Melanda Fitriana, Abdul MUN’IM, Firdayani, Wirawan Adikusuma
{"title":"EXPLORATION OF THE ACTIVE COMPOUNDS OF MORINGA OLEIFERA LAM AS HIV-1 REVERSE TRANSCRIPTASE INHIBITOR: A NETWORK PHARMACOLOGY AND MOLECULAR DOCKING APPROACH","authors":"Melanda Fitriana, Abdul MUN’IM, Firdayani, Wirawan Adikusuma","doi":"10.22159/ijap.2024v16i2.49855","DOIUrl":"https://doi.org/10.22159/ijap.2024v16i2.49855","url":null,"abstract":"Objective: This study aims to predict the active compound of Moringa oleifera for the treatment of Human Immunodeficiency Virus (HIV), specifically targeting the HIV-1 reverse transcriptase (HIV-1 RT) enzyme using network pharmacology and molecular docking approach.\u0000Methods: The active ingredients of M. oleifera, were screened from the Knapsack database. Subsequently, HIV-1 RT and its related target compounds were retrieved from the Genecard database. The analysis of common targets involved protein-protein interactions (PPI) analysis using string databases and constructing interaction IDs using Cytoscape software. Gene Ontology (GO) functional and the Kyoto Encyclopedia of Genes and Genomes (KEGG) pathway analyses were performed. Molecular docking studies were conducted using AutoDock Vina software to validate the results of the network pharmacological analysis.\u0000Results: A total of 63 active ingredients and 8601 targets related to HIV-1 RT were identified. The network analysis, encompassing GO and KEGG enrichment, revealed strong associations of common targets with key signaling pathways such as Tumor Necrosis Factor (TNF), Toll Like Receptor (TLR), and apoptosis. Additionally, 11 compounds of M. oleifera including apigenin, benzyl isothiocyanate, benzylamine, caffeic acid, ferulic acid, epicatechin, kaempferol, gallic acid, luteolin, syringic acid and vanillin were identified as potential vital compounds. Molecular docking analysis highlighted apigenin and kaempferol as the most promising compounds, exhibiting the lowest binding affinity to the HIV-1 RT enzyme. These compounds correlated with caspase-3(CASP3), caspase-9 (CASP9), and BCL2 Apoptosis Regulator (BAX) protein, stimulating cell apoptosis through multiple pathways. \u0000Conclusion: The study highlighted that apigenin and kaempferol are potential compound of M. oleifera in HIV-1 treatment through inhibition activity at HIV-1 RT Enzyme.","PeriodicalId":507178,"journal":{"name":"International Journal of Applied Pharmaceutics","volume":"55 17","pages":""},"PeriodicalIF":0.0,"publicationDate":"2024-03-07","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"140258795","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
{"title":"PREPARATION, CHARACTERIZATION AND EVALUATION OF GELLAN GUM/GLYCOL CHITOSAN BASED BAICALEIN HYDROGEL FOR WOUND HEALING","authors":"K. D. Baviskar, S. Lodhi","doi":"10.22159/ijap.2024v16i2.49661","DOIUrl":"https://doi.org/10.22159/ijap.2024v16i2.49661","url":null,"abstract":"Objective: The present work was emphasized on preparation, characterization and evaluation of baicalein loaded hydrogel to promote healing of wounds.\u0000Methods: Baicalein loaded hydrogel was developed using Gellan gum and Glycol chitosan polymers. Prepared hydrogels were characterized for various parameters like Field Emission Scanning Electron Microscopy (FE-SEM), swelling property, entrapment efficiency, rheology and drug release. Wound healing study was investigated by using incision dead space wound models. Healing effect was assessed by measurement of tensile strength, collagen content, hydroxyproline content, protein content and antioxidant status.\u0000Results: The percent entrapment efficiency of optimized hydrogel found to be 89.78±2.07 which resulted in controlled release of drug 85.03% in 12 h. The significant increased level of catalase and superoxide dismutase (SOD) was noticed in dead space wound model. The tensile strength study shows increase in collagen synthesis due to treatment with Baicalein loaded hydrogel. The higher collagen content, better granulation, increase in tensile strength was noticed. Histopathological examination also confirmed higher degree of re-epithelialization and enhanced cutaneous wound repair.\u0000Conclusion: In conclusion, biodegradable Baicalein loaded hydrogel might have high potential for wound healing with improved oxidative status and extended release of Baicalein.","PeriodicalId":507178,"journal":{"name":"International Journal of Applied Pharmaceutics","volume":"50 15","pages":""},"PeriodicalIF":0.0,"publicationDate":"2024-03-07","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"140258855","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
