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Background: Musa basjoo pseudostem juice (MBSJ) is a well-known Chinese medicine, and Miao people use MBSJ to treat diabetes. In this work, the active ingredients and molecular mechanism of MBSJ against diabetes were explored. Methods: Anti-diabetic activity of MBSJ was evaluated using diabetic rats, and then the ingredients in the small-polar parts of MBSJ were analyzed by gas chromatography-mass spectrometer (GC-MS). Targets were obtained from several databases to develop the "ingredienttarget- disease" network by Cytoscape. A collaborative analysis was carried out using the tools in Cytoscape and R packages, and molecular docking was also performed. Results: MBSJ improved the oral glucose tolerance and insulin tolerance, and reduced fasting blood glucose, glycosylated hemoglobin, total cholesterol, triglyceride, and low-density lipoprotein levels in the serum of diabetic rats. 13 potential compounds were identified by GC-MS for subsequent analysis, including Dibutyl phthalate, Oleamide, Stigmasterol, Stigmast-4-en-3-one, etc. The anti-diabetic effect of MBSJ was related to multiple signaling pathways, including Neuroactive ligand-receptor interaction, Phospholipase D signaling pathway, Endocrine resistance, Rap1 signaling pathway, EGFR tyrosine kinase inhibitor resistance, etc. Molecular docking at least partially verified the screening results of network pharmacology. Conclusion: MBSJ had good anti-diabetic activity. The small-polar parts of MBSJ were rich in anti-diabetic active ingredients. Furthermore, the analysis results showed that the anti-diabetic effect of the small-polar parts of MBSJ may be the result of multiple components, multiple targets, and multiple pathways. The current research results can provide important support for studying the active ingredients and exploring the underlying mechanism of MBSJ against diabetes.

Red seaweed species Eucheuma cottonii was thought to have potential as an anesthetic agent because it is shown to contain compounds with bioactivity as antimicrobial, antifungal, and also anticancer. There have been no studies regarding the active ingredients of anesthetized. The objective of the study was to examine the potential of E. cottonii extract as a candidate for fish anesthetic based on toxicity, phytochemistry, and active compounds contained in the extract. The stages of research include extraction, toxicity test extracts (BSLT), phytochemical test, quantitative test compound phytochemical results, and the identification of active compounds with LC-MS. Test results showed that E. cottonii extract contains a total of phenols of 4.60 ± 0.06 mg/GAE g which is one presentation of the active ingredient in the extract. The extract had bioactivity with LC50 of 221.71 ± 5.74 μg/mL. E. cottonii extract contained flavonoids compounds and saponins with a consecutive number of 24.48% and 0.22%. The results of identifying active compounds were found in several compounds that had activity asantidepressants or sedatives. E. cottonii extract can be used as a candidate for a fish anesthetic agent.

Elucidating the active components of traditional Chinese medicine (TCM) is essential to understand the mechanisms of TCM and promote its rational use as well as TCM-derived drug development. Recent studies have shown that surface plasmon resonance (SPR) technology is promising in this field. In the present study, we propose an SPR-based integrated strategy to screen and analyze the major active components of TCM. We used Radix Paeoniae Alba (RPA) as an example to identify the compounds that could account for its anti-inflammatory mechanism via tumor necrosis factor receptor type 1 (TNF-R1). First, RPA extraction was analyzed using an SPR-based screening system and the potential active ingredients were collected, enriched, and identified as paeoniflorin and paeonol. Next, the affinity constants of the paeoniflorin and paeonol were determined as 4.9 and 11.8 μM, respectively. Then, SPR-based competition assays and molecular docking were performed to show that the two compounds could compete with tumor necrosis factor-α (TNF-α) while binding to the subdomain 1 site of TNF-R1. Finally, in biological assays, the two compounds suppressed cytotoxicity and apoptosis induced by TNF-α in the L929 cell line. These findings prove that SPR technology is a useful tool for determining the active ingredients of TCM at the molecular level and can be used in various aspects of drug development. The SPR-based integrated strategy is reliable and feasible in TCM studies and will shed light on the elucidation of the pharmacological mechanism of TCM and facilitate its modernization.

The release and dissolution of an active pharmaceutical ingredient (API) from the solid oral formulation into the gastrointestinal (GI) tract is critical for the drug's absorption into systemic circulation. Extended-release (ER) solid oral dosage forms are normally subjected to physical shear and grinding forces as well as pressure exerted by peristaltic movements when passing through the GI tract. The complex physical contraction and sample friction exerted by the GI tract are not simulated well by compendial dissolution methods. These limitations render traditional in vitro dissolution testing unable to discriminate and predict a product's in vivo performance. The objective of this study was to develop a dissolution method that better simulates the GI environment that products are subject to when taken by patients. A newly designed Mechanical Apparatus under GI Conditions (MAGIC) was assembled with a dissolution platform and mechanical capabilities to allow in vitro dissolution testing under sample contractions and friction. The dissolution platform, with medium flow-through configuration, was manufactured by 3D printing. A 60 mg polymer matrix-based ER nifedipine product was tested. To simulate GI physiological conditions during the dissolution testing, the flow rate of the medium, and a combination of mechanical compression with rotation induced sample friction at various rotation frequencies were explored. The polymer matrix-based nifedipine ER formulation used here failed its controlled release functionality in the simulated GI environment under mechanical compression and sample friction. The results showed that the MAGIC system, with flow-through configuration under compression and sample friction, has advantages over compendial methods in testing ER solid oral formulations.

Background: Formulation of topical products for skin delivery that fulfill good formulation criteria has always been a challenge for pharmaceutical scientists. Despite the challenges, gelbased drug delivery offers some advantages such that it is non-invasive, painless, involves avoidance of the first-pass metabolism, and has satisfactory patient compliance. Objectives: In this study, C. odorata gel and quercetin gel (bioactive flavonoid compound) were successfully formulated and compared with placebo and conventional wound aid gel. The chromatographic profiling was conducted to screen the presence of phytoconstituents. Subsequently, all formulated gels were evaluated for physical characteristics and stability. Methods: Reverse Phase High-Performance Liquid Chromatography (RP-HPLC) of C. odorata methanolic leaves extract showed a distinct compound separation at a retention time of 8.4min to 34.8 min at 254nm. All gels were characterised by evaluating their rheological properties, including storage modulus, loss modulus, and plastic viscosity. Besides, texture analysis was performed to measure the firmness, consistency, cohesiveness, and viscosity index of the gels. Results: According to the results, C. odorata gel demonstrated better spreadability as compared to the other gels, which required less work and was found to be favourable for application on the skin. Moreover, C. odorata gel showed no changes in organoleptic properties and proven to be stable after 30 days of accelerated stability study at 40°C ± 2°C with Relative Humidity (RH) of 75% ± 5%. Conclusion: C. odorata gel was found to be stable, reflecting the combination of materials used in the formulation, which did not degrade throughout the study. This work suggests the potential of this gel as a vehicle to deliver the active ingredients of C. odorata to the skin, which can be further explored as a topical application for antimicrobial wound management or other skin diseases study.

