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Pingping Li,1 Syed Nasir Abbas Bukhari,2 Tahseen Khan,3 Renukaradhya Chitti,4 Davan B Bevoor,5 Anand R Hiremath,6 Nagaraja SreeHarsha,7 Yogendra Singh,8 Kumar Shiva Gubbiyappa9 1Department of Nephrology, Zhengzhou Central Hospital Affiliated to Zhengzhou University, Zhengzhou City, Henan Province 450007, People’s Republic of China; 2Department of Pharmaceutical Chemistry, College of Pharmacy, Jouf University, Sakaka, Aljouf 2014, Saudi Arabia; 3School of Pharmacy, Suresh Gyan Vihar University, Jaipur, India; 4Department of Pharmacy Practice, Sri Adichaunagiri College of Pharmacy, Adichunchanagiri University, Adichunchanagiri, Mandya, India; 5Department of Pharmacy Practice, SCS College of Pharmacy, Harapanahalli, Karnataka, India; 6Department of Pharmacology, Bapuji College of Pharmacy, Davanagere, Karnataka, India; 7Department of Pharmaceutical Sciences, College of Clinical Pharmacy, King Faisal University, Al‐Ahsa, Saudi Arabia; 8Department of Pharmaceutical Sciences, Mahatma Gandhi College of Pharmaceutical Sciences, Jaipur, India; 9School of Pharmacy, GITAM University, Hyderabad, IndiaCorrespondence: Yogendra Singh Email yogendra.singh12223@gmail.comBackground: Apigenin is known to have a broad-spectrum efficacy in oxidative stress and conditions due to inflammation, although weak absorption, fast metabolic rate and a fast elimination (systemic) limit the pharmacological efficacy of this drug. Hence, we propose the usage of highly bioavailable Apigenin-solid lipid nanoparticles (SLNPs) to recognize such limitations. The defensive function of Apigenin-SLNPs on renal damage induced by streptozotocin (STZ) in animals was studied.Materials and Methods: We initially injected the rats with 35 mg kg− 1 streptozocin intraperitoneally, and after 7 days, the rats were then injected 150 mg kg− 1 of metformin intragastrically followed by a once-daily intragastric dose of Apigenin-SLNP (25 or 50 mg kg− 1) for a continuous period of 30 days. We then measured the level of insulin and blood glucose, superoxide dismutase, catalase and malondialdehyde in the tissues of the kidney. We also observed messenger-RNA expression of Interleukin-1β, Interleukin-6 and Tumor Necrosis Factor-alpha in renal tissue through RT-PCR technique. Moreover, H&E staining and Western blotting observed the histopathological variations and protein expression of nuclear factor erythroid 2-related factor 2/heme oxygenase/Nuclear Factor-κB signaling pathway, respectively.Results: An enhancement in the expressing of nuclear factor erythroid 2-related factor 2 and heme oxygenase-1 and a suppression in the expression of Nuclear Factor-κB occurred due to Apigenin-SLNPs treatment, which was a result of the protective mechanism of Apigenin-SLNPs which is because of not only its anti-inflammatory function (by inhibition of release of inflammatory factors) but also their anti-oxidant activity (through reduction of lipid peroxidation production).Conclusion: We found that a protective effect on diabetic nephropathy was shown due to Apigenin-SLNPs, in rats induced with streptozocin maybe through the pathway of nuclear factor erythroid 2-related factor 2/heme oxygenase-1/Nuclear Factor-κB.Keywords: Apigenin-SLNPs, DN, Nrf2, HO-1, NF-κB

