psychology ,Oral medicine ,General Nursing ,Oral retinoid ,Original Research - Abstract
Lisa Musharyanti,1 Fitri Haryanti,2 Mora Claramita3 1School of Nursing, Faculty of Medicine and Health Sciences, Universitas Muhammadiyah Yogyakarta, Yogyakarta, Indonesia; 2Department of Pediatric and Maternity Nursing, Faculty of Medicine, Public Health and Nursing, Universitas Gadjah Mada, Yogyakarta, Indonesia; 3Department of Medical, Health Professions Education and Bioethics, Faculty of Medicine, Public Health and Nursing, Universitas Gadjah Mada, Yogyakarta, IndonesiaCorrespondence: Lisa MusharyantiSchool of Nursing, Faculty of Medicine and Health Sciences, Universitas Muhammadiyah Yogyakarta, Jalan Brawijaya, Tamantirto, Kasihan, Bantul, Yogyakarta, IndonesiaTel +62 81252126958Email lisa.musharyanti@gmail.comIntroduction: Learning medication-safety has become a focus in many countries to improve medication-safety competencies in nursing students. Research on instructional design for medication-safety is still limited, especially about the use of the Four Components Instructional Design (4C/ID) model. This study aimed to compare the knowledge and skills in medication safety of nursing students after the medication-safety training using four components of instructional design known as 4C/ID.Methods: This was a posttest-only quasi-experimental study using an intervention and control group. The participants were the third-semester students of a nursing school at Yogyakarta, Indonesia (intervention: n=55, control: n=40). The intervention group was trained for five weeks using the 4C/ID approach with interactive lectures, small group discussions, reflections, and skills simulation sessions. An observational skills evaluation and Multiple-Choice Questionnaire were administered in the last week after the training completed. Independent sample t-test and Mann Whitney tests were used to analyze the mean differences of knowledge and skills in giving oral medicine and drug injections between the two groups.Results: The majority of respondents were female (74.1%), aged 19– 20 years (77.8%), with GPA > 3 (87.37%) and, the majority had never received instruction about patient safety (69%). There were significant mean differences in overall knowledge (p< 0.05) and also in the skills of oral drug and intramuscular drug administration (p< 0.05) between the intervention and control groups.Conclusion: Training in medication-safety using the 4C/ID approach could improve the medication-safety knowledge and skills of the nursing students based on simple to complex learning.Keywords: 4C/ID model, medication-safety, nursing students’ education and training
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- 2021
35. Retinoids
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Saurat, J. H., Katsambas, Andreas D., editor, and Lotti, Torello M., editor
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- 2003
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36. Clinical translation of silica nanoparticles
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Janjua, Taskeen Iqbal, Cao, Yuxue, Yu, Chengzhong, and Popat, Amirali
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Materials science ,Comment ,Nanoparticle ,Nanotechnology ,Surfaces, Coatings and Films ,Electronic, Optical and Magnetic Materials ,Biomaterials ,Silica nanoparticles ,Drug delivery ,Materials Chemistry ,Nanoparticles ,Photothermal ablation ,Oral retinoid ,Energy (miscellaneous) - Abstract
Silica nanoparticles have entered clinical trials for a variety of biomedical applications, including oral drug delivery, diagnostics, plasmonic resonance and photothermal ablation therapy. Preliminary results indicate the safety, efficacy and viability of silica nanoparticles under these clinical scenarios.