Background: The bitter taste and strong irritation of valnemulin hydrochloride limit its wide clinical application in pigs by oral. Method: In order to improve its palatability and residence time in the body, the valnemulin hydrochloride taste-masking granules with sustained-release were prepared by combining solid dispersion based on fatty acid with wet granulation. The formulation was screened by orthogonal test with content, yield, grain size and angle of repose as evaluation indexes. Result: The results showed that the optimal granules were composed of corn starch, sucrose, citric acid, valnemulin hydrochloride and myristic acid at a ratio of 40: 20: 20: 11: 19. The daily feed intake of pigs in the optimum taste-masking granule groups was similar to that of its self-control, and significantly higher than that in the valnemulin hydrochloride active ingredient group, suggesting that the optimum granules have satisfactory palatability. The prepared granules improved the oral bioavailability of valnemulin hydrochloride by 3.04 folds and extended its mean residence time (MRT) by 2.33 folds. Conclusion: The granules developed in this study could obviously improve the palatability and sustained release of valnemulin hydrochloride. The producing method of granules by combining solid dispersion powder with wet granulation can provide ideas for other drugs with poor palatability and a short half-life.

Objective: Salvia Miltiorrhiza (SM) is a traditional Chinese medicine used clinically to treat cardiovascular diseases including atherosclerosis and myocardial infarction. Its therapeutic effect has been confirmed by many clinical and pharmacological studies. However, the optimal formulation of active ingredients in SM for treating cardiovascular diseases remains unclear. In this study, we determined the ratio of the optimal compatibility of SM ingredients DSS, Sal-A, Sal-B, and PAL (SABP）with a uniform and orthogonal optimized experimental design. In addition, we determined the anti-oxidation effect of SABP using Adventitial Fibroblasts (AFs). Methods: By using a combination of uniform and orthogonal designs, we determined the optimal formulation of aqueous extract from SM. MTT assay was used to determine the inhibitory effects of these 4 components of SM on the AFs, which were isolated and cultured from aorta. The reactive oxygen species (ROS) production in AFs was compared before and after SABP treatment. Results: The optimal formulation of these 4 aqueous extracts from SM were 150︰7︰300︰500, and their concentrations were S(1.5×10-4 mol/L), A(7×10-6 mol/L), B(3×10-4 mol/L), and P(5×10-4 mol/L). There were some synergies between these 4 components. Moreover, SABP decreased ROS production in AFs. Conclusion: These findings suggest that SABP inhibits the proliferation and oxidation stress in AFs. The present study provides a new evidence that the efficacy and function generated from optimal formulation of active ingredients in SM are better than lyophilized powder of SM.

Cycloastragenol (CA) is a plant saponin that functions as a telomerase activator, and it has been made as an oral anti-aging supplement and use as active ingredient in topical cosmetic products. The anti-aging performance in cosmetic products have only been evaluated by description of skin appearance, while direct topical penetration of CA across the skin barrier still needs to be confirmed. The objective of this work was to design encapsulation vehicles to deliver CA across the skin barrier using commercially available ingredients through scalable processes, and to prove its topical penetration. Phospholipid vesicles including liposomes, ethosomes, and transethosomes were prepared using soy and sunflower phospholipids and different penetration enhancers, including ethanol and surfactants. The loading capacity of CA was analyzed using high performance liquid chromatography, and the topical penetration of CA was evaluated using Franz diffusion cells with pig skin. Transethosomes using Tween 80, Span 40, or dicetylphosphate as the penetration enhancer showed better CA delivery across the skin barrier than ethosomes or emulsifier α-gels. Results of this work provide evidence that CA encapsulated in phospholipid vesicles can be transported across the skin barrier. These encapsulation systems could be used for the design of CA-containing anti-aging cosmetic products.

The article deals with the problem of cough in bronchopulmonary diseases, in particular, the attention is paid to cough with increased secretion of viscous sputum, i.e., productive cough. It is noticed that derivative of vasicine alkaloid — ambroxol belongs to effective secretolytic mucoactive drugs. A review of researches on ambroxol efficacy in pediatrics is provided, the characteristics of Ambrolitin manufactured by European pharmaceutical company «Sopharma», which active ingredient is ambroxol, are given.

Background Bioactive peptides have been studied in several sources due to their valuable potential in pharmaceutical, food and cosmetic industries. Algae, mussels and fish are examples of marine sources of bioactive peptides. Several biological properties have been identified in these peptides, such as antioxidant, antiatherosclerosis, anticancer, anticoagulant, anti-inflammatory, antihypertensive and antimicrobial activities. Furthermore, peptides derived from marine sources may also be of great interest due to their functional properties, such as solubility, emulsifying and foaming properties, which could be beneficial for industrial application. Scope and approach This paper aims to review information about bioactive peptides isolated from different marine sources, focusing on the different biological activities and functional properties already described, and the different industrial applications exploited. Key findings and conclusions Enzymatic hydrolysis appears as the most used method for peptide production. Bioactive peptides have not been widely used individually, although marine protein hydrolysates are already used with different industrial purposes. However, due to all the bioactivities showed, marine peptides may be of great interest to industrial applications, such as active ingredients for food or cosmetic products; preservatives for food or cosmetics; anti-inflammatory cosmeceuticals; pharmaceutical or nutraceutical products to treat or prevent diseases, with potentially fewer side effects when compared with synthetic drugs. To incorporate peptides in industrial matrices it is essential to guarantee that they will not suffer modifications or lose bioactivity inside new matrices. To empower peptides action in pharmaceuticals, food or cosmetics, they must be able to resist to adverse external factors. Encapsulation may be of one of the most interesting approaches to increase peptides protection.

Designing stimuli-responsive therapeutic scaffolds to deliver hydrophobic chemo drugs with controlled and sustained release at the tumour site would be promising in cancer treatment. In a quest for the stimuli-responsive drug delivery system with sustained release, herein we have fabricated active pharmaceutical ingredient based ionic liquid (IL) based hydrogel with self-healable and injectable properties. The ionic hydrogel makes a localized, long-term co-delivery system with self-healable, injectable, and stimuli-responsiveness. Further, the smart hybrid ionic hydrogel was constructed through encapsulating doxorubicin (DOX) within the 3D matrix of the ionic hydrogel, which responds to an intracellular biological stimulus (e.g., pH and temperature) and releases the DOX in 57 h. Experimental results of IL-IL, IL-DOX interactions are supported through Density Functional Theory (DFT) calculations. In vitro cellular studies revealed that DOX loaded hybrid ionic hydrogel shows a synergistic anticancer effect against MCF-07 cells. These results demonstrate the ability of the ionic hydrogel as a promising candidate for local cancer therapeutics.