Katharigatta N Venugopala, 1, 2 Christophe Tratrat, 1 Melendhran Pillay, 3 Sandeep Chandrashekharappa, 4 Omar Husham Ahmed Al-Attraqchi, 5 Bandar E Aldhubiab, 1 Mahesh Attimarad, 1 Osama I Alwassil, 6 Anroop B Nair, 1 Nagaraja Sreeharsha, 1 Rashmi Venugopala, 7 Mohamed A Morsy, 1, 8 Michelyne Haroun, 1 Hezekiel M Kumalo, 9 Bharti Odhav, 2 Koleka Mlisana 3 1Department of Pharmaceutical Sciences, College of Clinical Pharmacy, King Faisal University, Al-Ahsa 31982, Kingdom of Saudi Arabia; 2Department of Biotechnology and Food Technology, Durban University of Technology, Durban 4001, South Africa; 3Department of Microbiology, National Health Laboratory Services, KZN Academic Complex, Inkosi Albert Luthuli Central Hospital, Durban 4001, South Africa; 4Institute for Stem Cell Biology and Regenerative Medicine, NCBS, TIFR, Bangalore 560 065, India; 5Department of Pharmaceutical Sciences, Faculty of Pharmacy, Philadelphia University, Amman 19392, Jordan; 6Department of Pharmaceutical Sciences, College of Pharmacy, King Saud Bin Abdulaziz University for Health Sciences, Riyadh, Saudi Arabia; 7Department of Public Health Medicine, University of KwaZulu-Natal, Howard College Campus, Durban 4001, South Africa; 8Department of Pharmacology, Faculty of Medicine, Minia University, El-Minia 61511, Egypt; 9Department of Medical Biochemistry, School of Laboratory Medicine and Medical Sciences, University of KwaZulu-Natal, Medical School, Durban 4001, South AfricaCorrespondence: Katharigatta N VenugopalaDepartment of Pharmaceutical Sciences, College of Clinical Pharmacy, King Faisal University, P.o. Box-400, Al-Ahsa 31982, Kingdom of Saudi ArabiaTel +96613 589 8842Email kvenugopala@kfu.edu.saSandeep ChandrashekharappaInstitute for Stem Cell Biology and Regenerative Medicine, National Center for Biological Sciences, Tata Institute of Fundamental Research, GKVK, Bellary Road, Bangalore 560 065, IndiaTel +9194486 39413Email sandeepc@instem.res.inBackground and Purpose: Tuberculosis has been reported to be the worldwide leading cause of death resulting from a sole infectious agent. The emergence of multidrug-resistant tuberculosis and extensively drug-resistant tuberculosis has made the battle against the infection more difficult since most currently available therapeutic options are ineffective against these resistant strains. Therefore, novel molecules need to be developed to effectively treat tuberculosis disease. Preliminary docking studies revealed that tetrahydropyrimidinone derivatives have favorable interactions with the thymidylate kinase receptor. In the present investigation, we report the synthesis and the mycobacterial activity of several pyrimidinones and pyrimidinethiones as potential thymidylate kinase inhibitors.Methods: The title compounds ( 1a–d) and ( 2a–b) were synthesized by a one-pot three-component Biginelli reaction. They were subsequently characterized and used for whole-cell anti-TB screening against H37Rv and multidrug-resistant (MDR) strains of Mycobacterium tuberculosis (MTB) by the resazurin microplate assay (REMA) plate method. Molecular modeling was conducted using the Accelry’s Discovery Studio 4.0 client program to explain the observed bioactivity of the compounds. The pharmacokinetic properties of the synthesized compounds were predicted and analyzed.Results: Of the compounds tested for anti-TB activity, pyrimidinone 1a and pyrimidinethione 2a displayed moderate activity against susceptible MTB H37Rv strains at 16 and 32 μg/mL, respectively. Only compound 2a was observed to exert modest activity at 128 μg/mL against MTB strains with cross-resistance to rifampicin and isoniazid. The presence of the trifluoromethyl group was essential to retain the inhibitory activity of compounds 1a and 2a. Molecular modeling studies of these compounds against thymidylate kinase targets demonstrated a positive correlation between the bioactivity and structure of the compounds. The in-silico ADME (absorption, distribution, metabolism, and excretion) prediction indicated favorable pharmacokinetic and drug-like properties for most compounds.Conclusion: Pyrimidinone 1a and pyrimidinethione 2a were identified as the leading compounds and can serve as a starting point to develop novel anti-TB therapeutic agents.Keywords: thymidylate kinase inhibitors, tetrahydropyrimidinones, tetrahydropyrimidinethiones, multidrug resistance, Mycobacterium tuberculosis, molecular modeling

Li P, Bukhari SNA, Khan T, et al. Int J Nanomedicine. 2020;15:9115–9124. The Editor and Publisher of International Journal of Nanomedicine wish to retract the published article. Concerns were raised regarding the alleged duplication of H&E images in Figure 4. Specifically, Figure 4A, Control, appears to have been duplicated with the same image for Figure 4E, Apigenin-SLNPs (50). In addition, images from Figure 4 also appear to have been duplicated with similar images from Figure 7 in Arellano-Buendia et al (2014), Oxidative Medicine and Cellular Longevity (https://doi.org/10.1155/2014/961326). Specifically, Images for Figure 4A, Control and Figure 4E, Apigenin-SLNPs (50) appear to have been duplicated with a similar image for Figure 7a and 7c from Arellano-Buendia et al (2014). The image for Figure 4C, Metformin, appears to have been duplicated with a similar image for Figure 7f from Arellano-Buendia et al (2014). The image for Figure 4D, Apigenin-SLNPs (25) appears to have been duplicated with a similar image for Figure 7d from Arellano-Buendia et al (2014). The authors did respond to our queries but were unable to provide a satisfactory explanation for the duplicated images and the Editor requested for the article to be retracted. Our decision-making was informed by our policy on publishing ethics and integrity and the COPE guidelines on retraction. The retracted article will remain online to maintain the scholarly record, but it will be digitally watermarked on each page as “Retracted”.