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- 2021
37. Oral drug delivery systems using core–shell structure additive manufacturing technologies: a proof-of-concept study
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Jiaxiang Zhang, Michael A. Repka, Pengchong Xu, and Anh Q. Vo
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Drug ,Materials science ,media_common.quotation_subject ,Administration, Oral ,Pharmaceutical Science ,3D printing ,Nanotechnology ,02 engineering and technology ,Proof of Concept Study ,030226 pharmacology & pharmacy ,03 medical and health sciences ,Drug Delivery Systems ,0302 clinical medicine ,Technology, Pharmaceutical ,Acetaminophen ,media_common ,Pharmacology ,business.industry ,021001 nanoscience & nanotechnology ,Research Papers ,Bioavailability ,Drug Liberation ,Solubility ,Proof of concept ,Delayed-Action Preparations ,Printing, Three-Dimensional ,Drug delivery ,Pharmaceutical manufacturing ,Extrusion ,0210 nano-technology ,business ,Oral retinoid ,Tablets - Abstract
Objectives The aim of this study was to couple fused deposition modelling 3D printing with melt extrusion technology to produce core–shell-structured controlled-release tablets with dual-mechanism drug-release performance in a simulated intestinal fluid medium. Coupling abovementioned technologies for personalized drug delivery can improve access to complex dosage formulations at a reasonable cost. Compared with traditional pharmaceutical manufacturing, this should facilitate the following: (1) the ability to manipulate drug release by adjusting structures, (2) enhanced solubility and bioavailability of poorly water-soluble drugs and (3) on-demand production of more complex structured dosages for personalized treatment. Methods Acetaminophen was the model drug and the extrusion process was evaluated by a series of physicochemical characterizations. The geometries, morphologies, and in vitro drug-release performances were compared between directly compressed and 3D-printed tablets. Key findings Initially, 3D-printed tablets released acetaminophen more rapidly than directly compressed tablets. Drug release became constant and steady after a pre-determined time. Thus, rapid effectiveness was ensured by an initially fast acetaminophen release and an extended therapeutic effect was achieved by stabilizing drug release. Conclusions The favourable drug-release profiles of 3D-printed tablets demonstrated the advantage of coupling HME with 3D printing technology to produce personalized dosage formulations.
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- 2021
38. A systematic review on Oral drug delivery as a fast dissolving film to improve therapeutic effectiveness
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Shashikant N. Dhole, Puja S. Wakase, Nilesh S. Kulkarni, and Pratiksha S. Indore
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medicine.medical_specialty ,First pass effect ,Therapeutic effectiveness ,business.industry ,medicine ,Pharmacology (medical) ,Intensive care medicine ,business ,Pharmacology, Toxicology and Pharmaceutics (miscellaneous) ,Oral retinoid - Published
- 2021
39. Poszt-Covidban jelentkező lokalizált és kiterjedt fájdalom kezelési lehetőségei
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V. Edit
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medicine.medical_specialty ,business.industry ,Treatment options ,Chronic fatigue ,Inflammation ,General Medicine ,Disease ,Nociception ,medicine ,Anxiety ,Pain perception ,medicine.symptom ,Intensive care medicine ,business ,Oral retinoid - Abstract
Data on the new coronavirus caused disease and its treatment have been accumulating for more than a year. There are four main disease courses: no or mild symptoms, unavoidable hospitalisation, severe or lethal outcome, and permanent or posthoc manifestations. The last course is usually referred to as post-COVID syndrome. As a part of the acute and post-COVID symptomatology there were published pain perceptions with frequent but heterogeneous localisation. It is practical to classify them by the origin of pain: nociceptive/inflammatory, peripheral neuropathic or central. Additionally, we have to clear which phase is the post-COVID patient in i.e. the patient has the prolonged COVID- or persistent post-COVID syndrome. However, in addition to an acute general inflammatory reaction, a true inflammation of joints and muscles is very rare in the musculoskeletal system. The diffuse musculoskeletal pain, chronic fatigue, generalised anxiety and depressive disposition manifest themselves in both acute and persistent forms. Their explanation is essentially of neurological nature: there are para-infectious “neuro-inflammation”, i.e. neuropathic and central mechanisms in the background. Accordingly, therapeutic options must be chosen while concerning the neuropharmacological action mechanisms of analgesics. Elderly patients at high iatrogenic risk and with multiple co-morbidities may be treated transdermal instead of oral drug administration. © 2021 Literatura Medica Publishing House. All rights reserved.
