International Journal of Applied Pharmaceutics最新文献

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UNRAVELLING THE INTERACTION BETWEEN GARCINISIDONE-A AND HER2 PROTEIN IN BREAST CANCER: A COMPUTATIONAL STUDY 揭示加西尼酮-A 与乳腺癌中 her2 蛋白的相互作用:一项计算研究
International Journal of Applied Pharmaceutics Pub Date : 2024-02-15 DOI: 10.22159/ijap.2024.v16s1.24
Mainal Furqan, Dachriyanus, Meri Susanti, Purnawan Pontana Putra, F. Wahyuni
{"title":"UNRAVELLING THE INTERACTION BETWEEN GARCINISIDONE-A AND HER2 PROTEIN IN BREAST CANCER: A COMPUTATIONAL STUDY","authors":"Mainal Furqan, Dachriyanus, Meri Susanti, Purnawan Pontana Putra, F. Wahyuni","doi":"10.22159/ijap.2024.v16s1.24","DOIUrl":"https://doi.org/10.22159/ijap.2024.v16s1.24","url":null,"abstract":"Objective: One substance found in the leaves of Garcinia cowa Roxb that has anticancer properties is garcinisidone-A. The study aims to simulate the docking of garcinisidone-A (Gar-A), molecular dynamics, and predict the ADME by predicting the binding of the HER2 protein in breast cancer cells and developing new drug candidate options for cancer treatment, often starting with computational analysis. \u0000Methods: The research method involves computational utilization of pkCSM applications, Gar-A docking simulation with the HER2 protein using Gnina software version 1.0.2, and molecular dynamics conducted with GROMACS 2022.2 and CHARMMGUI applications. \u0000Results: Gar-A has a molecular weight of less than 500, a Log P value of greater than 5, a limited amount of water solubility, a low level of skin permeability, good intestinal permeability, and a Convolutional Neural Network (CNN) pose score on the HER2 protein of 0.6178. It also does not readily cross the blood-brain barrier, and total clearance values indicate rapid elimination via other excretory routes or enzyme metabolism. Gar-A is thought to have interactions with HER2. There are hydrogen bond interactions with amino acids Lys753 and Asp863, carbon-hydrogen bonds with amino acids Leu785, Ser783, Thr862, and alkyl bonds with amino acids Leu726, Leu852, and Ile767. The stability of the Gar-A-substrate interaction could have been more evident during 100 ns molecular dynamics simulation. \u0000Conclusion: The physicochemical properties of Gar-A align with Lipinski's rule for drug candidates. ADME predictions indicate good intestinal permeability for Gar-A; however, it suggests it cannot penetrate the blood-brain barrier. The docking results reveal that Gar-A has a value close to one which indicates similar action to its natural ligand and molecular dynamics simulations that Gar-A is less stable. The results illustrate that Gar-A has the potential as a breast anticancer.","PeriodicalId":13737,"journal":{"name":"International Journal of Applied Pharmaceutics","volume":null,"pages":null},"PeriodicalIF":0.0,"publicationDate":"2024-02-15","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"139963095","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}
引用次数: 0
OPTIMIZATION AND CHARACTERIZATION OF MICROSPHERES OF BERBERINE HYDROCHLORIDE USING BOX-BEHNKEN DESIGN 采用盒-贝肯设计优化盐酸小檗碱微球并确定其特性
International Journal of Applied Pharmaceutics Pub Date : 2024-01-07 DOI: 10.22159/ijap.2024v16i1.49254
Gautam Kumar, Narendra Kumar Pandey, Vijay Mishra, Suraj Pal Verma, Jitender Singh, BIMLESH KUMAR, Sachin Kumar Singh, D. S. Baghel, Kalvatala Sudhakar, Saurabh Singh
{"title":"OPTIMIZATION AND CHARACTERIZATION OF MICROSPHERES OF BERBERINE HYDROCHLORIDE USING BOX-BEHNKEN DESIGN","authors":"Gautam Kumar, Narendra Kumar Pandey, Vijay Mishra, Suraj Pal Verma, Jitender Singh, BIMLESH KUMAR, Sachin Kumar Singh, D. S. Baghel, Kalvatala Sudhakar, Saurabh Singh","doi":"10.22159/ijap.2024v16i1.49254","DOIUrl":"https://doi.org/10.22159/ijap.2024v16i1.49254","url":null,"abstract":"Objective: The current work sought to optimize Berberine hydrochloride (BBH)-loaded microspheres by examining the link between design parameters and experimental results.