Nagaraja SreeHarsha,1,2 Katharigatta N Venugopala,1,3 Anroop B Nair,1 Teeka S Roopashree,4 Mahesh Attimarad,1 Jagadeesh G Hiremath,2 Bandar E Al-Dhubiab,1 Chandramouli Ramnarayanan,5 Pottathil Shinu,6 Mukund Handral,7 Micheline Haroun,1 Christophe Tratrat1 1Department of Pharmaceutical Sciences, College of Clinical Pharmacy, King Faisal University, Al-Ahsa, Saudi Arabia; 2Department of Pharmaceutics, Vidya Siri College of Pharmacy, Bengaluru, India; 3Department of Biotechnology and Food Technology, Durban University of Technology, Durban 4001, South Africa; 4Department of Pharmacognosy, Government College of Pharmacy, Bengaluru, India; 5Department of Quality Assurance, Krupanidhi College of Pharmacy, Bengaluru, India; 6Department of Biomedical Sciences, College of Clinical Pharmacy, King Faisal University, Al-Ahsa, Saudi Arabia; 7Department of Pharmacology, Faculty of Pharmaceutical Sciences, PES University, Bengaluru, IndiaCorrespondence: Nagaraja SreeHarshaDepartment of Pharmaceutical Sciences, College of Clinical Pharmacy, King Faisal University, PO Box 400, Al-Ahsa, Saudi ArabiaTel +96-653-548-5322Email sharsha@kfu.edu.saBackground: Chronic diseases such as diabetes, asthma, and heart disease are the leading causes of death in developing countries. Public health plays an important role in preventing such diseases to improve individuals’ quality of life. Conventional dosage schemes used in public health to cure various diseases generally lead to undesirable side effects and renders the overall treatment ineffective. For example, a required concentration of drug cannot reach the lungs using conventional methods to cure asthma. Microspheres have emerged as a confirmed drug-delivery system to cure asthma.Method: In this paper, a salbutamol-loaded poly lactic acid-co-glycolic acid-polyethylene glycol (PLGA-PEG) microsphere (SPP)-based formulation was prepared using a Buchi B-90 nanospray drier. Face-centered central composite design (CCD) was applied to optimize the spray-drying process.Results: The drug content and product yield were found to be 72%±0.8% and 86%±0.4%, respectively; drug release (91.1%) peaked for up to 12 hrs in vitro. Microspheres obtained from the spray dryer were found to be shriveled. The experiments were carried out and verified using various groups of rabbits. In our study, the particle size (8.24 μm) was observed to be an essential parameter for drug delivery. The in vivo results indicated that the targeting efficacy and drug concentration in the lung was higher with the salbutamol-loaded PLGA-PEG SPP formulation (1,410.1±10.11 μg/g, 15 mins), as compared to the conventional formulation (92±0.56 μg/g, 10 min). The final product was stable under 5°C±2°C, 25°C±2°C, and 40°C±2°C/75%±5% relative humidity. In addition, these co-polymers have a good safety profile, as determined by testing on human alveolar basal epithelium A549 cell lines.Conclusion: Our results prove that microspheres are an alternative drug-delivery system for lung-targeted asthma treatments used in public health.Keywords: polylactic acid-co-glycolic acid, public health, spray dryer, microspheres