Aims: To establish a rapid and simultaneous determination of multiple effective ingredients in anti-cold drugs. Background: Anti-cold drugs are stock medicines at home, and most anti-cold formulations are compound preparations. Although the active ingredients of compound preparations have significant effects on the treatment of colds, the excessive dosage or long-term use can produce a series of adverse reactions, including dependence, liver and kidney function damage, digestive system reaction, blood system damage. Now, there are many mature methods for analyzing the active ingredients of anti-cold drugs. However, these methods may have shortcomings, such as a long analysis time or a small number of analysis components. Objective: Establish a gas chromatography-flame ionization detector method for the simultaneous determination of six active ingredients, including acetaminophen, dextromethorphan hydrobromide, pseudoephedrine hydrochloride, chlorpheniramine maleate, diphenhydramine hydrochloride, and caffeine in anti-cold drugs. Method: After the standard was accurately weighed, dissolved in ethanol, filtered by 0.22 μm membrane and ultrasonically degassed, the gas chromatograph was used for detection. After the actual sample was removed from the coating, ground and crushed, accurately weighed, dissolved in ethanol, filtered by 0.22 μm membrane and ultrasonically degassed, the gas chromatograph was used for detection. Result: The six components can be completely separated within 7.0min. This method has good sensitivity, precision, accuracy and recovery rate. Under the optimum testing conditions, the limit of detection was 0.360-2.50μg/mL, the limit of quantification was 1.20-8.30μg/mL. The calibration curves showed good linearity (R2≥0.9932) over the investigated concentration range between 1.20 and 400μg/mL. The recoveries were 89.2% to 109.2%. The RSD of intra-day precision was less than 1.0%. The RSD of inter-day precision was less than 3.2%. The established method was used to determine the ingredients of three anti-cold drugs on the market, and the results showed that the method can accurately determine the ingredients. Conclusion: The method can quickly and simultaneously determine multiple active ingredients in anti-cold medicines. Compared with the published methods in literature, the proposed method has the advantages of fast, the number of analysis components wide application range, convenience, low cost, etc. It provides a reference method for quality control of active ingredients of anti-cold drugs.

Nanofibrous materials are used in drug delivery as carriers of active ingredients. These can be incorporated into the materials with various electrospinning methods that differ mainly in the way spinning solutions are prepared. Each method affects primarily the encapsulation efficiency and distribution of active ingredients in the materials. This study focuses on the incorporation of octenidine dihydrochloride (OCT) and triclosan (TRI) into nanofibrous materials electrospun from native hyaluronic acid emulsions, dispersions, and blends. OCT had no substantial effect on fiber morphology, which is affected by the solvent system. All OCT encapsulation efficiencies were comparable (approximately 90%). TRI encapsulation efficiencies varied greatly depending on the method used. Merely 3% of TRI was encapsulated when it was spun from a dispersion. Encapsulation efficiency was higher, and TRI was incorporated in clusters when an emulsion was used. The best result was achieved with a blend, in which case 96% of TRI was encapsulated.

The crystallization of active pharmaceutical ingredients (APIs) in matrix-type transdermal patches has implications for the rate of drug absorption through the skin and patch adhesion strength. Therefore, the presence or absence and the degree of API crystallinity must be controlled to guarantee the quality of patches. In this study, the utility of laboratory-level X-ray diffractometers for the detection and analysis of crystalline APIs in transdermal patches was investigated using medical patches of tulobuterol and isosorbide dinitrate. Several matrix-type patches employ a controlled drug delivery system containing intentionally crystallized API. Both benchtop and high-resolution laboratory X-ray diffractometers can detect several characteristic peaks of the APIs in these patches even if the patches are wrapped in an outer bag, although a benchtop model provides peak heights one-seventh to one-fifth that of a high-resolution instrument. An isosorbide dinitrate patch containing an unintentionally crystallized spot was wrapped in an outer bag, followed by measurements using both X-ray diffractometers. For both instruments, several isosorbide dinitrate-derived peaks were detected only at the crystallized spot, although the signal-to-noise ratio was poorer for the benchtop model. These results show that a high-resolution X-ray diffractometer is advantageous for high-detection sensitivity and offers a high degree of freedom of the measurement position on the sample. It was concluded that a laboratory-level high-resolution X-ray diffractometer can be used to examine the crystalline state of APIs in patches inside an unopened outer bag.

Microencapsulation technology is used for providing stability of the active ingredient in food products, which may otherwise render undesirable functionality. Having an improved understanding of the molecular and physicochemical interaction of the active ingredient and material composition is critical to creating such a dynamic system. This chapter describes the factors and the theoretical mechanisms that impact the stability, mass transport, and offer triggered release.

Yeast cells, fundamental in the brewery and bakery industry and present in human nutrition for thousands of years, from an attractive and novel encapsulation matrix. The structure of the yeast cells, which includes the thick and mechanically strong cell wall and the lipid plasma membrane, allows the encapsulation of both hydrophobic and hydrophilic active ingredients and provides high loading capacity. Yeast encapsulation mainly involves whole cells or cell walls of Saccharomyces cerevisiae, although Candida utilis, Kluyveromyces fragilis, Torulopsis lipofera, Endomyces vernalis, and oleaginous yeast (Cryptococcus curvatus) have also been used for encapsulation. The encapsulation process is simple and cost-effective and the yeast capsules prepared provide particular thermo-stability during heat processes, which is extremely beneficial for volatile compounds. Yeast encapsulation is also profitable for stabilization of the active compounds against light or oxygen damage, for along-lasting flavor release, and for targeted oral delivery.

Objective: The objective of this study was to develop and optimize a microflora-triggered colon targeted sustained-release dosage form using Gum Ghatti (GG) and Hydroxypropyl Methylcellulose (HPMC K100). Methods: GG and HPMC K100 were used to prepare microflora triggered colon targeted sustained- release dosage form. For evaluation, two different tablets comprising metoprolol succinate and mesalamine as an active ingredient were used with the objective of developing a platform technology for various categories of drugs. The tablets were coated with Eudragit® L100 and Eudragit® S100 to provide enteric coating and evaluated for hardness, thickness, friability, weight variation, disintegration, and drug content. in vitro release studies for the prepared tablets were carried out mimicking the physiological transit time. Further, the effects of microflora were evaluated using rat cecal content. Results: The in vitro dissolution profile of coated matrix tablets showed that 86.03±0.43% of metoprolol succinate and 80.26±0.67% of mesalamine were released at the end of 12 h. The ex vivo dissolution profile of coated matrix tablets showed that 96.50±0.27% of metoprolol succinate and 92.58±0.39% of mesalamine were released at the end of 12 h in the presence of rat ceacal content. The developed formulation was stable when subjected to the standard ICH stability study conditions. Conclusion: The result of this study showed that gum ghatti together with hydroxypropyl methylcellulose could be successfully used for the preparation of microflora-triggered colon targeted matrix tablets.

Background Flaxseed (Linum usitatissimum L.) oil is an excellent functional oil containing various unsaturated fatty acids, mainly composed of linolenic acid, which is believed to have a variety of beneficial physiological and functional properties. However, the conversion efficiency of linolenic acid in the human body is low, and the research on flaxseed oil lacks a systematic review and evaluation. Scope and approach This review summarizes the research progress of flaxseed oil in recent years, including the main components, extraction and analysis methods of flaxseed oil; the main biological activities of flaxseed oil and its digestion, absorption, bioavailability and application in food; existing problems, possible solutions and prospects for future research. Key findings and conclusions Flaxseed oil is rich in alpha-linolenic acid (ALA) and other active ingredients, but the stability of ALA and its conversion to eicosapentaenoic acid (EPA) and docosahexaenoic acid (DHA) in human body are very low. Improving the stability of ALA can promote its digestion and absorption in the gastrointestinal tract, thereby playing a beneficial role. The establishment of fat emulsion delivery system is an effective way to improve the stability and bioavailability of flaxseed oil. This review could benefit comprehensive understanding the value of flaxseed oil and promote its nutrition research and commercial product development.