\u0000Methods: BBH-loaded microspheres were prepared by using the water-in-oil emulsion cross-linking process and optimized with a three-factor, three-level Box-Behnken design (BBD). Grafted gum polyvinyl alcohol (PVA) ratio (w/w) (A), Revolutions per minute (RPM) (B), and Span 20 (%) (C) were independent variables. The dependent variables were Percent Entrapment Efficiency (% EE) (R1), Percent Drug Loading (% DL) (R2), and Particle Size (µm) (R3). The generated polynomial equations and response surface plots were used to relate the dependent and independent variables. Microscopic examination, %EE, and % DL were determined to evaluate the optimized formulation. Fourier transforms infrared (FT-IR) spectroscopy studies and stability studies of optimized formulation were also carried out.\u0000Results: The optimized formulation (FMS6) had a polymer content of 2% w/v [Grafted gum (36.96): PVA (63.04)], a span 20 (0.78 %), and a prepared at the speed of 1225.92 rpm. The observed responses were close to the improved formulation's predicted values. The particle size, % EE, and % DL were found to be 1.10 µm, 82.79% and 16.48%, respectively. FT-IR spectroscopy study indicated that the drug was entrapped in microspheres.\u0000Conclusion: BBD provides a systematic approach to optimize the BBH microsphere preparation process. Additionally, the stability study results confirmed that FMS6 is not only the ideal formulation but also stable, ensuring its suitability for practical applications.","PeriodicalId":13737,"journal":{"name":"International Journal of Applied Pharmaceutics","volume":null,"pages":null},"PeriodicalIF":0.0,"publicationDate":"2024-01-07","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"139448221","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}
引用次数: 0
OPTIMIZATION OF FAST-DISSOLVING TABLETS OF CARVEDILOL USING 23 FACTORIAL DESIGN 采用 23 个因子设计优化卡维地洛速溶片剂
International Journal of Applied Pharmaceutics Pub Date : 2024-01-07 DOI: 10.22159/ijap.2024v16i1.49535
Anusha Kusuma, S. KUMAR R.
{"title":"OPTIMIZATION OF FAST-DISSOLVING TABLETS OF CARVEDILOL USING 23 FACTORIAL DESIGN","authors":"Anusha Kusuma, S. KUMAR R.","doi":"10.22159/ijap.2024v16i1.49535","DOIUrl":"https://doi.org/10.22159/ijap.2024v16i1.49535","url":null,"abstract":"Objective: Optimization of carvedilol fast-dissolving tablets through a 23 factorial design employing starch hyaluronate as a new superdisintegrating agent.\u0000Methods: The esterification method was used for producing starch hyaluronate. A direct compression process was used to develop carvedilol tablets utilizing a mix of starch hyaluronate (SH) as a novel superdisintegrant, crospovidone, and sodium starch glycolate. The prepared tablets are analyzed for physical characteristics, drug dissolution, in vivo pharmacokinetic, and stability studies.\u0000Results: New superdisintegrant synthesized was a fine, free-flowing crystalline powder. In the DSC study, starch hyaluronate had no interaction with the drug. NMR and FTIR investigations supported the ester connection between starch and hyaluronic acid. CF2, the optimized formulation, had the shortest disintegration time of 26±2 seconds. The percentage of drugs dissolved in ten minutes from the optimized composition was 93.4±1.32%. The optimized composition achieved peak plasma concentration in a short time and demonstrated higher relative bioavailability for the drug.\u0000Conclusion: A formula containing a 5% concentration of starch hyaluronate was optimized and has a proper potential for application in the formulation of rapidly disintegrating tablets, in addition to improving clinical obedience throughout the efficacious treatment of hypertension.","PeriodicalId":13737,"journal":{"name":"International Journal of Applied Pharmaceutics","volume":null,"pages":null},"PeriodicalIF":0.0,"publicationDate":"2024-01-07","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"139448799","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}
引用次数: 0
PREPARATION AND SOLID-STATE CHARACTERIZATION OF KETOPROFEN-SUCCINIC ACID-SACCHARIN CO-CRYSTAL WITH IMPROVED SOLUBILITY 具有更好溶解性的酮洛芬-琥珀酸-糖精共晶体的制备及固态表征