Nagaraja SreeHarsha,1 Rahul Maheshwari,2,3 Bandar E Al-Dhubiab,1 Muktika Tekade,4 Mukesh Chandra Sharma,4 Katharigatta N Venugopala,1,5 Rakesh Kumar Tekade,2,6–7 Abdullah M Alzahrani8 1Department of Pharmaceutical Sciences, College of Clinical Pharmacy, King Faisal University, Al-Ahsa, Saudi Arabia; 2National Institute of Pharmaceutical Education and Research (NIPER) – Ahmedabad, Gandhinagar, Gujarat 382355, India; 3School of Pharmacy and Technology Management, SVKM’s NMIMS, Hyderabad Campus, Hyderabad, Telangana 509 301, India; 4School of Pharmacy, Devi Ahilya Vishwavidyalaya, Takshila Campus, Indore, MP 452001, India; 5Department of Biotechnology and Food Technology, Durban University of Technology, Durban 4001, South Africa; 6Department of Pharmaceutical Technology, The International Medical University, School of Pharmacy, Kuala Lumpur 57000, Malaysia; 7Department of Materials Engineering, Indian Institute of Technology-Jammu, Jammu - 181 221, J&K, India; 8Department of Biological Sciences, College of Science, King Faisal University, Al-Ahsa, Saudi ArabiaCorrespondence: Nagaraja SreeHarshaDepartment of Pharmaceutical Sciences, College of Clinical Pharmacy, King Faisal University, PO Box 380, Al-Ahsa 31982, Saudi ArabiaEmail sharsha@kfu.edu.saBackground: Prostate cancer (PC) has the highest prevalence in men and accounts for a high rate of neoplasia-related death. Doxorubicin (DOX) is one of the most widely used anti-neoplastic drugs for prostate cancer among others. However, it has low specificity and many side effects and affects normal cells. More recently, there have been newly developed drug delivery tools which are graphene or graphene-based, used to increase the specificity of the delivered drug molecules. The graphene derivatives possess both π-π stacking and increased hydrophobicity, factors that increase the likelihood of drug delivery. Despite this, the hydrophilicity of graphene remains problematic, as it induced problems with stability. For this reason, the use of a chitosan coating remains one way to modify the surface features of graphene.Method: In this investigation, a hybrid nanoparticle that consisted of a DOX-loaded reduced graphene oxide that is stabilized with chitosan (rGOD-HNP) was developed.Result: The newly developed rGOD-HNP demonstrated high biocompatibility and efficiency in entrapping DOX (∼65%) and releasing it in a controlled manner (∼50% release in 48 h). Furthermore, it was also demonstrated that rGOD-HNP can intracellularly deliver DOX and more specifically in PC-3 prostate cancer cells.Conclusion: This delivery tool offers a feasible and viable method to deliver DOX photo-thermally in the treatment of prostate cancer.Keywords: graphene, photothermal, chitosan, hybrid nanoparticles, HNP, prostate cancer

Nagaraja SreeHarsha,1 Ravindra V Ghorpade,2 Abdullah Mossa Alzahrani,3 Bandar E Al-Dhubiab,1 Katharigatta N Venugopala1,41Department of Pharmaceutical Sciences, College of Clinical Pharmacy, King Faisal University, Al-Ahsa, Saudi Arabia; 2Chemical Engineering and Process Development Division, CSIR-National Chemical Laboratory, Pune 411 008, India; 3Department of Biological Sciences, College of Science, King Faisal University, Al-Ahsa, Saudi Arabia; 4Department of Biotechnology and Food Technology, Durban University of Technology, Durban 4001, South AfricaPurpose: Here, we present the successful preparation of a highly efficient gallic acid resin grafted with magnetic nanoparticles (MNPs) and containing a branched brush polymeric shell.Methods: Using a convenient co-precipitation method, we prepared Fe3O4 nanoparticles stabilized by citric acid. These nanoparticles underwent further silica modification and amino functionalization followed by gallic acid functionalization on their surface. Under alkaline conditions, we used a condensation reaction that combined formaldehyde and gallic, to graft the gallic acid−formaldehyde resin on the surface. We then evaluated the polymer-grafted MNPs to assay the Candida Antarctica B lipase(Cal-B) immobilization via physical adsorption.Conclusion: Furthermore, during optimization of parameters that defined conditions of immobilization, we found that the optimum immobilization was achieved in 15 mins. Also, optimal immobilization temperature and pH were 38ºC and 7.5, respectively. In addition, the reusability study of immobilized lipase polymer-grafted MNPs was done by isolating the MNPs from the reaction medium using magnetic separation, which showed that grafted MNPs reached 5 cycles with 91% activity retention.Keywords: nanoparticles, Candida Antarctica lipase B, grafting, immobilization