The use of PLGA in the pharmaceutical industry has only increased as we move towards more and more advanced delivery carrier systems. The qualities of PLGA like biocompatibility, biodegradability and a tunable degradation and drug release has only helped in keeping up the release requirements desired for various delivery platforms. Fine-tuning the release and degradation rate is gaining more and more attention as researchers keep pushing the boundaries of novel delivery carriers. Various experiments are being performed to understand the degradation behavior of PLGA under various physiological and process-related conditions. The understanding of these parameters has helped formulate various ways in which one can fine-tune the properties that can lead to the release of active ingredients encapsulated within. Various techniques have been tried and tested including changes like chemical modification, physical blending and surface modifications and have found to be effective means of release modulation in delivery systems like parenteral, orals, topicals and tissue engineering scaffolds. In this review, all these experiments and implications thereon have been discussed in detail.

Background: Having various limitations in conventional drug delivery system, it is important to focus on the target-specific drug delivery system where we can deliver the drug without any degradation. Among various challenges that are thrown to a formulation scientist, delivering the drug to its right site, in its right dose, is also an important aim. A focused drug transport aims to extend, localize, target and have a safe drug interaction with the diseased tissue. Objective: The aim of targeted drug delivery is to make the required amount of the drug available at its desired site of action. Drug targeting can be accomplished in a number of ways that include enzyme mediation, pH-dependent release, use of special vehicles, receptor targeting, among other mechanisms. Intelligently designed targeted drug delivery systems also offer the advantages of a low dose of the drug along with reduced side effects which ultimately improves patient compliance. Incidences of dose dumping and dosage form failure are negligible. A focused drug transport aims to have a safe drug interaction with the diseased tissue. Conclusion: This review focuses on the available targeting techniques from experiment to perfection for delivery to the colon, brain, and other sites of interest. Overall, the article should make an excellent read for the researchers in this area. Newer drug targets may be identified and exploited for successful drug targeting.

To relieve the severe economic and social burdens and patient suffering caused by the increasing incidence of chronic wounds, more effective treatments are urgently needed. In this study, we focused on developing a novel sprayable wound dressing with the active ingredient β-1,3/1,6-glucan (βG). Since βG is already available as the active ingredient in a commercial wound healing product provided as a hydrogel in a tube (βG-Gel), the sprayable format should bring clinical benefit by being easily sprayed onto wounds; whilst retaining βG-Gel’s physical stability, biological safety and wound healing efficacy. Potentially sprayable βG hydrogels were therefore formulated, based on an experimental design setup. One spray formulation, named βG-Spray, was selected for further investigation, as it showed favorable rheological and spraying properties. The βG-Spray was furthermore found to be stable at room temperature for more than a year, retaining its rheological properties and sprayability. The cytotoxicity of βG-Spray in keratinocytes in vitro, was shown to be promising even at the highest tested concentration of 100 μg/ml. The βG-Spray also displayed favorable fluid affinity characteristics, with a capacity to both donate and absorb close to 10% fluid relative to its own weight. Finally, the βG-Spray was proven comparably effective to the commercial product, βG-Gel, and superior to both the water and the carrier controls (NoβG-Spray), in terms of its ability to promote wound healing in healing-impaired animals. Contraction was found to be the main wound closure mechanism responsible for the improvement seen in the βG-treatment groups (βG-Spray and βG-Gel). In conclusion, the novel sprayable βG formulation, confirmed its potential to expand the clinical use of βG as wound dressing.

This present work describes the possible advantages of carboxymethylcellulose (CMC) blending with ball-milled glutinous starch (BMGS) on the modification of release and penetration of model water-soluble active ingredient, lidocaine hydrochloride, from the blended matrix. The 20–67% CMC mass containing CMC-BMGS matrices were fabricated by casting the aqueous dispersion of CMC-BMGS onto the tray and oven-dried. BMGS and CMC were compatible as revealed by SEM and ATR-FTIR. Irrespective of the CMC mass, all CMC-BMGS matrices showed comparable matrix mass, thickness, moisture content, moisture absorption as well as mechanical and mucoadhesive properties. The surface pH of CMC-BMGS tended to increase with the CMC mass. Depends on CMC mass, matrix properties, release, and penetration rates were modulated significantly. CMC had shown a substantial role in the swelling and erosion behaviors of BMGS films, and thus modulated the release and penetration significantly. The release and penetration mechanisms of active ingredient from the CMC-BMGS matrices were Fickian diffusion-controlled, with rates of release and penetration ranging from 2.05 ± 0.21 to 7.55 ± 1.08%/min½, and from 3.48 ± 0.28 to 8.04 ± 0.64 μg/cm2/min½, respectively. The capability of CMC-BMGS matrices as mucoadhesive delivery systems to provide sustained delivery of water-soluble active ingredients was disclosed.

Platform tests are usually simple and rapid quality control tests which serve as a basis for accepting, setting aside or rejecting raw milk. Some of the rapid antibiotic residues test kits available in the Kenyan market include: Delvo test Fast BL, Delvo Sulphadiazine Penicillin No Tablet (SPNT), Mtusbio Beta-lactam BLQ Rapid Test Kit and Ringbio beta-lactam, tetracycline, sulfa drugs, BTS 3 in 1 TriTest S. Ndungu Antibiotic residues (NAR) is a colour comparison test that is simple, rapid and does not require electric power in its analysis procedure. This study compared these four rapid antibiotics tests with novel NAR test method in terms of sensitivity and specificity. A total of 28 samples were prepared; 8 milk samples without residues were spiked with milk known to have beta-lactam residues while 10 had no residues and 10 had known beta-lactam (benzyl penicillin) residues. The four analysis methods were carried out as described in their technical bulletins and manuals. For the NAR test, 50 mg of its active ingredient was mixed with 3 ml of milk and colour change observations made. The sensitivity and specificity of the NAR test was found to be 66.7 and 100% respectively while for all the other four tests, sensitivity and specificity was established to be 100% for each. The Kappa coefficient was 0.5882 which indicates moderate agreement, between NAR test method and the other test methods, according to Landis-Koch scale. The odds ratio exhibited positive association between the NAR test and the four methods. NAR test is best applicable at the milk collection routes or farm level before bulking for transportation. Key words: Antibiotic residues, rapid test kit, beta-lactam, beta-lactamase, NAR test.