International Journal of Applied Pharmaceutics Pub Date : 2024-01-07 DOI: 10.22159/ijap.2024v16i1.48829
Teguh Imanto, E. R. Wikantyasning, Setyo Nurwaini, Monica Amalia, N. Sambudi, N. Y. Harun
{"title":"PREPARATION AND SOLID-STATE CHARACTERIZATION OF KETOPROFEN-SUCCINIC ACID-SACCHARIN CO-CRYSTAL WITH IMPROVED SOLUBILITY","authors":"Teguh Imanto, E. R. Wikantyasning, Setyo Nurwaini, Monica Amalia, N. Sambudi, N. Y. Harun","doi":"10.22159/ijap.2024v16i1.48829","DOIUrl":"https://doi.org/10.22159/ijap.2024v16i1.48829","url":null,"abstract":"Objective: This study aimed to improve the solubility of Ketoprofen, a non-steroidal anti-inflammatory drug (NSAID) that belongs to the Biopharmaceutical Classification System (BCS) Class II, through co-crystallization using succinic acid and saccharin coformers in a 1:1:1 and 2:1:1 molar ratio.\u0000Methods: The slurry method was utilized to prepare the ketoprofen co-crystals, which were then subjected to various physical-chemical characterization techniques such as melting point determination, dissolution studies, differential scanning calorimetry (DSC), X-ray diffraction (XRD), and Fourier transform infrared (FTIR) spectroscopy.\u0000Results: The results showed that the 1:1:1 molar ratio of ketoprofen-succinic acid-saccharin co-crystal (Formula 1) exhibited higher solubility than the solubility standard of Ketoprofen and the 2:1:1 molar ratio of the co-crystal (Formula 2). The dissolution profile (Q30) of Formula 1, Formula 2, and standard Ketoprofen were 96.73±1.77, 93.09±1.16, and 70.22±4.72, respectively. These findings suggest that co-crystallization with succinic acid and saccharin conformers using the slurry method can significantly enhance the solubility of Ketoprofen.\u0000Conclusion: The 1:1:1 molar ratio of ketoprofen-succinic acid-saccharin co-crystal (Formula 1) was the most effective formulation among the tested samples, demonstrating the highest solubility. This research may provide valuable insights for developing novel drug formulations with improved bioavailability and therapeutic efficacy.","PeriodicalId":13737,"journal":{"name":"International Journal of Applied Pharmaceutics","volume":null,"pages":null},"PeriodicalIF":0.0,"publicationDate":"2024-01-07","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"139449119","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}
引用次数: 1
FORMULATION AND EVALUATION OF TRANSDERMAL PATCHES FROM ELEUTHERINE BULBOSA URB. BULB EXTRACT WITH PLASTICIZER VARIATIONS 榄香脂透皮贴剂的制备与评估鳞茎提取物与增塑剂的变化
International Journal of Applied Pharmaceutics Pub Date : 2024-01-07 DOI: 10.22159/ijap.2024v16i1.46421
Wahyudin Bin Jamaludin, Rahmi Muthia, K. Kartini, Finna Setiawan, Siti Juhrah, Nuril Yulida
{"title":"FORMULATION AND EVALUATION OF TRANSDERMAL PATCHES FROM ELEUTHERINE BULBOSA URB. BULB EXTRACT WITH PLASTICIZER VARIATIONS","authors":"Wahyudin Bin Jamaludin, Rahmi Muthia, K. Kartini, Finna Setiawan, Siti Juhrah, Nuril Yulida","doi":"10.22159/ijap.2024v16i1.46421","DOIUrl":"https://doi.org/10.22159/ijap.2024v16i1.46421","url":null,"abstract":"Objective: This research aimed to develop a transdermal drug delivery system from Eleutherine bulbosa Urb. bulbs as an alternative treatment with minimum side effects compared to other pain medications and increased drug penetration by determining the optimum formula(s) for transdermal patches prepared with varying plasticizer concentrations.\u0000Methods: Eleutherine bulbosa Urb. bulbs were extracted by maceration using 96% ethanol. The extract was formed into transdermal patches using the solvent casting method with six formulations (F1-F6) and different types and concentrations of the plasticizer: polyethylene glycol (PEG) 400 or dibutyl phthalate. The derived patches were then evaluated for their organoleptic properties, homogeneity, weight uniformity, thickness, folding endurance, pH level, moisture content, and acceptability (hedonic scale).