Sibghatullah Sangi,1 Nagaraja SreeHarsha,2 Abdulhakim Bawadekji,3 Mouhanad Al Ali4 1Department of Clinical Pharmacy, Faculty of Pharmacy, Northern Border University, Rafha, Saudi Arabia; 2Department of Pharmaceutical Sciences, College of Clinical Pharmacy, King Faisal University, Al-Ahsa, Saudi Arabia; 3Department of Biological Sciences, College of Science, Northern Border University, Arar, Saudi Arabia; 4Higher Institute of Health and Bio-products of Angers (ISSBA), Angers- France, Université d’Angers, Angers, France Purpose: Currently, microsphere technology plays a major role in the development of many new cancer therapies. In the current study, we proposed a targeted drug-delivery system to improve the treatment efficacy of one of the common conventional chemotherapeutic drugs used to treat lung tumors, 5-fluorouracil (5-FU).Materials and methods: Following the preparation and optimization of small, solid microspheres, ranging in diameter between 5 and 15 µm, the final product 5-fluorouracil gelatin (5-FUG) was formulated using a Buchi Nano Spray Dryer by varying the drug:polymer ratio.Results: Particle yield was calculated as 65% ± 1.2%, and the drug content in the formulation was recorded as 74% ± 1.6%. Particle surface morphology was examined as shriveled shape (crumpled/folded); particle size distribution displayed a binomial distribution, with a mean diameter of 9.6 µm. In vitro drug release studies revealed that ~36.4% of the 5-FU in 5-FUG was released in the first hour after injection. Clinically, this would lead to initial or burst release, facilitating a quick rise to therapeutic levels. In contrast to the pure 5-FU drug (89.2% of the drug released in the first 30 minutes), 99.1% of the drug in 5-FUG was released from the spray-dried particles for a period of 12 hours. A two-compartment model was used to generate plasma concentration–time curves. 5-FUG injection has a much different distribution in vivo in contrast to intravenous injection of 5-FU. In addition, the half-life after intravenous injection of 5-FUG, t1/2(α) = 1.23 hours and t1/2(β) = 18.3 hours, was considerably longer than that of 5-FU, t1/2(α) = 0.34 hours and t1/2(β) = 8.62 hours. Examination of stained lung tissue sections showed no histopathological tissue changes or evidence of gross pathology. In addition, the optimized formulation demonstrated an increased stability under both long-term and refrigerated storage conditions.Conclusion: Our goal was to develop similar delivery systems for other chemotherapeutic drugs that are site specific to different disease models/tumor types. Keywords: spray drying, 5-fluorouracil, cancer, microspheres, targeting

Polymers are a fundamental part of numerous industries and can be conjugated with many other materials and components to have a vast array of products. Biomaterials have been extensively studied for their application in pharmaceutical formulation development, tissue engineering, and biomedical areas. However, the native form of many polymers has limitations concerning microbial contamination, susceptibility, solubility, and stability. Chemical or physical modifications can overcome these limitations by tailoring the properties of polymers to meet several requirements. The polymer modifications are interdisciplinary, cutting across conventional materials, physics, biology, chemistry, medicine, and engineering limitations. Microwave irradiation has become a well-established technique for a few decades to drive and promote chemical modification reactions. This technique allows ease of temperature and power control to perform the synthesis protocols efficiently. Additionally, microwave irradiation contributes to green and sustainable chemistry. In this contribution, microwave-assisted polymer modifications were described with a special focus on their application in developing several novel dosage forms.

Comprehensive preoperative evaluation of potential donors is crucial for selecting the right donor, with adequately functioning kidneys, and the best surgical approach for harvesting the organs to prevent donor-related complications and to assure good recipient graft function. Multidetector computed tomography is the choice of imaging in the preoperative evaluation of living renal donors with an accuracy of 95%–100%. The donor must retain one normal kidney. The left kidney is preferred for living donor nephrectomy because it has a longer renal vein and it is technically easier to remove. It is always preferable to choose kidneys with a single artery because both donor and recipient surgeries are less complicated and there is less risk for arterial thrombosis. We report in a case of successful transplantation wherein the donor had an early division of the main renal artery bilaterally as well as bilateral accessory renal arteries.

The polyphenol chrysin is a frequent food component. It has been demonstrated to have a number of favorable benefits on a variety of skin ailments and disorders. It’s anti-inflammatory and antioxidant properties are high. It has been demonstrated to protect skin from UV exposure by neutralizing reactive oxygen species that cause cutaneous damage and skin cancer. In acne, psoriasis, wound healing, and cutaneous leishmaniasis, chrysin has shown promising therapeutic advantages. It is increasingly being used in anti-aging skin cosmetics especially those for reducing under-eye dark circles. However, chrysin is not yet clinically translated as a drug. This present review highlights the potential and future scope of chrysin as a therapeutic agent in skin disorders and also as a cosmeceutical.