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- 2021
40. Role of favipiravir in the treatment of COVID-19
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Mangesh Tiwaskar, Hanmant Barkate, Deepak Talwar, Shashank Joshi, Agam Vora, Jalil Parkar, Abdul Ansari, and Saiprasad Patil
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0301 basic medicine ,Microbiology (medical) ,Clinical guidelines ,medicine.medical_specialty ,Coronavirus disease 2019 (COVID-19) ,030106 microbiology ,Viral clearance ,Pharmacokinetic ,Review ,Favipiravir ,medicine.disease_cause ,Antiviral Agents ,lcsh:Infectious and parasitic diseases ,03 medical and health sciences ,0302 clinical medicine ,In vitro ,medicine ,Humans ,lcsh:RC109-216 ,030212 general & internal medicine ,Intensive care medicine ,Pandemics ,Coronavirus ,SARS-CoV-2 ,business.industry ,Pandemic influenza ,COVID-19 ,Lopinavir ,General Medicine ,Amides ,COVID-19 Drug Treatment ,Anti-viral ,Infectious Diseases ,Pyrazines ,Pharmacodynamics ,Ritonavir ,business ,Oral retinoid ,medicine.drug - Abstract
Highlights • Favipiravir is approved by some countries, including India, for COVID-19 treatment. • Favipiravir has shown rapid viral clearance and faster clinical improvement. • Various treatment recommendations include favipiravir for COVID-19 treatment. • Several ongoing clinical trials will further substantiate favipiravir role., The coronavirus disease-2019 (COVID-19) outbreak all over the world has led the researchers to strive to develop drugs or vaccines to prevent or halt the progression of this ailment. To hasten the treatment process, repurposed drugs are being evaluated. Favipiravir is one such oral drug that was approved for new and reemerging pandemic influenza in Japan in 2014 and has shown potent in vitro activity against severe acute respiratory syndrome coronavirus-2. It has a wide therapeutic safety margin indicated by a wide CC50/EC50 ratio for a high dose. From the clinical studies in COVID-19, it has shown rapid viral clearance as compared to lopinavir/ritonavir (LPV/RTV) and superior recovery rate than umifenovir. Overall, favipiravir has shown promising results in clinical studies in China, Russia, and Japan, and more trials are underway in multiple countries, including USA, UK, and India. Recently, treatment guidelines from many countries and some states from India have included favipiravir in the treatment protocol. This review provides insights into the evidence-based evolving role of favipiravir in the management of COVID-19 infection with emphasis on benefits of initiating an early antiviral therapy with special focus on favipiravir, its pharmacodynamic, pharmacokinetic, in vitro, clinical data, and inclusion in the treatment protocols of COVID-19.
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- 2021
41. A pH-sensitive and sustained-release oral drug delivery system: the synthesis, characterization, adsorption and release of the xanthan gum-graft-poly(acrylic acid)/GO–DCFP composite hydrogel
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Bingmi Liu, Guo Zhongqiu, Xiyan Zheng, Yu Liu, Hao Pan, Pan Chunjiao, and Li Li
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Chemistry ,General Chemical Engineering ,Composite number ,02 engineering and technology ,General Chemistry ,010402 general chemistry ,021001 nanoscience & nanotechnology ,01 natural sciences ,0104 chemical sciences ,chemistry.chemical_compound ,Adsorption ,Chemical engineering ,medicine ,Delivery system ,0210 nano-technology ,Xanthan gum ,Oral retinoid ,medicine.drug ,Acrylic acid - Abstract
In this study, graphene oxide (GO) was successfully prepared using the improved Hummers method, and the prepared GO powder was dissolved in distilled water and subjected to ultrasonic stripping.
