Objective: The present research study was undertaken to formulate mucoadhesive sustained release buccal tablets and patches of 5-fluorouracil (5-FU).Method: For the research experiment work design expert software version 10, stat-ease, Inc. has been used. A 3 2 full factorial design was selected for the formulation of the buccal tablet as well as buccal patches. In this research work, formulated tablets and patches using different polymers such as carbopol 974p, polyvinylpyrrolidone-K 30, sodium deoxycholate, microcrystalline cellulose, and polyvinyl alcohol. An after formulation of batches formulated products studied for characterization, namely, Fourier transform infrared (FTIR) and differential scanning calorimeter (DSC). Evaluation parameters studied such as weight uniformity, thickness, hardness, friability, and content uniformity also carried out. For drug release purpose from the formulation of buccal tablet and patches in vitro drug released performed. In vivo drug releases study also carried out using Rabbit for drug reaction point of view.Results: Design expert showed the significant results on independent and dependent variables. The R-Squared 0.9943 for drug release and 0.9985 for swelling index is in reasonable agreement with the formulations. FTIR and DSC indicating compatibility of the drug and polymers in the tablet formulation and patch formulations at the molecular level. The drug release of buccal tablet showed 75.10-99.34% and buccal patches showed 58.41-81.43%. These formulations showed good results when compared to the conventional tablet. Conclusion:Formulation of mucoadhesive sustained release buccal tablets and patches of 5-FU successfully done using different polymers, which would definitely help in increasing bioavailability of the drug.
Background: Triphala, which is a combination of fruits of Terminalia chebula, Terminalia bellerica and Embilica officinalis generally recommended as herbal drug formulation in the Indian traditional medicine system. Study Design: To study the in-silico inhibitory potential of Triphala constituents against cytochrome P450 2E1 (CYP2E1) for the prevention of Thioacetamide-induced Hepatotoxicity Place and Duration of Study: The work has been performed at MUP's College of Pharmacy (B Pharm), Degaon, Risod, Washim, Maharashtra, India in between February 2021 to May 2021. Methodology: We have studied the inhibitory potential of Triphala on CYP2E1 by applying molecular docking tools. The major chemical constituents of Triphala i.e. gallic acid, chebulic acid, ellagic acid, epicatechin, syringic acid, and ascorbic acid were docked on CYP2E1. Results: Docking results revealed the very good inhibitory potential of Triphala in terms of binding affinity towards CYP2E1. All the chemical constituents have formed at least 2 and at most 6 hydrogen bonds with the crystal structure of CYP2E1. The binding energies (kcal/mol) of gallic acid, chebulic acid, ellagic acid, epicatechin, syringic acid, and ascorbic acid are -6.1, -7.1, -9.1, -8.3, -6.3, and -5.7, respectively. Ellagic acid has formed strong hydrogen bonds with Thr-303 and Thr-304 with bond length of 1.98 A0 and 2.26 A0 which confirms the excellent inhibition of CYP2E1. Conclusion: These findings can be used to control the CYP2E1-facilitated biotransformation and drug interactions in the development of new chemical entities. In future, these phytoconstituents can be used as lead molecules to overcome the cancer associated with oxidative stress resulting from the hyperactivity of CYP2E1.
1,3,4-oxadiazole and 1,2,4-oxadiazole derivatives are amongst the family of heterocycles which showed many promising pharmaceutical applications.Extensive literature survey of 1,3,4-oxadiazole scaffold revealed the activities such as antimicrobial, anti-inflammatory, anti-tubercular, anti-oxidant, anti-cancer, anti-convulsant, anti-diabetic and analgesic properties. 1,2,4-oxadiazole, have shown activity against a variety of diseases like Alzheimer's, parasitic worms (helminths) and other internal parasites, edema, infectious diseases, diabetes, pain and cramp, cardiovascular disease, HIV, tuberculosis, antioxidant, cancer, seizure disorders, and arthritis.As oxadiazoles exhibited many different types of pharmacological activities, we reviewed its pharmacological activities reported by different researchers in the field.In present article we reviewed different articles which has been published in English literature. The search engine used to search for the articles were Scopus, Google scholar, Bentham science, Science direct, Tayler and Francis, Springer nature, Frontiers, and Hindawi. Oxadiazole patent applications have grown by 100% in the previous 9 years, reaching a total of 646, making this a highly sought-after compound in the scientific community. From present review we concluded that Oxadiazoles are potent enough to be developed as potential antidiabetic agents more precisely as DPP-IV inhibitors. We believe that present review can provide insight to the researchers working to develop some novel Oxadiazole derivatives as potential antidiabetic agents.
Anorectal abscess, an infection in the anal area is a potentially debilitating and painful condition requiring urgent drainage to prevent septicemia. Commonly performed under neuraxial anaesthesia, we report surgical drainage of bilateral ischiorectal abscess under bilateral pudendal nerve blocks and general anaesthesia in a patient with severe ischaemic heart disease. Through our case we add to the existing literature, the importance of administrating peripheral nerve block in highly co-morbid patients. Keywords: Anorectal abscess, Bilateral pudendal block, Severe ischaemic heart disease.
Background: Pharmacological treatments for diabetes are based on increasing insulin availability and improving insulin sensitivity. Today, glucagon-like peptide 1 (GLP-1) -based therapies aim to control glucose through DPP-4 inhibitors. DPP-4 is a transmembrane glycoprotein belonging to the prolyl oligopeptidase family, with the specificity of eliminating the X-Pro or X-Ala dipeptides from the N-terminal end of the polypeptides. The effect of GLP-1 in stimulating the release of glucose-dependent insulin from pancreatic islets inhibits inappropriate glucagon release after meals and slow gastric emptying promotes intestinal permeability. Study Design: The current study investigated the inhibitory activity of DPP-4 along with the antioxidant activity of Enicostemma littorale extract. Place and Duration of Study: The present study was conducted at Anurag University, Hyderabad between June-2021 to Sept-2021. Methodology: The extracts tested for a range of activities such as hydroxyl radical scavenging activity test, In-vitro DPP-IV enzyme test activity test, DPPH free radical scavenging. Results: The extract shows dose-dependent DPPH and hydrogen peroxide radical scavenging activity. In in-vitro DPP-IV enzyme assay activity, Enicostemma littorale ethyl acetate extract showed greater inhibitory activity of DPP-IV compared to vildagliptin with IC50 values of 165.64μg/ml, respectively. Vildagliptin, based on the reference standard for DPP-IV inhibitor activity, has an IC50 value of 57.44 μg/ml. According to the in-vitro analysis, the Enicostemma littorale extract has a strong inhibitory activity of DPP-IV. Conclusion: We concluded that the Enicostemma littorale will be a better source for further development as new antidiabetic drugs. To the best of our knowledge, there is no report and study on the bark part of this species.
Innovation development and standardization of Novel Herbal Formulation
scite is a Brooklyn-based organization that helps researchers better discover and understand research articles through Smart Citations–citations that display the context of the citation and describe whether the article provides supporting or contrasting evidence. scite is used by students and researchers from around the world and is funded in part by the National Science Foundation and the National Institute on Drug Abuse of the National Institutes of Health.
hi@scite.ai
10624 S. Eastern Ave., Ste. A-614
Henderson, NV 89052, USA
Copyright © 2024 scite LLC. All rights reserved.
Made with 💙 for researchers
Part of the Research Solutions Family.