In less agroecological parts of the Asian, Arabian, and African deserts, Camelus dromedarius play an important role in human survival. For many years, camels have been employed as a source of food, a tool of transportation, and a means of defense. They are becoming increasingly important as viable livestock animals in many desert climates. With the help of camel genetics, genomics and proteomics known so far, this review article will summarize camel enzymes and proteins, which allow them to thrive under varied harsh environmental situations. An in-depth study of the dromedary genome revealed the existence of protein-coding and fast-developing genes that govern a variety of metabolic responses including lipid and protein metabolism, glucoamylase, flavin-containing monooxygenase and guanidinoacetate methyltransferase are other metabolic enzymes found in the small intestine, liver, pancreas, and spleen. In addition, we will discuss the handling of common medications by camel liver cytochrome p 450, which are different from human enzymes. Moreover, camels developed several paths to get optimum levels of trace elements like copper, zinc, selenium, etc., which have key importance in their body for normal regulation of metabolic events. Insulin tolerance, carbohydrate and energy metabolism, xenobiotics metabolizing enzymes, vimentin functions, behavior during the rutting season, resistance to starvation and changes in blood composition and resistance to water loss were among the attractive aspects of camel enzymes and proteins peculiarities in the camels. Resolving the enigma of the method of adaptation and the molecular processes linked with camel life is still a developing repository full of mysteries that need additional exploration.

Abstract The high fat diet alters intestinal microbiota due to increased intestinal permeability and susceptibility to microbial antigens leads to metabolic endotoxemia. But probiotic juices reported for various health benefits. In this background we hypothesized that pectinase treated probiotic banana juice has diverse effects on HFD induced obesity and non-alcoholic steatohepatitis. 20 weeks fed HFD successfully induced obesity and its associated complications in experimental rats. The supplementation of probiotic banana juice for 5 months at a dose of 5 mL/kg bw/day resulted significant decrease (p

Introduction: We report our results of preputial flap onlay urethroplasty for the one-stage repair of mid- and proximal penile hypospadias with chordee. Materials and Methods: We retrospectively reviewed the hospital data base for children undergoing onlay flap urethroplasty and hypospadias repair for mid- or proximal penile hypospadias with chordee. Results: During the study period January 2000–December 2017, 21 children underwent onlay preputial flap urethroplasty. The procedure was successful in 15 (71.42%) children with no need to undergo further procedures or operations. There were five urethrocutaneous fistulas and dehiscence of glans in one. Conclusions: An onlay urethroplasty using the preputial flap yields results comparable to those of staged techniques and results in fewer procedures under anesthesia in children.

The 4-allyl guaiacol is a natural phenolic molecule that has been widely studied for its antioxidant capacity against reactive-oxygen-species-mediated cellular damage. Therefore, we hypothesized that concomitant use of an antioxidant and NSAID may decrease the risk of gastrointestinal toxicity and make the therapy safer. To address the gastrointestinal toxicity of conventional NSAIDs, a new S-naproxen-4-allyl guaiacol chimera (MAS-1696) was computationally developed, chemically synthesized, and tested for anti-inflammatory effectiveness and gastrointestinal safety. The inhibitory potency of MAS-1696 tested against cyclooxygenase-2 (COX2), 15-lipoxygenase-2 (15-LOX2), and lipoxygenase-5 (5-LOX) in vitro revealed a stronger inhibition of COX2. Furthermore, the MAS-1696 chimera increased the COX selectivity index by 23% as compared to the parent compound naproxen, implying higher efficacy and gastric safety. In vivo data showed that MAS-1696 was less likely to cause gastrointestinal harm than naproxen while also exerting anti-inflammatory and analgesic effects equivalent to or superior to naproxen. In conclusion, MAS-1696 is orally active, bio-labile, and crystalline, making it a medication that may be administered orally.

Diabetes mellitus (DM) and its complications are a severe public health concern due to the high incidence, morbidity, and mortality rates. The present study aims to synthesize and characterize silver nanoparticles (AgNPs) using the aqueous leaf extract of Psidium guajava (PGE) for investigating its antidiabetic activity. Psidium guajava silver nanoparticles (PGAg NPs) were prepared and characterized by various parameters. The in vivo study was conducted using PGE and PGAg NPs in Streptozotocin (STZ)-induced diabetic rats to assess their antidiabetic properties. STZ of 55 mg/kg was injected to induce diabetes. The PGE, PGAg NPs at a dose of 200 and 400 mg/kg and standard drug Metformin (100 mg/kg) were administered daily to diabetic rats for 21 days through the oral route. Blood glucose level, body weight changes, lipid profiles, and histopathology of the rats’ liver and pancreas were examined. In the diabetic rats, PGE and PGAg NPs produced a drastic decrease in the blood glucose level, preventing subsequent weight loss and ameliorating lipid profile parameters. The histopathological findings revealed the improvements in pancreas and liver cells due to the repercussion of PGE and PGAg NPs. A compelling effect was observed in all doses of PGE and PGAg NPs; however, PGAg NPs exhibited a more promising result. Thus, from the results, it is concluded that the synthesized PGAg NPs has potent antidiabetic activity due to its enhanced surface area and smaller particle size of nanoparticles.