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- 2021
42. Solid lipid nanoparticles for oral drug delivery
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M. Syed Muzammil, S. Khaleel Basha, R. Dhandayuthabani, and V. Sugantha Kumari
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010302 applied physics ,Drug ,Chemistry ,media_common.quotation_subject ,Nanotechnology ,02 engineering and technology ,Penetration (firestop) ,021001 nanoscience & nanotechnology ,Uniform size ,01 natural sciences ,body regions ,0103 physical sciences ,Drug delivery ,Solid lipid nanoparticle ,Physical stability ,Delivery system ,0210 nano-technology ,Oral retinoid ,media_common - Abstract
Solid lipid nanoparticles (SLNs) are an incredibly resourceful drug delivery platform because of its diverse determination and modifiable lipid materials are making the topic exceptionally captivated in the latest year.The network of the SLNs improves drug stability, maintaining a strategic distance from proteolytic debasement after organization, and releasing the drug in a controlled way, which additionally offer a few advantages over ordinary details, including great physical stability, spherical morphology, uniform size, positive zeta potentials, typical high cell penetration efficiency, core–shell pattern and excipients of GRAS status make the SLNs delivery system all the more promising.Subsequently this fresh methodology of solid lipid nanoparticles hold tremendous promise for reaching at the objective of controlled and site exact for both oral and parenteral drug delivery system. The aim of the article is to review the diverse instrumental techniques have been decorated and oral administration of SLNs is logistically reviewed.
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- 2021
43. Controlled drug release rate and contemporary issues in oral drug delivery formulations
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Ritu Jain, Ajay Kumar Shukla, Rama Shankar Dubey, Ritesh Tiwari, and Aarti Tiwari
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business.industry ,Drug release rate ,Medicine ,General Medicine ,Pharmacology ,business ,Oral retinoid - Published
- 2021
44. Soft-chewable paracetamol tablets by melt granulation method: Formulation and characterization
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Juzaili Azizi, Awis Sukarni Mohmad Sabere, Nur Anis Najlaa Mohd Suhaimi, Mohd Muzamir Mahat, Qamar Uddin Ahmed, and Nazreen Che Roslan
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Drug ,Chromatography ,QD71-142 ,Arabic ,Chemistry ,paracetamol ,media_common.quotation_subject ,Drug administration ,Bioengineering ,Have Difficulty Swallowing ,General Biochemistry, Genetics and Molecular Biology ,language.human_language ,Dosage form ,melt granulation ,RS1-441 ,Granulation ,Pharmacy and materia medica ,language ,Drug release ,Original Article ,General Pharmacology, Toxicology and Pharmaceutics ,Analytical chemistry ,Oral retinoid ,media_common ,chewable tablets - Abstract
Background: Oral drug delivery is the most preferred route for drug administration in the world, with tablets being one of the most common dosage forms. However, some people, particularly children and the elderly, have difficulty swallowing the tablets. Chewable tablets are the dosage form that can address the issue while also providing a valuable masking effect on drug taste, allowing patients to swallow the drugs more easily. Materials and Methods: In this study, the chewable tablets were manufactured using the melt granulation method, which resulted in tablets with a chewy texture. The tablets contained paracetamol as well as Arabic gum, starch, agar, and mannitol. Results: The drug release profiles for the fragmented form showed that 50% of the drug was released within 4 min and 100% was released within 30 min of the dissolution process. The intact form released nearly 90% of the drug within 2 h. Conclusion: Formulation 2 was determined as the best formulation. This tablets' formulation had passed all characterization tests and displayed a moderate hardness and chewy texture.