INTRODUCTION This study investigated the role of natural polymers as moisturizers with low toxicity and biodegradability in the cosmetic and pharmaceutical industries. We isolated a polysaccharide extract from Dendrobium candidum (D. candidum) and determined its efficacy in skin hydration when used as an active cosmetic ingredient. METHODS The molecular weight distribution of D. candidum polysaccharides was analyzed via gel permeation chromatography (GPC). We performed real-time reverse transcription PCR (RT-PCR) and western blotting assays to investigate the physiological mechanism of the polysaccharides extracted from D. candidum (PDC). Based on in vitro data, the efficacy of PDC in improving skin condition was tested on the face of 21 volunteers. RESULTS The expression of filaggrin (FLG), caspase-14, and bleomycin hydrolase, which are the major components contributing to skin hydration, was significantly increased in the PDC-treated group. Further, the PDC upregulated the mRNA expression of occludin and claudin-1, which play a key role in epidermal barrier function. In addition, a topical application of PDC markedly increased skin hydration and improved trans-epidermal water loss (TEWL) and skin elasticity after 2 weeks. CONCLUSIONS It is the first study reporting the efficacy of PDC-mediated FLG mechanism associated with positive skin hydration. PDC can be used as an active ingredient in moisturizers. Long-term application of PDC-based moisturizers may result in significant improvement in elasticity and barrier function.

Introduction. Intranasal delivery of in situ gel-forming systems is a complex but promising direction. Due to the high cost of developing a new chemical object or genetically engineered modification of biological molecules, pharmaceutical companies are focusing on developing technologies for new delivery systems for existing active pharmaceutical ingredients to improve their effectiveness and bioavailability. In situ systems for intranasal delivery, due to increased viscosity and mucoadhesion to the nasal mucosa, allow overcoming mucociliary clearance and ensuring complete absorption and prolonged release of drugs.Text. The article discusses the main advantages of intranasal in situ delivery systems shown in preclinical studies, as well as approaches to the technology of obtaining and standardization of these systems. The results of scientific research in this field over the past 15 years are summarized, the most promising polymers for creating thermoreversible and pH-sensitive compositions are identified, and modern methods for evaluating the sol-gel transition in situ are analyzed.Conclusion. The use of in situ systems for intranasal administration allows providing a high targeting of the delivery of synthetic and biological molecules to the brain. Currently, numerous pharmacokinetic and pharmacodynamic preclinical studies confirm the effectiveness of such systems, as well as their safety. Thermoreversible commercially available and directionally synthesized polymers (poloxamer 407, PLGA, NIPAAm, etc.), as well as chitosan, remain the most popular for the design of in situ delivery systems. In vitro and ex vivo methods with mucosa and artificial nasal fluid are widely used to assess the parameters of in situ gelation, but to increase the reproducibility of the methods and improve the correlation in vitro/in vivo, it is recommended to conduct modeling of the nasal cavity. Developing the technology and methods of screening of intranasal reversible systems will help to get closer to clinical trials and the entry of these delivery systems into the global pharmaceutical market.

The development of metastable form crystals of active pharmaceutical ingredients is an effective method to improve the bioavailability of poorly soluble drugs, while the thermodynamic instability p...

An efficient protocol for assessing both the chemical and physical stability of cocrystalline forms of active pharmaceutical ingredients (APIs) is proposed. In this protocol, the cocrystalline material is used to prepare two standard formulations, mimicking wet granulations, to make low-dose tablets. After designed stress testing at a range of temperatures and RH conditions, degradant formation is modeled from the data using ASAPprime® to determine if the tablets have a minimum of a one-year shelf-life (25 °C/60% RH open). When the cocrystals provide a kinetic solubility enhancement over the un-complexed API, a physical assessment of the cocrystal stability is carried out using the same tablets at selected stress conditions. For this assessment, kinetic solubility (where the amount of buffer used to dissolve the tablet is adjusted to completely dissolve the cocrystalline form but leave most of the un-complexed form out of solution) changes are used to indicate whether there is a significant risk for physical instability on long-term storage. This process was exemplified using model cocrystals of APIs.

The fat obtained from the ripened seeds of Diploknema butyracea is widely used as a vegetable oil in rural areas of Nepal. This study was aimed for the physicochemical evaluation (acid value, iodine value, saponification value, peroxide value, ester value, pH, and liquefaction point) of the Diploknema butyracea seed extract (chyuri fat) and the formulation of 2% w/w ketoconazole ointment by using it as a base. All the physicochemical parameters were determined quantitatively by using the method of Indian Pharmacopoeia (IP), volume-I. By fusion method, 3 different formulations F-A, F-B, and F-C were prepared, in which different proportions of chyuri fat, polyethylene glycol 6000 (PEG 600), Tween 80, and propylene glycol were used as an ointment base. Various quality parameters such as spreadability, extrudability, viscosity, smoothness, pH, average fill weight, assay, content uniformity, accelerated stability, and drug release profiles were determined. HPLC was used for the determination of ketoconazole content in the ointment formulations. Physicochemical evaluation of the chyuri fat ensured its suitability for industrial purpose. The active ingredient release profile of formulations F-A (87.71%), F-B (88.89%), and F-C (91.09%) after 5 hours were within acceptable range along with other parameters. Assay of the formulations F-A, F-B, and F-C were reported to be 103.01, 107.9, and 102.45%, respectively. Overall, evaluation of the formulation F-A, prepared by using chyrui fat only, gave satisfactory results and most of the parameters were statistically similar (p>0.05) to the F-B and F-C formulated by incorporating a certain proportion of synthetic base. Thus it can be concluded that chyuri fat can be the best alternative to replace the expensive synthetic base.

Hair is one of the distinguishing characteristics of mammals, and it serves a variety of functions including protection from external forces, production of sebum, apocrine sweat, and pheromones. However, the unwanted hair growth is always a worrying aspect among teenage girls and women. The present study is the need of selecting herbal depilatories over chemical depilatories due to its high efficacy, safety and lesser side effects. The various types of hair removal process, herbs showing depilatory action and their composition for herbal cream are studied. According to statistics, the use of depilatories has been steadily expanding, and the global hair removal products market was valued at USO 2.2 billion in 2018, with a CAGR of 5.5 percent predicted from 2019 to 2025. Depilatories are the cosmetic preparation which is used to remove the hair from skin, in chemical depilatories the main active ingredients are salts of thioglycolic acids, sulphides and stannites which can produce rashes and side effects on long time usage, whereas herbal depilatories include active ingredients like Turmeric, Indian neetle, Neem, Tanner’s cassia, Apple cider vinegar, Paw-paw extract etc. which are tremendously safe to use. Hence in this study we have been discussed about importance of few folklore herbal medicine and preparation methods of both chemical and herbal depilatories.

Accurate and reliable feeding of small quantities of powder is crucial in many industries. It is particularly true in the case of pharmaceutical manufacturing. First, the exact dosage of highly potent active pharmaceutical ingredients (APIs) is essential. Second, due to the shift towards continuous manufacturing, processing agents must be supplied continuously. Last, with regard to personalized medicine products, small doses of API have to be processed with high flexibility. In all these applications, a few grams of powder or less per hour have to be fed, which makes processing very challenging. The common route of pre-blending causes additional effort in processing and quality control compared to direct continuous feeding, while material properties influence the performance of conventional feeders with conveying screw elements. In this study, a novel micro-feeding system based on active volumetric displacement is investigated and compared to commercial LIW feeders of various scales. In the micro-feeder, the powder is filled into a cylindrical cartridge and pushed towards the process by a piston in a controlled manner. Tests are carried out with a free-flowing grade of lactose and croscarmellose sodium as an example of cohesive powder. At feed rates of a few grams per hour, for the investigated materials, the system has at least the same performance as conventional feeders at significantly higher feed rates. Especially at low feed rates, less fluctuations are obvious and accuracy and precision of the micro-feeder are at the same level as for the established feeding technology at rates ten times higher. For the two types of investigated materials (free-flowing and cohesive), the micro-feeding system shows similar or better performance than conventional and commercially applied LIW feeders. The technology offers the potential for highly accurate, continuous feeding in the low-dose range.