Nanotechnology utilizes the mechanics to control the size and morphology of the particles in the required nano range for accomplishing the intended purposes. There was a time when it was predominantly applied only to the fields of matter physics or chemical engineering, but with time, biological scientists recognized its vast benefits and explored the advantages in their respective fields. This extension of nanotechnology in the field of dentistry is termed ‘Nanodentistry.’ It is revolutionizing every aspect of dentistry. It consists of therapeutic and diagnostic tools and supportive aids to maintain oral hygiene with the help of nanomaterials. Research in nanodentistry is evolving holistically but slowly with the advanced finding of symbiotic use of novel polymers, natural polymers, metals, minerals, and drugs. These materials, in association with nanotechnology, further assist in exploring the usage of nano dental adducts in prosthodontic, regeneration, orthodontic, etc. Moreover, drug release cargo abilities of the nano dental adduct provide an extra edge to dentistry over their conventional counterparts. Nano dentistry has expanded to every single branch of dentistry. In the present review, we will present a holistic view of the recent advances in the field of nanodentistry. The later part of the review compiled the ethical and regulatory challenges in the commercialization of the nanodentistry. This review tracks the advancement in nano dentistry in different but important domains of dentistry.

Introduction: Lymphocele formation following renal transplantation is a well-known complication. Mostly these are small and inconsequential, but large lymphocele may cause symptoms like pain, infection , renal dysfunction, surgical drainage of lymphatics Surgical damage of the lymphatics of the graft during the procurement and of the lymphatics around the iliac vessels of the recipients has been responsible with development of lymphocele. Several factors such as diabetes, obesity, blood coagulation abnormalities, anticoagulation prophylaxis, high dose of diuretics, delay in graft function and immunosuppressive drugs are known to be related to these complications. We report three cases of symptomatic lymphoceles managed at our centre during the past one year. Patients and Methods: We retrospectively reviewed patients undergoing renal transplant at our centre. Out of 18 transplant recipients 3 cases developed large symptomatic lymphoceles. These were evaluated by Computed Tomography (CT) scan/ Ultrasound (USG) and serum creatinine levels. These patients were managed by ultrasound guided aspiration and instillation of doxycyline. Results: All three patients underwent USG guided aspiration and doxycyline instillation had significant reduction in serum creatinine levels with no recurrence of lymphoceles on follow-up. Conclusions: lymphocele remains important surgical complications following renal transplantation. Prompt diagnosis and early intervention is crucial to prevent permanent renal damage..

Skin, an exterior interface of the human body is home to commensal microbiota and also acts a physical barrier that protects from invasion of foreign pathogenic microorganisms. In recent years, interest has significantly expanded beyond the gut microbiome to include the skin microbiome and its influence in managing several skin disorders. Probiotics play a major role in maintaining human health and disease prevention. Topical probiotics have demonstrated beneficial effects for the treatment of certain inflammatory skin diseases such as acne, rosacea, psoriasis etc., and also found to have a promising role in wound healing. In this review, we discuss recent insights into applications of topical probiotics and their influence on health and diseases of the skin. Patents, commercially available topical probiotics, and novel probiotic impregnated fabrics have been emphasized. A thorough understanding of the relationship between probiotics and the skin microbiome is important for designing novel therapeutic approaches in using topical probiotics.

Antibiotic resistance continues to be a most serious threat to public health. This situation demands that the scientific community increase their efforts for the discovery of alternative strategies to circumvent the problems associated with conventional small molecule therapeutics. The Global Antimicrobial Resistance and Use Surveillance System (GLASS) Report (published in June 2021) discloses the rapidly increasing number of bacterial infections that are mainly caused by antimicrobial-resistant bacteria. These concerns have initiated various government agencies and other organizations to educate the public regarding the appropriate use of antibiotics. This review discusses a brief highlight on the timeline of antimicrobial drug discovery with a special emphasis on the historical development of antimicrobial resistance. In addition, new antimicrobial targets and approaches, recent developments in drug screening, design, and delivery were covered. This review also discusses the emergence and roles of various antibiotic adjuvants and combination therapies while shedding light on current challenges and future perspectives. Overall, the emergence of resistant microbial strains has challenged drug discovery but their efforts to develop alternative technologies such as nanomaterials seem to be promising for the future.