{"title":"THE DEVELOPMENT AND VALIDATION OF ANALYTICAL METHOD FOR EVALUATING GALLIC ACID IN ETHYL ACETATE FRACTION (EAF) OF SNEDDS FORMULATION: QUANTITATIVE ANALYSIS WITH IN VITRO ASSAY","authors":"P. Apridamayanti, L. Pratiwi, R. Sari","doi":"10.22159/ijap.2024v16i2.49830","DOIUrl":"https://doi.org/10.22159/ijap.2024v16i2.49830","url":null,"abstract":"Objective: This study aimed to develop a simple, accurate, precise, sensitive, robust, and stable analytical method for the evaluation of gallic acid in Self-Nanoemulsifying Drug Delivery System (SNEDDS) incorporating ethyl acetate fraction (EAF) of Melastoma malabathricum leaves in combination with Gentamicin.\u0000Methods: Validation process followed ICH guidelines and applied a reverse phase HPLC method with a mobile phase of acetonitrile-phosphoric buffer at pH 3.03 (20:80 v/v). The stationary phase consisted of a VP-ODS shim-pack C-18 column (250x4.6 mm) with a flow rate of 0.2 ml/min and detection at 263 nm using an Ultraviolet detector. Additionally, antioxidant activity was assessed through the DPPH and FRAP methods, and SPF value was determined with a UV/Vis spectrophotometer in the 290-390 nm wavelength range.\u0000Results: The results showed that the retention time of quercetin was 16.648 min with a tailing factor of 1.623. The regression equation (y=224689x-989000) had a concentration range of 10-55 µg/ml and a correlation value of 0.9920. Limit of Detection (LOD) and Limit of Quantification (LOQ) were found to be 2.394±0.086 and 7.254±0.260 µg/ml, respectively. Method accuracy, determined by recovery values at concentrations of 50%, 100%, and 150%, ranged from 91.18% to 109.49%. Repeatability inter-day variations were expressed as %RSD values of 1.027-1.963% for AUC and 0.150-0.145 for RT. Moreover, the applied method showed stability within a temperature range of 14 °C–35 °C. Analysis showed gallic acid content of 1.773±0.049 mg/g in SNEDDS EAF formulation. Antioxidant activity measured through the DPPH and FRAP methods yielded IC50 values of 4.167±0.552 µg/ml and 20.253±0.619 µg/ml, respectively, while SPF value at SNEDDS concentration of 150 µg/ml was 36.993±0.183.\u0000Conclusion: This study successfully developed a precise, accurate, specific, and stable method for quantifying gallic acid levels in SNEDDS EAF of Melastoma malabathricum leaves in combination with Gentamicin. Therefore, SNEDDS EAF formulation exhibited an effective wound-healing potential, supported by a robust quality control process.","PeriodicalId":507178,"journal":{"name":"International Journal of Applied Pharmaceutics","volume":"45 20","pages":""},"PeriodicalIF":0.0,"publicationDate":"2024-03-07","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"140259398","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
{"title":"BIOSURFACTANTS: SUSTAINABLE ALTERNATIVE TO SYNTHETIC SURFACTANTS AND THEIR APPLICATIONS","authors":"Praveena Poomalai, Janesha Krishnan, Ashwin Ravichandran, Raman Sureshkumar","doi":"10.22159/ijap.2024v16i2.50061","DOIUrl":"https://doi.org/10.22159/ijap.2024v16i2.50061","url":null,"abstract":"Biosurfactants are surface active agents produced by microorganisms, which help reduce surface or interfacial tension between two immiscible liquids like oil and water. In recent years, Due to their environmentally friendly nature and wide range of applications in various industries, they can act as a sustainable alternative to synthetic surfactants. This review article provides an overview of biosurfactants, emphasizing their need for biosurfactants, the production process, and their classification based on molecular weight, charge, and the microorganism they derived. The advantages include biodegradability, biocompatibility, low toxicity, surface activity, and specificity, and various areas where the biosurfactant used are emulsification, thermal stability, pH stability, wetting ability, foaming ability, and spreadability. Research on using biosurfactants in various formulations like nanoparticles, liposomes, transdermal application, nanoemulsion, and nanocapsules is also highlighted in this review to support its application in the medical field. Biosurfactants are also utilized in various fields like the pharmaceuticals, cosmetics, food, and oil industries. However, they have their drawbacks, which include high production costs, variability in production yield, sensitivity to the environment, lack of standardization, hurdles in regulatory approval, and research and development limitations. Despite certain drawbacks, biosurfactant offers a sustainable alternative to synthetic surfactants.","PeriodicalId":507178,"journal":{"name":"International Journal of Applied Pharmaceutics","volume":"20 11","pages":""},"PeriodicalIF":0.0,"publicationDate":"2024-03-07","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"140259902","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