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- 2021
45. JAK inhibitors: Evolving therapies in rheumatoid arthritis
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Shiva Shankar Jha
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Oncology ,medicine.medical_specialty ,Tofacitinib ,business.industry ,medicine.medical_treatment ,Inflammation ,medicine.disease ,Cytokine ,Internal medicine ,Rheumatoid arthritis ,medicine ,Methotrexate ,In patient ,Tumor necrosis factor alpha ,medicine.symptom ,business ,Oral retinoid ,medicine.drug - Abstract
In rheumatoid arthritis, there has been a paradigm shift from controlling symptoms to controlling the disease progress with abrogation of inflammation. Achieving this remission or very low disease activity has become increasingly possible with USA FDA approved first JAK inhibitor, Tofacitinib in November 2012 (not in Europe). This new small molecule JAK inhibitors are oral drug working intra-cellularly in comparison to TNF? inhibitors targeting a singly cytokine within extra-cellular space confining themselves to cell surface receptors. The second JAK inhibitor Baracitinib approved in Europe in February 2017 and in USA in May 2018 has greater promises. Once daily 2 mg oral dose used either as monotherapy or in combination with methotrexate in moderate to severe active rheumatoid arthritis in adults have provided remission, even in patients who have responded inadequately or are intolerant to one or more DMARDs / bDMARDs. It is a safe second line therapy after methotrexate. In DMARD naive patients, it is likely to become first-line agents Keywords: JAK inhibitor, TNF? inhibitor, NSAID, bDMARD, Methotrexate, Tofacitinib.
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- 2020
46. Biorelevant Dissolution Method Development For Dutasteride/Tamsulosin Hydrochloride Modified Release Capsule - A Prognostic Tool For Oral Drug Absorption
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Devi Thamizhanban, Gampa Tulja Rani, and Kathiresan Krishnasamy
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Chromatography ,010401 analytical chemistry ,Factorial experiment ,Absorption (skin) ,Dutasteride ,030226 pharmacology & pharmacy ,01 natural sciences ,Method development ,0104 chemical sciences ,03 medical and health sciences ,chemistry.chemical_compound ,0302 clinical medicine ,chemistry ,Tamsulosin ,medicine ,General Pharmacology, Toxicology and Pharmaceutics ,Dissolution ,Oral retinoid ,Tamsulosin hydrochloride ,medicine.drug - Abstract
The research work was aimed to develop a biorelevant dissolution method for fixed dose combination containing Dutasteride 0.5 mg in immediate-release form and Tamsulosin 0.4 mg in modified-release form. Mean plasma concentration achieved after oral administration to human under pre-prandial condition are deconvoluted using Wagner-Nelson deconvolution method, to achieve target dissolution profile. The dissolution profile observed using office of generic drugs recommended dissolution media was observed to be faster than the target dissolution profile. Tamsulosin being a modified-release multiparticulate system, biorelevant dissolution method was developed with Fasted state simulated change over dissolution media, using USP Apparatus 3 (reciprocating cylinder). Dutasteride being an immediate-release form, dissolution method was developed with single dissolution media, by extending the dissolution run time upto C max . Dissolution media, media volume and Dips Per Minute (DPM) are optimized by performing full factorial design of experiment. The ANOVA result interprets the biorelevant dissolution media for Tamsulosin part is 250 ml of Fasted state simulated change over dissolution media with 15 DPM, based on desirability factor of 0.7768 and for Dutasteride part 250 ml of pH 6.5 Fasted state simulated intestinal fluids with 7 DPM, based on desirability factor of 0.8988. The regression co-efficient (R 2 ) value of 0.999 and 0.996 demonstrates a very good in-vitro/in-vivo correlation under pre-prandial condition for Tamsulosin and Dutasteride respectively. The developed method shall be used as a predictive in-vitro tool for evaluation of in-vivo performance under pre-prandial condition.