The emerging contaminant 4-nonylphenol is an active ingredient in many surfactants. Though 4-nonylphenol has been reported in Mexican waterbodies, no stringent law is available to establish its per...

Diversity of pesticide discovery provided a solution to resistance. Here, we presented a strategy of azo-incorporating to promote the diverse developments of fungicide. A series of novel fungicides were synthesized by incorporating azobenzene derivatives into fluxapyroxad. Much better in vitro fungicidal activity increases for compound 9d were observed compared to the positive control, fluxapyroxad against Botrytis cinerea and Rhizoctonia solani. Compound 9d (IC50 = 0.03 μM) also had a great enzyme-inhibiting activity increase toward succinate dehydrogenase in comparison with fluxapyroxad (IC50 = 4.40 μM). A comparatively equivalent biological activity was observed between compounds 8a and 9d. SEM analysis helped us to observe clearly the morphology of the fungi before and after active ingredient delivery. Our results of molecular docking analysis, fluorescence quenching analysis, and enzymatic assays demonstrated that compound 8a and 9d act on SDH. An increase in inhibitory activity could be occurring after incorporation of azobenzene, which provided a new strategy for molecular design in pesticide discovery.

Background: In the growing environmental concern use of natural products, efficient processes and devices are necessary. Solid-Liquid extraction of active Ingredients from Plant materials is one of the important unit operations in Chemical Engineering and need to be enhanced. Objectives: Since, these active ingredients are firmly bound to the plant cell wall membrane, which pose mass-transfer resistance and need to get detached through the use of suitable process intensification tools such as ultrasound and suitable devices. Therefore, detailed analysis and review is essential on development made in this area through Publications and Patents. Hence, the present paper illustrates the development of ultrasound assisted device for solid-liquid extraction are presented in this paper. Methods: Advantages such as % Yield, Reduction in extraction time, use of ambient conditions, better process control, avoidance or minimizing multi stage extraction could be achieved due to the use of ultrasound in extraction as compared to conventional processes. Conclusions: Use of ultrasound to provide significant improvements in the extraction of Vegetable tannins, Natural dyes for application in Leather processing has been demonstrated and reported earlier. These enhancement could be possible through various effects of ultrasound such as better flow of solvents through micro-jet formation, mass transfer enhancement due to rupture of plant cell wall membranes through acoustic cavitation, better leaching due to micro-mixing and acoustic streaming effects. This approach would minimize material wastage; thereby, leading to eco-conservation of plant materials, which is very much essential for better environment. Hence, various methods and design for application of ultrasound assisted solid-liquid extractor device are necessary.

Because of its rich active ingredients, Chinese date is one of the key plants in the study of natural products. Polysaccharide is an important active ingredient in Chinese date. Recent studies have shown that Chinese date polysaccharide has good antioxidant activity, anti-tumor activity, anti-inflammatory activity, immunomodulatory activity and hepatoprotective effect. Herein, the research progress on the extraction, purification, structure, activity and derivatization of Chinese date polysaccharides was reviewed. Several common extraction methods of Chinese date polysaccharide were compared, the new extraction methods of Chinese date polysaccharide were discussed, the purification methods of Chinese date polysaccharide were summarized, and the structure and activity of Chinese date polysaccharide were mainly discussed. Suggestions for structural reconstruction were put forward. The results provided a reference for the follow-up research, production and application of Chinese date polysaccharide, and laid a foundation for the development of Chinese date polysaccharide-related foods.

A practical and efficient two-step synthetic process for the preparation of (R)-(-)-denopamine has been developed. The key step asymmetric hydrogenation was conducted at mild temperature (60 ​°C) under a hydrogen pressure of 50 ​atm by using Ir/f-amphox as catalyst at low catalyst loading (S/C ​= ​20 ​000). Under the optimized condition, the desired product (R)-(-)-denopamine was obtained with 70% total yield and > 99.9% ee after crystallization. The pilot-scale experiment has been performed at 500 ​g level, showing great potential for the production of high quality active pharmaceutical ingredient (API).

Objective: The present paper aims to evaluate the quality of five different brands (local and imported) of oral film-coated tablets of generic Amlodipine besylate 5 mg marketed in Sana`a-Yemen, through physiochemical parameters. Methods: Different physicochemical parameters, including the uniformity of tablet weight, hardness, thickness, disintegration time, and an assay of active ingredients, were conducted to validate the quality of generics Amlodipine Besylate 5 mg according to USP specification. Results: From the obtained results, it was observed that all the brands of Amlodipine Besylate 5 mg have passed the tests and met the specifications of USP. Results of weight variation, hardness, thickness, and disintegration time were ranged from-3.8 % to+5.13 % to-1.25 % to+3.25 %, 5.06±0.31 to 13.21±1.5, 2.682±0.04 to 3.676±0.01 and 25 s to 2 min: 30 s, respectively. The dissolution test and the assay results of all the brands are also ranged within the acceptable label claim 93.7±2.24 to 98.4±0.85 and 93.22±0.38 to 100.15±0.33, respectively. However, there is no relation was found between the disintegration time and the dissolution test. Conclusion: According to the finding, all the selected Amlodipine Besylate 5 mg brands are met pharmacopeia standards and USP specifications. Therefore, the local and imported Amlodipine Besylate 5 mg can be used safely to get the desired therapeutic efficiency.

One of the tablet manufacturing processes using the wet granulation method is the process of mixing the active ingredient granules, fillers, binders and pelicans. The parameters of the mixing process are important to study because they will affect the physical properties of the tablet. This study studied the effect of the variable duration and the size of the mixing cycle on the physical properties of paracetamol tablets using a 2D double mixer. The results of the analysis and testing showed that the variation of mixing time and the size of the rotation had a significant effect on the flow properties of the granules and the hardness of the tablets. In addition, the optimal parameter results to obtain optimal tablet hardness occurred at 15 minutes of mixing process and 50 rpm of rotation.

BACKGROUND Echinacea is a perennial and herbaceous herb containing the most active phenolic compounds and valuable antimicrobial and antioxidant content, such as chicoric acid, which increases the body immune function. The root of this plant is mainly used in pharmaceutical fields to treat inflammation, kidney infections and colds. In the present study, we investigated the drying of echinacea root in an infrared dryer with airborne ultrasonic pretreatment aiming to determine shrinkage, color changes, extraction, total phenolic content, flavonoid content and radical inhibition of 2,2-diphenyl-1-picrylhydrazyl (DPPH). The experiments were performed in an infrared dryer at three temperature levels of 40, 45 and 50 °C, with ultrasonic pretreatment at frequencies of 2000, 3000 and 4000 Hz and a time duration of 20, 40 and 60 min in three replications. RESULTS Shrinkage and color changes of the samples varied in the range 27.2-6.3% and 39.82-39.64%, respectively. According to all of the evaluated physical and chemical factors, the optimal conditions for echinacea root processing were a drying temperature of 40 °C, a frequency of 3000 Hz and an ultrasound duration of 60 min, in which case shrinkage was 3.35% and color changes were 38.25%. Total phenolic content was 27.41 mg g-1 , flavonoid content was 39.36 mg g-1 and DPPH radical inhibition was 34.87%. CONCLUSION Therefore, the use of airborne ultrasound pretreatment demonstrates increased chemical properties compared to the optimal state when drying the echinacea root with an infrared dryer by 54/21-81/64%. Hence, ultrasound pretreatment preserves the quality and quantity of active ingredients in the therapeutic root of Echinacea. © 2021 Society of Chemical Industry.