Background: Intranasal route offers a direct nose-to-brain delivery via olfactory and trigeminal nerves and minimizes the systemic exposure of the drug. Although reliable and non-invasive, intranasal administration of lipophilic neuroprotective agents for brain targeting is still challenging. Literature focuses on naturally-derived compounds as a promising therapeutics for chronic brain diseases. Naringin, a natural flavonoid obtained from citrus fruits possesses neuroprotective effects. By regulating multiple crucial cellular signaling pathways, naringin acts on several therapeutic targets that make it suitable for the treatment of neurodegenerative diseases like Alzheimer’s disease and making it a suitable candidate for nasal administration. However, the hydrophobicity of naringin is the primary challenge to formulate it in an aqueous system for nasal administration. Method: We designed a lipid-based nanoemulsifying drug delivery system of naringin using Acrysol K140 as an oil, Tween 80 as a surfactant and Transcutol HP as a cosolvent, to improve solubility and harness the benefits of nanosizing like improved cellular penetration. Intranasal instillations of therapeutic agents have limited efficacy due to drug washout and inadequate adherence to the nasal mucosa. Therefore, we reconstituted the naringin self-emulsifying system in a smart, biodegradable, ion-triggered in situ gelling hydrogel and optimized for desirable gel characteristics. The naringin-loaded composition was optimized and characterized for various physicochemical and rheological properties. Results: The formulation showed a mean droplet size 152.03 ± 4.6 nm with a polydispersity index Conclusion: In situ gelling system with nanoemulsified naringin demonstrated a safe nasal delivery providing a new dimension to the treatment of chronic neurodegenerative diseases using small hydrophobic phytoconstituents with minimization of dose and related systemic adverse effects.

Background: Infectious diseases still affect large populations causing significant morbidity and mortality. Bacterial and fungal infections for centuries were the main factors of death and disability of millions of humans. Despite the progress in the control of infectious diseases, the appearance of resistance of microbes to existing drugs creates the need for the development of new effective antimicrobial agents. In an attempt to improve the antibacterial activity of previously synthesized compounds modifications to their structures were performed. Methods: Nineteen thiazolidinone derivatives with 6-Cl, 4-OMe, 6-CN, 6-adamantan, 4-Me, 6-adamantan substituents at benzothiazole ring were synthesized and evaluated against panel of four bacterial strains S. aureus, L. monocytogenes, E. coli and S. typhimirium and three resistant strains MRSA, E. coli and P. aeruginosa in order to improve activity of previously evaluated 6-OCF3-benzothiazole-based thiazolidinones. The evaluation of minimum inhibitory and minimum bactericidal concentration was determined by microdilution method. As reference compounds ampicillin and streptomycin were used. Results: All compounds showed antibacterial activity with MIC in range of 0.12–0.75 mg/mL and MBC at 0.25–>1.00 mg/mL The most active compound among all tested appeared to be compound 18, with MIC at 0.10 mg/mL and MBC at 0.12 mg/mL against P. aeruginosa. as well as against resistant strain P. aeruginosa with MIC at 0.06 mg/mL and MBC at 0.12 mg/mL almost equipotent with streptomycin and better than ampicillin. Docking studies predicted that the inhibition of LD-carboxypeptidase is probably the possible mechanism of antibacterial activity of tested compounds. Conclusion: The best improvement of antibacterial activity after modifications was achieved by replacement of 6-OCF3 substituent in benzothiazole moiety by 6-Cl against S. aureus, MRSA and resistant strain of E. coli by 2.5 folds, while against L. monocytogenes and S. typhimirium from 4 to 5 folds.

The SARS-CoV-2 outbreak is the COVID-19 disease, which has caused massive health devastation, prompting the World Health Organization to declare a worldwide health emergency. The corona virus infected millions of people worldwide, and many died as a result of a lack of particular medications. The current emergency necessitates extensive therapy in order to stop the spread of the coronavirus. There are various vaccinations available, but no validated COVID-19 treatments. Since its outbreak, many therapeutics have been tested, including the use of repurposed medications, nucleoside inhibitors, protease inhibitors, broad spectrum antivirals, convalescence plasma therapies, immune-modulators, and monoclonal antibodies. However, these approaches have not yielded any outcomes and are mostly used to alleviate symptoms associated with potentially fatal adverse drug reactions. Nanoparticles, on the other hand, may prove to be an effective treatment for COVID-19. They can be designed to boost the efficacy of currently available antiviral medications or to trigger a rapid immune response against COVID-19. In the last decade, there has been significant progress in nanotechnology. This review focuses on the virus’s basic structure, pathogenesis, and current treatment options for COVID-19. This study addresses nanotechnology and its applications in diagnosis, prevention, treatment, and targeted vaccine delivery, laying the groundwork for a successful pandemic fight.