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- 2020
47. Recent Advances in Oral Nano-Antibiotics for Bacterial Infection Therapy
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Jun Zhao, Rong Xu, and Ze-Liang Wu
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Drug ,medicine.medical_specialty ,medicine.drug_class ,media_common.quotation_subject ,Antibiotics ,Biophysics ,Pharmaceutical Science ,Bioengineering ,02 engineering and technology ,010402 general chemistry ,01 natural sciences ,Biomaterials ,Infection disease ,Drug Discovery ,medicine ,Intensive care medicine ,media_common ,business.industry ,Organic Chemistry ,General Medicine ,021001 nanoscience & nanotechnology ,0104 chemical sciences ,Drug delivery ,Delivery efficiency ,Nanomedicine ,Delivery system ,0210 nano-technology ,business ,Oral retinoid - Abstract
Bacterial infections are the main infectious diseases and cause of death worldwide. Antibiotics are used to treat various infections ranging from minor to life-threatening ones. The dominant route to administer antibiotics is through oral delivery and subsequent gastrointestinal tract (GIT) absorption. However, the delivery efficiency is limited by many factors such as low drug solubility and/or permeability, gastrointestinal instability, and low antibacterial activity. Nanotechnology has emerged as a novel and efficient tool for targeting drug delivery, and a number of promising nanotherapeutic strategies have been widely explored to overcome these obstacles. In this review, we explore published studies to provide a comprehensive understanding of the recent progress in the area of orally deliverable nano-antibiotic formulations. The first part of this article discusses the functions and underlying mechanisms by which nanomedicines increase the oral absorption of antibiotics. The second part focuses on the classification of oral nano-antibiotics and summarizes the advantages, disadvantages and applications of nanoformulations including lipid, polymer, nanosuspension, carbon nanotubes and mesoporous silica nanoparticles in oral delivery of antibiotics. Lastly, the challenges and future perspective of oral nano-antibiotics for infection disease therapy are discussed. Overall, nanomedicines designed for oral drug delivery system have demonstrated the potential for the improvement and optimization of currently available antibiotic therapies.
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- 2020
48. Changes in structural and functional connectivity during two years of fingolimod therapy for multiple sclerosis
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Robert J. Fox, Mark J. Lowe, Kenneth Earl Sakaie, Pallab K. Bhattacharyya, H. Li, and Jian Lin
- Subjects
Adult ,Male ,medicine.medical_specialty ,Multiple Sclerosis ,Biomedical Engineering ,Biophysics ,030218 nuclear medicine & medical imaging ,Functional networks ,03 medical and health sciences ,0302 clinical medicine ,Physical medicine and rehabilitation ,medicine ,Humans ,Radiology, Nuclear Medicine and imaging ,Effects of sleep deprivation on cognitive performance ,Fingolimod Hydrochloride ,business.industry ,Multiple sclerosis ,Functional connectivity ,Brain ,Cognition ,Middle Aged ,medicine.disease ,Fingolimod ,Diffusion Tensor Imaging ,Disease Progression ,Female ,business ,030217 neurology & neurosurgery ,Oral retinoid ,Diffusion MRI ,medicine.drug - Abstract
Background Fingolimod, an oral drug, has been reported to reduce relapse rate in multiple sclerosis (MS). However disease progression may still occur in spite of control of inflammation. Functional imbalances within and between cerebral networks associated with disruption of structural and functional network integrity, have been reported in MS. An effective therapy is expected to stabilize such functional network integrity. Objective The purpose of this study was to investigate changes in structural and resting-state functional connectivity of motor and cognitive networks, and associated changes in neurologic scores in MS, during 2 years of fingolimod therapy. Methods Twenty five subjects with MS were recruited for this study. Subjects were scanned with diffusion tensor imaging (DTI) and resting-state functional connectivity MRI (fcMRI) scan protocol at 3 T with 6-month interval over a period of 2 years. Neurologic performance scores of motor and cognitive performances were also obtained. Results DTI measures worsened during the 1st year and then stabilized; any trend of stabilization of fcMRI was delayed until the 2nd year. While motor performance did not change, cognitive performance showed improvement. Several baseline DTI measures correlated with relevant neurologic scores. Conclusion Initial worsening of motor and cognitive network was reported after 1 year of treatment, but seems DTI and fcMRI measures seem to stabilize after around one year fingolimod therapy.