Objectives Combinatorial drugs are among the leading pharmacotherapeutic agents, including those used for the treatment of herpetic infections, which require complex treatment. We have developed a soft dosage form of ointment, which includes acyclovir and miramistin, which have antimicrobial, anti-inflammatory, and local immunoadjuvant activity. The study aimed to investigate the rheological properties of ointment bases in order to substantiate the composition of a soft dosage form with antiviral effect using the active ingredients miramistin and acyclovir. Materials and methods The object of the study was to determine the heterogeneous and homogeneous composition models of the bases made using a wide range of excipients. Structural and mechanical studies were performed using the "Rheolab QC" rotary viscometer by Anton Paar (Austria) with coaxial cylinders CC27/S-SN29766. The rheological parameters were investigated at a temperature of 25°C±0.5°C. The samples were thermostated using a thermostat MLM U15c. The batch of sample weighing about 15.0±0.5 g was placed in the container of an external stationary cylinder. The required temperature of the experiment was set and the thermostating time was 20 min. The device is equipped with RheoPlus 32 V3.62 software. Results The rheological behavior of the model compositions was analyzed in terms of indicators, such as yield strength, hysteresis square, coefficients of dynamic flow, and mechanical stability. It was found that all samples have a non-Newtonian pseudoplastic type of flow. The model of spreading optimums was used to evaluate consumer properties. According to the rheological parameters, it is advisable to use the sample based on paraffin and vaseline oil for further research. Conclusion The findings from this study will be relevant in the development of the soft dosage form for the treatment of herpes viral diseases.

This article takes a step forward in understanding the mechanisms involved during the preparation and performance of cross-linked high-drug-loading (HDL) amorphous solid dispersions (ASDs). Specifically, ASDs, having 90 wt % poorly water-soluble drug indomethacin (IND), were prepared via in situ thermal cross-linking of poly(acrylic acid) (PAA) and poly(vinyl alcohol) (PVA) and thoroughly evaluated in terms of physical stability and in vitro supersaturation. Results showed that HDL ASDs having excellent active pharmaceutical ingredient (API) amorphous stability and prolonged in vitro supersaturation were prepared by fine tuning the cross-linking procedure. Unraveling of the processes involved during ASD's formation shed light on the significant role of the cross-linking conditions (i.e., temperature and time), the physicochemical properties of the API, and the hydrolysis level of the cross-linker as key factors in modulating ASD's stability. In-depth analysis of the prepared systems revealed the (1) reduction of API's molecular motions within the cross-linked polymeric networks (through API's strong spatial confinement), (2) the structural changes in the prepared cross-linked matrices (induced by the high API drug loading), and (3) the tuning of the cross-linking density via utilization of low-hydrolyzed PVA as the major mechanisms responsible for ASD's exceptional performance. Complementary analysis by means of molecular dynamics simulations also highlighted the vital role of strong drug-polymer intermolecular interactions evolving among the ASD components. Overall, the impression of the complexity of in situ cross-linked ASDs has been reinforced with the excessive variation of parameters investigated in the current study, offering thus insights up to the submolecular level to lay the groundwork and foundations for the comprehensive assessment of a new emerging class of HDL amorphous API formulations.

Active Pharmaceutical Ingredients (APIs) are the ingredients in pharmaceutical, personal care products, and agriculture that are biologically active, causing detrimental effects to humans and the environment. The detection of pharmaceutical contaminants in Malaysian rivers suggests a high risk for the contaminants to reach tap water since the river is the primary source of water intake points for all drinking water treatment plants and the inability of these plants to treat emerging pollutants like the APIs. In response to the issue, this study aims to evaluate selected documents on the characteristics and properties of pharmaceutical contaminants that are harmful and examine how the Malaysian legislative framework could prevent the contaminants in tap water. A systematic search was carried out on selected pharmaceutical-related documents, and content analysis was conducted to discover patterns and ideas within the selected documents. The finding of this study demonstrates that Malaysian legislative framework has the capacity and capability to carry out a risk mitigation on APIs as well as the insertion of selected types of pharmaceutical contaminants as new parameters. This study’s findings provide insights for the improvement of the Malaysian legislative framework against the potential risks of APIs contamination of our tap water.

Indonesia, which is located in the tropics, causes people's skin to easily experience premature aging and tan. Most of these cosmetic products contain dangerous synthetic chemicals. For this reason, cosmetic products with natural active ingredients or phytocosmetics that are effective and safe to use need to be developed. One of the typical natural plant plants from South Kalimantan that has the potential to be developed as a cosmetic preparation is Sungkai (Peronema canescens Jack). The aim of the study was to determine the antioxidant activity and sunscreen activity of Sungkai leaves. The method used for the determination of antioxidant activity is the DPPH method using a uv-vis spectrophotometer and for the determination of sunscreen activity using a uv-vis spectrophotometer. The results showed that the P. canescens plant extract contained anthraquinones, flavonoids, saponins, tannins, and phenols. P.canescens plants have an Inhibitory Concentration 50 (IC50 ) of 42.219±19.440 ppm and have sunscreen activity with spf (Sun Protecting Factor) values ??with concentrations of 600 ppm, 400 ppm, 200 respectively as follows: 24±0.31; 16±0.34; and 8±0.3. The conclusion of this study Sungkai (Peronema canescens Jack) has antioxidant activity and has sunscreen activity so that it has the potential to be developed into natural skin care.

Pesticides are commonly used in modern agriculture and are important for global food security. However, postapplication losses due to degradation, photolysis, evaporation, leaching, surface runoff, and other processes may substantially reduce their efficacy. Controlled-release formulations can achieve the permeation-regulated transfer of an active ingredient from a reservoir to a target surface. Thus, they can maintain an active ingredient at a predetermined concentration for a specified period. This can reduce degradation and dissipation and other losses and has the potential to improve efficacy. Recent developments in controlled-release technology have adapted the concepts of intelligence and precision from the pharmaceutical industry. In this review, we present recent advances in the development of controlled-release formulations and discuss details of the preparation methods, material improvements, and application technologies.