\u0000Results: The evaluation of the physical properties found that all patches were dark brown, opaque, smooth-textured, and had a typical odor of the bulb’s ethanol extract and uniform weight and thickness. Other characteristics included pH ranging from 5.0±0.00 to 5.86±0.04 and a moisture content between 1.04±0.04% and 4.13±0.08%. In addition, the folding endurance was 267 times for F1 and >300 times for F2-F6. The acceptability test using the five-point hedonic scale showed different preferences for these formulas.\u0000Conclusion: F6 is the optimum formula for producing transdermal patches with excellent physical properties.","PeriodicalId":13737,"journal":{"name":"International Journal of Applied Pharmaceutics","volume":null,"pages":null},"PeriodicalIF":0.0,"publicationDate":"2024-01-07","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"139448442","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}
引用次数: 0
APTAMERS: NANOMATERIALS AS A POTENTIAL AGENT FOR ANTIVIRAL THERAPEUTIC DRUG DELIVERY DEVELOPMENT: A SYSTEMATIC LITERATURE REVIEW aptamers:作为抗病毒治疗药物输送开发潜在媒介的纳米材料:系统文献综述
International Journal of Applied Pharmaceutics Pub Date : 2024-01-07 DOI: 10.22159/ijap.2024v16i1.48266
M. R. Reddy, S. K. Gubbiyappa, Shaik Harun Rasheed, K. Parameshwar
{"title":"APTAMERS: NANOMATERIALS AS A POTENTIAL AGENT FOR ANTIVIRAL THERAPEUTIC DRUG DELIVERY DEVELOPMENT: A SYSTEMATIC LITERATURE REVIEW","authors":"M. R. Reddy, S. K. Gubbiyappa, Shaik Harun Rasheed, K. Parameshwar","doi":"10.22159/ijap.2024v16i1.48266","DOIUrl":"https://doi.org/10.22159/ijap.2024v16i1.48266","url":null,"abstract":"Chemotherapeutic experts have been utilised to cure a variety of disorders, but their practical application is restricted due to their regrettable selectivity and outrageous fundamental optional effects. Short single-stranded DNA or RNA oligonucleotides known as aptamers are released from randomised libraries and have strong propensity and differentiation towards targets like antibodies as well as characterised structures and ties to targets like proteins. They commonly suppress protein interactions while restricting proteins, which may elicit positive effects like threat. Aptamers have recently demonstrated their amazing promise for use in medicines, biosensors, and bioimaging thanks to a number of advantages, such as minimal immunogenicity, simplicity of giant degree blend, low pack to-bunch collection, genuinely substance modification, and programmability. At any rate, the steady for the most part accomplishment speed of aptamer is far from being brilliant, despite everything needs to overwhelm the gigantic obstruction in propensity, constancy for utilitarian application, explicit illness cell affirmation. The sensible method of controlling the binding execution of aptamers and dealing with their show in the practical application is of great significance and these single-abandoned DNA or RNA aptamers could outline with astoundingly poisonous chemotherapy drugs, hurts, strong RNAs or different particles as novel aptamer-drug structures, which are prepared to do endlessly out working on the obliging plentifulness and decreasing the critical danger of solutions and have unprecedented possible in living spaces for appointed ailment treatment. In this survey, we have extensively covered and summarised the ongoing improvements in the aptamer-drug structure philosophy for designated drug transport in the assessment methodologies of aptamers for unambiguous disease biomarkers. A modified strategy utilising aptamers could be a reliable system for quick and precise advancement of biopharmaceutics for use in infection-related treatment, especially in light of the enormous advances in modernised thinking for protein and RNA structure conjectures. Additionally, the likelihood of future conception is also summarised.","PeriodicalId":13737,"journal":{"name":"International Journal of Applied Pharmaceutics","volume":null,"pages":null},"PeriodicalIF":0.0,"publicationDate":"2024-01-07","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"139448482","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}
引用次数: 0