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- 2020
49. Solid Lipid Nanoparticles for Oral Drug Delivery: A Review
- Author
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Iti Chauhan, Pawan Kumar Saraswat, Madhu Verma, Mohd Yasir, Alok Singh, and Manish Gautam
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Chemistry ,Biomedical Engineering ,Medicine (miscellaneous) ,Bioengineering ,02 engineering and technology ,Pharmacology ,021001 nanoscience & nanotechnology ,030226 pharmacology & pharmacy ,body regions ,03 medical and health sciences ,0302 clinical medicine ,Solid lipid nanoparticle ,0210 nano-technology ,Oral retinoid - Abstract
Background: The high molecular weight and increasing lipophilicity of drug face many problems starting from the drug development to formulation and conduction of pharmacological, toxicological and pharmacokinetic studies to its biological application. To overcome this problem, nano-sized formulations are in trend recently. The use of Solid lipid nanoparticles (SLNs) offers new insight into the formulation of the poor soluble and low bioavailable drug. Objective: The study aimed to investigate the literature concerning the development of SLNs for oral drug delivery of poorly soluble drugs, with a view survey the various methods of manufacturing and evaluation of formulation of SLNs and future prospects of SLNs and application of SLNs in oral delivery systems. Conclusion: Oral drug delivery is looking ahead progressively into newer directions due to the realization of various poor performance limiting factors such as reduced drug solubility or absorption, rapid metabolism, high actuation in plasma level of drug and variability caused due to food effect. These play a vital role in disappointing in vivo results, which leads in the failure of the conventional delivery system. Since the last decade, oral drug delivery has taken a new dimension with the increasing application of SLNs as a carrier for the delivery of poorly water-soluble or lipophilic drugs. The site-specific and sustained release effect of the drug is better achieved by using SLNs. This review highlights the various pros and cons, manufacturing techniques, characterization, and future prospects of SLNs in oral drug delivery systems.
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- 2020
50. The Introduction of a New Flexible In Vivo Predictive Dissolution Apparatus, GIS-Alpha (GIS-α), to Study Dissolution Profiles of BCS Class IIb Drugs, Dipyridamole and Ketoconazole
- Author
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Andre Hermans, Michael Wang, Filippos Kesisoglou, Sanjaykumar Patel, and Yasuhiro Tsume
- Subjects
Drug ,media_common.quotation_subject ,Administration, Oral ,Pharmaceutical Science ,02 engineering and technology ,030226 pharmacology & pharmacy ,03 medical and health sciences ,0302 clinical medicine ,In vivo ,medicine ,Dissolution testing ,Solubility ,Dissolution ,media_common ,Chromatography ,Chemistry ,Reproducibility of Results ,Dipyridamole ,Hydrogen-Ion Concentration ,021001 nanoscience & nanotechnology ,Ketoconazole ,Intestinal Absorption ,Pharmaceutical Preparations ,0210 nano-technology ,Oral retinoid ,medicine.drug - Abstract
The physiological pH changes and peristalsis activities in gastrointestinal (GI) tract have big impact on the dissolution of oral drug products, when those oral drug products include APIs with pH-dependent solubility. It is well documented that predicting the bioperformance of those oral drug products can be challenging using compendial methods. To overcome this limitation, in vivo predictive dissolution apparatuses, such as the transfer model, have been developed to predict bioperformance of oral formulation candidates and drug products. In this manuscript we utilize a new transfer-model dissolution apparatus, the gastrointestinal simulator-α (GIS-α), to characterize its behavior in terms of transfer kinetics and pH, assess its reproducibility and adaptability to mimic different transfer conditions, as well as study dissolution of ketoconazole and dipyridamole as model BCS class IIb compounds. Availability of commercially available dissolution transfer systems with similar configuration to compendial dissolution apparatus, may be helpful to simplify and standardize in vivo predictive dissolution methodologies for BCS class IIb compounds in the future.
- Published
- 2020
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