Pasam Jyothirmayi, Arigela Bharathi, D. R. SEKHARA REDDY
{"title":"FORMULATION AND EVALUATION OF MODIFIED PULSATILE CAPSULE FOR CHRONOPHARMACOTHERAPY OF RHEUMATOID ARTHRITIC PAIN","authors":"Pasam Jyothirmayi, Arigela Bharathi, D. R. SEKHARA REDDY","doi":"10.22159/ijap.2024v16i2.49073","DOIUrl":"https://doi.org/10.22159/ijap.2024v16i2.49073","url":null,"abstract":"Objective: The objective of the present study was to design and evaluate pulsincap system for chrono pharmacotherapy of rheumatoid arthritis that combines advantages of both immediate and sustained release technology with the suitable delay of drug release.\u0000Methods: Pulsatile drug delivery system based on pulsincap® technology was designed using mucoadhesive microspheres and Tramadol bilayer tablet plugs. The drug-excipient interaction was carried out by FTIR. Hardness, thickness, lag time, and swelling index all play a role in optimizing tablet plugs. The microspheres were examined for parameters such as particle size, surface morphology, encapsulation efficiency, swelling index, % mucoadhesion, and in vitro dissolution.\u0000Results: In modified pulsincaps, bilayer tablet plug shows drug release within 40 min and hydrogel plugs shows good swelling index and suitable lag time. In microspheres formulations, MF9 is the most suitable among them as it shows better drug content, particle size, surface morphology, in vitro drug release, and release kinetics. The drug is released right away, followed by the dissolution of the enteric coating at pH 6.8, followed by a suitable delay of 6 hours, and then the maximum amount of drug release is 99.62% at the end of 10th h.\u0000Conclusion: The pulsatile delivery system developed with HPMCK4M and tamarindus gum as plugging material showed a satisfactory lag period when compared to Tamarindus gum alone. Drug release can be achieved from treated gelatin capsule and hydrogel plug for a prolonged period by MF9 formulation.","PeriodicalId":507178,"journal":{"name":"International Journal of Applied Pharmaceutics","volume":"2 4","pages":""},"PeriodicalIF":0.0,"publicationDate":"2024-03-07","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"140260136","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
Nur Hasanah, F. Saputri, A. Bustamam, Vannajan SANGHIRAN LEE, Arry Yanuar
{"title":"DECODING THE THERAPEUTIC POTENTIAL OF EMPON-EMPON: A BIOINFORMATICS EXPEDITION UNRAVELING MECHANISMS AGAINST COVID-19 AND ATHEROSCLEROSIS","authors":"Nur Hasanah, F. Saputri, A. Bustamam, Vannajan SANGHIRAN LEE, Arry Yanuar","doi":"10.22159/ijap.2024v16i2.50128","DOIUrl":"https://doi.org/10.22159/ijap.2024v16i2.50128","url":null,"abstract":"Objective: This study aims to elucidate the main compounds and mechanisms of action of Empon-empon (EE), a traditional Indonesian herb used for treating COVID-19 and atherosclerosis, utilizing an integrated network pharmacology and molecular docking approach.\u0000Methods: Active compounds in EE were obtained through the KNApSAcK, screening active compounds using parameters: oral bioavailability (OB) ≥ 30% and drug-likeness (DL) ≥ 0.18. Compound-related target genes were collected from GeneCard, ChemBL, and Traditional Chinese Medicine Systems Pharmacology (TCMSP). Disease targets were obtained from the GeneCard database. The protein-protein interaction (PPI) network was built using STRING and visualized using Cytoscape. Gene ontology (GO) and Kyoto Encyclopedia of Genes and Genomes (KEGG) analysis using ShinyGO. Molecular docking analysis using Autodock Vina in PyRx.\u0000Results: We identified 18 main compounds in EE. PPI analysis obtained 5 central EE targets involved in treating COVID-19 and atherosclerosis, namely E1A Binding Protein P300 (EP300), Heat Shock Protein 90 Alpha Family Class A Member 1 (HSP90AA1), SRC Proto-Oncogene (SRC), Estrogen Receptor 1 (ESR1), and RELA Proto-Oncogene (RELA). GO and KEGG analysis illustrated EE's pharmacological effects through pathways in cancer, lipid and atherosclerosis, and PI3K-Akt signaling, including Coronavirus disease. Catechin and quercetin exhibited the strongest binding affinity to EP300; licarin B and delphinidin to HSP90AA1; epicatechin and delphinidin to SRC; galangin and ellagic acid to ESR1; and guaiacin and licarin B to RELA.\u0000Conclusion: This research provides a strong foundation regarding the main compound and mechanism action of EE in treating atherosclerosis and COVID-19, suggesting potential as a novel therapeutic agent.","PeriodicalId":507178,"journal":{"name":"International Journal of Applied Pharmaceutics","volume":"9 6","pages":""},"PeriodicalIF":0.0,"publicationDate":"2024-03-07","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"140260887","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}