VIRTUAL SCREENING OF FDA-APPROVED DRUGS BY MOLECULAR DOCKING AND DYNAMICS SIMULATION TO RECOGNIZE POTENTIAL INHIBITORS AGAINST MYCOBACTERIUM TUBERCULOSIS ENOYL-ACYL CARRIER PROTEIN REDUCTASE ENZYME 通过分子对接和动力学模拟对 FDA 批准的药物进行虚拟筛选,以识别针对结核分枝杆菌烯酰-酰载体蛋白还原酶的潜在抑制剂
International Journal of Applied Pharmaceutics Pub Date : 2024-01-07 DOI: 10.22159/ijap.2024v16i1.49471
H. Odhar, Ahmed Fadhil Hashim, S. Ahjel, S. Humadi
{"title":"VIRTUAL SCREENING OF FDA-APPROVED DRUGS BY MOLECULAR DOCKING AND DYNAMICS SIMULATION TO RECOGNIZE POTENTIAL INHIBITORS AGAINST MYCOBACTERIUM TUBERCULOSIS ENOYL-ACYL CARRIER PROTEIN REDUCTASE ENZYME","authors":"H. Odhar, Ahmed Fadhil Hashim, S. Ahjel, S. Humadi","doi":"10.22159/ijap.2024v16i1.49471","DOIUrl":"https://doi.org/10.22159/ijap.2024v16i1.49471","url":null,"abstract":"Objective: This in silico study is aimed at identification of new possible inhibitors against Mycobacterium tuberculosis InhA enzyme by screening a library of FDA-approved drugs.\u0000Methods: In this in silico study, a library of FDA-approved drugs was screened by molecular docking against the monomer of enoyl-acyl carrier protein reductase to recognize potential inhibitors. Then, those best drugs with minimum docking energy were subjected to molecular dynamics simulation.\u0000Results: Out of the top ten docking hits, only revefenacin was able to maintain the closet proximity to InhA enzyme binding pocket during the two rounds of dynamics simulation. Analysis of molecular dynamics (MD) simulation data indicated that the antimuscarinic drug revefenacin has a ligand movement Root-Mean-Square Deviation (RMSD) that didn’t exceed 4 Angstrom. Also, in this MD study, revefenacin has a superior binding energy of -35.59 Kcal/mol as compared to -13.88 Kcal/mol for the other hit ergotamine. These favorable MD simulation records for revefenacin can be explained by its ability to continuously interact with enzyme binding pocket by two hydrogen bonds.\u0000Conclusion: We report that the antimuscarinic drug revefenacin may have the potential to inhibit the enoyl-acyl carrier protein reductase for Mycobacterium tuberculosis. However, these preliminary results must be further evaluated by in vitro and in vivo studies.","PeriodicalId":13737,"journal":{"name":"International Journal of Applied Pharmaceutics","volume":null,"pages":null},"PeriodicalIF":0.0,"publicationDate":"2024-01-07","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"139448596","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}
引用次数: 0
THE POTENTIAL EFFECT OF APORPHINE ALKALOIDS FROM NELUMBO NUCIFERA GAERTN. AS ANTI-BREAST CANCER BASED ON NETWORK PHARMACOLOGY AND MOLECULAR DOCKING 基于网络药理学和分子对接的罂粟碱抗乳腺癌的潜在作用研究基于网络药理学和分子对接的抗乳腺癌潜在作用
International Journal of Applied Pharmaceutics Pub Date : 2024-01-07 DOI: 10.22159/ijap.2024v16i1.49171
Adrian, Muhammad Fauzan Lubis, R. A. Syahputra, Ririn Astyka, S. Sumaiyah, Muhammad Andika, Yudha Harahap, Zahratul Aini, Muhammad Fauzan Lubis
{"title":"THE POTENTIAL EFFECT OF APORPHINE ALKALOIDS FROM NELUMBO NUCIFERA GAERTN. AS ANTI-BREAST CANCER BASED ON NETWORK PHARMACOLOGY AND MOLECULAR DOCKING","authors":"Adrian, Muhammad Fauzan Lubis, R. A. Syahputra, Ririn Astyka, S. Sumaiyah, Muhammad Andika, Yudha Harahap, Zahratul Aini, Muhammad Fauzan Lubis","doi":"10.22159/ijap.2024v16i1.49171","DOIUrl":"https://doi.org/10.22159/ijap.2024v16i1.49171","url":null,"abstract":"Objective: To demonstrate the efficacy and benefits of aporphine alkaloids from Nelumbo nucifera Gaertn. as anti-breast cancer agents.\u0000Methods: In this study, a combination of network pharmacology and molecular docking was used to investigate the pharmacological actions and underlying mechanisms of action of nuciferine, nor-nuciferine, and roemerine against breast cancer.\u0000Results: Fifty-five potential targets of compounds against breast cancer were identified. The Epidermal Growth Factor Receptor (EGFR), Mitogen-Activated Protein Kinase 8 (MAPK8), Janus Kinase 2 (JAK2), Inhibitor of Nuclear Factor Kappa B Kinase Subunit Beta (IKBKB), and Protein Kinase C Epsilon (PRKCE) were identified as the top five targets of compounds against breast cancer. Molecular docking demonstrated that these compounds could bind spontaneously to the screened top 4 targeted proteins.\u0000Conclusion: The present study demonstrates that these compounds have pharmacological effects against breast cancer via a multi-target and multi-pathway manner.","PeriodicalId":13737,"journal":{"name":"International Journal of Applied Pharmaceutics","volume":null,"pages":null},"PeriodicalIF":0.0,"publicationDate":"2024-01-07","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"139448602","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}