Background : Lime leaves contain flavonoids, tannins, and saponins. This content is known to have activity as an antibacterial and protective of gums and teeth. Based on these activities, lime leaves can be developed as an active ingredient in gel toothpaste preparations. In the manufacture of gel toothpaste, the component that plays an important role is the gelling agent. Purpose: In this study, a variation of the gelling agent Carbomer 940 will be used to make a gel toothpaste with lime leaf extract. Methods: The independent variable used is Carbomer 940 with a variation of 3 formulas, namely 0.6%; 1.2%; and 1.8%. The evaluations carried out on gel toothpaste were organoleptic, homogeneity, pH, adhesion, spreadability and pH. Data analysis was carried out with SPSS software to see the differences between each formula. Results: The results showed that the formula 1-3 was homogeneous with a clear, homogeneous color, and a characteristic smell of menthol with a pH range of 5.85-7.49; spreading area 20.60-29.91 cm2, adhesion 6.01-35.1 seconds. The results of statistical tests with one-way ANOVA obtained a significant difference between each formula.

Background: Calcium hydroxide is the gold standard medicament for root canal treatment. Enterococcus faecalis, the primary cause of intraradicular persistent endodontic infection, is often identified even after endodontic treatment. Thymoquinone, an active ingredient of Nigella sativa, has an antimicrobial effect on both gram-negative and positive bacteria, including E. faecalis. Purpose: This study aimed to evaluate the inhibitory effect of calcium hydroxide combined with Nigella sativa extract and determine the best ratio for the combined material. Methods: This is an experimental study comprised of six groups (n = 4 per group) based on the material and its ratio, namely; (1) calcium hydroxide; (2) Nigella sativa extract; and groups of the combination of calcium hydroxide and Nigella sativa extract with a ratio (3) 70:30, (4) 50:50, (5) 30:70, (6) 10:90. The inhibitory effect against E. faecalis was evaluated by the agar well diffusion method in Muller–Hinton agar. Observation of the inhibitory zone was performed on the first, third, and seventh days. The collected data were analysed by a one-way ANOVA and LSD post hoc test. Results: Calcium hydroxide has the highest inhibitory effect, and the combination of Nigella sativa extract with calcium hydroxide ratio 50:50 was second. The inhibitory zone of these two groups was significantly higher than in any other group (p

Hydroxyanthraquinones from plants have been used as both medicinal active ingredients and adulterants in slimming food supplements. Although sensible doses of certain natural hydroxyanthraquinones for laxative effects are generally safe in the short term, chronic intake has been related to tumorigenic, carcinogenic, and genotoxic effects. However, an increasing number of researchers are reporting the antiproliferative properties of the same ingredients in cancer cells, pointing towards a potential nutraceutical value for cancer prevention. Previous studies have evaluated anthraquinones’ anti-proliferative activity against various tumour cell lines and bioavailability in Caco-2 cells. However, there are scarce data about both their cytotoxicity in the later cell line and long-term stability. Therefore, this study will check the purity of several ‘aged’ samples using mutually complementary analytical techniques such as HPTLC and NMR assays as well as evaluate the anti-proliferative activity of the purest of these samples using the Caco-2 cell line. The chromatographic and spectroscopic analyses confirmed the long-term stability of those compounds, and their cytotoxic activity resulted in chrysazin (15 µg/mL) &gt, catenarin (27.29 µg/mL) &gt, rhein (49.55 µg/mL) &gt, helminthosporin (52.91 µg/mL) &gt, aloe-emodin (55.34 µg/mL). Our succinct review of the cytotoxicity of these compounds afforded two results: that this is the first clear report for catenarin being active in colon cancer cells and that this class of compounds needs to be better studied to clearly evaluate their benefit/risk profile in regard to both new chemo preventative nutraceuticals and anticancer therapies.

The effective atomic number, electron density and mass attenuation coefficient of some selected active pharmaceutical ingredients such as Diclofenac Sodium, Femotidine, Alprazolam, Amiodar, Amiodarone, Ciprofloxacin, and Nimesulide have been calculated over the energy range from 1 keV to 100 GeV for total and partial photon interactions by using WinXCom. The obtained data shows that the change in mass attenuation coefficient and electron density varies with energy and chemical composition of the active pharmaceutical ingredients (API’s) in drugs. The results in the variation of photon interaction with energy and effective atomic number of the API’s in drug are shown in the logarithmic graphs.

The current analytical exploration illustrated developing a reversed-phase high-performance liquid chromatography (RP-HPLC) technique and consequent substantiation for analyzing lamotrigine (LAM) active pharmaceutical ingredient (API) using a Quality-by-design (QbD) approach (Central Composite Design), in bulk product as well as in the tablet formulations. In this experiment, based on systematic scouting, four key components (viz., mobile phase, column, flow-rate, and wavelength) were studied by the RP-HPLC method. 13 experimental runs were done with acetonitrile (ACN) (40-60% v/v) having flow-rate in the range 0.8 mL/min to 1.2 mL/min. The proposed analytical method was thoroughly corroborated in terms of ruggedness linearity, robustness, accuracy, and precision in accordance with ICH guideline Q2A and ICH guideline Q2B. Under the optimum chromatographic environment; Intersil C8 column of 250 mm length, 4.6 mm (i.d.); 20 μL injection volume; and mobile phase ACN: Methanol (60:40 v/v), a retention time of 2.542 min was noticed at 220 nm detection wavelength. The method was found to be extremely reproducible, accurate, linear, precise, robust, and economically adequate to execute the estimation. The intended analytical technique was thoroughly assessed through statistical tools and could be an imperative concern for the habitual scrutiny of LAM in bulk products and its formulation.

Active food packaging materials that are sustainable, biodegradable, and capable of precise delivery of antimicrobial active ingredients (AIs) are in high demand. Here, we report the development of novel enzyme- and relative humidity (RH)-responsive antimicrobial fibers with an average diameter of 225 ± 50 nm, which can be deposited as a functional layer for packaging materials. Cellulose nanocrystals (CNCs), zein (protein), and starch were electrospun to form multistimuli-responsive fibers that incorporated a cocktail of both free nature-derived antimicrobials such as thyme oil, citric acid, and nisin and cyclodextrin-inclusion complexes (CD-ICs) of thyme oil, sorbic acid, and nisin. The multistimuli-responsive fibers were designed to release the free AIs and CD-ICs of AIs in response to enzyme and RH triggers, respectively. Enzyme-responsive release of free AIs is achieved due to the degradation of selected polymers, forming the backbone of the fibers. For instance, protease enzyme can degrade zein polymer, further accelerating the release of AIs from the fibers. Similarly, RH-responsive release is obtained due to the unique chemical nature of CD-ICs, enabling the release of AIs from the cavity at high RH. The successful synthesis of CD-ICs of AIs and incorporation of antimicrobials in the structure of the multistimuli-responsive fibers were confirmed by X-ray diffraction and Fourier transform infrared spectrometry. Fibers were capable of releasing free AIs when triggered by microorganism-exudated enzymes in a dose-dependent manner and releasing CD-IC form of AIs in response to high relative humidity (95% RH). With 24 h of exposure, stimuli-responsive fibers significantly reduced the populations of foodborne pathogenic bacterial surrogates Escherichia coli (by ∼5 log unit) and Listeria innocua (by ∼5 log unit), as well as fungi Aspergillus fumigatus (by >1 log unit). More importantly, the fibers released more AIs at 95% RH than at 50% RH, which resulted in a higher population reduction of E. coli at 95% RH. Such biodegradable, nontoxic, and multistimuli-responsive antimicrobial fibers have great potential for broad applications as active and smart packaging systems.