引用次数: 0
REVOLUTIONIZING THERAPEUTIC DELIVERY: DIOSGENIN-LOADED SOLID LIPID NANOPARTICLES UNLEASH ADVANCED CARRIERS 彻底改变治疗递送方式:加载地奥孕宁的固体脂质纳米颗粒释放出先进载体的能量
International Journal of Applied Pharmaceutics Pub Date : 2024-01-07 DOI: 10.22159/ijap.2024v16i1.49306
Ramsha Aslam, V. Tiwari, Prashant Upadhyay, Abhishek Tiwari
{"title":"REVOLUTIONIZING THERAPEUTIC DELIVERY: DIOSGENIN-LOADED SOLID LIPID NANOPARTICLES UNLEASH ADVANCED CARRIERS","authors":"Ramsha Aslam, V. Tiwari, Prashant Upadhyay, Abhishek Tiwari","doi":"10.22159/ijap.2024v16i1.49306","DOIUrl":"https://doi.org/10.22159/ijap.2024v16i1.49306","url":null,"abstract":"Objective: The pharmaceutical industry has paid a lot of attention to solid lipid nanoparticles (SLN) because they show promise as drug delivery vehicles. The purpose of this research was to create and characterize SLN loaded with Diosgenin.\u0000Methods: To create SLN, the natural bioactive component diosgenin was encapsulated in a solid lipid matrix of compritol ATO 888. A modified solvent emulsification-evaporation process was used to create the SLN. Using a Box-Behnken Design (BBD), we were able to identify the optimal values for the drug-to-solid lipid ratio, surfactant concentration, and ultrasonication period that constitute an effective formulation.\u0000Results: It was found that the improved formulation had particle sizes of 170.96 nm, polydispersity indices (PDI) of 0.231, and entrapment efficiencies of 64.549±0.553% %. The zeta potential value of -40.2 mV was indicative of a steady dispersion. The average particle size of the SLN was measured to be 103.1429 nm, and their spherical morphology was validated by scanning electron microscopy (SEM) imaging. The optimized formulation did not undergo any chemical changes, as shown by differential scanning calorimetry (DSC) testing. The in vitro drug release investigation showed that the SLN released Diosgenin continuously for 28 h.\u0000Conclusion: The optimized formulation of SLN, achieved through the BBD, offers a promising strategy to improve drug solubility while ensuring controlled drug release and long-term storage stability.","PeriodicalId":13737,"journal":{"name":"International Journal of Applied Pharmaceutics","volume":null,"pages":null},"PeriodicalIF":0.0,"publicationDate":"2024-01-07","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"139449126","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}
引用次数: 0
THE SIMULTANEOUS QUANTIFICATION OF RIFAMPICIN AND ISONIAZID IN PATIENTS WITH TUBERCULOSIS APPLIED TO VOLUMETRIC ABSORPTIVE MICROSAMPLING DEVICES USING HIGH-PERFORMANCE LIQUID CHROMATOGRAPHY 利用高效液相色谱法在体积吸收式微型取样装置中同时定量检测结核病患者体内的利福平和异烟肼
International Journal of Applied Pharmaceutics Pub Date : 2024-01-07 DOI: 10.22159/ijap.2024v16i1.49108
Hema Novita Rendati, Y. Harahap, Rahmayanti
{"title":"THE SIMULTANEOUS QUANTIFICATION OF RIFAMPICIN AND ISONIAZID IN PATIENTS WITH TUBERCULOSIS APPLIED TO VOLUMETRIC ABSORPTIVE MICROSAMPLING DEVICES USING HIGH-PERFORMANCE LIQUID CHROMATOGRAPHY","authors":"Hema Novita Rendati, Y. Harahap, Rahmayanti","doi":"10.22159/ijap.2024v16i1.49108","DOIUrl":"https://doi.org/10.22159/ijap.2024v16i1.49108","url":null,"abstract":"Objective: Rifampicin and isoniazid are the main tuberculosis treatment regimens requiring blood level measurement to optimize the treatment process. This study aims to analyze rifampicin and isoniazid quantitatively in volumetric absorptive microsampling (VAMS) prepared from a small volume of TB patients using HPLC.\u0000Methods: Analytes on the VAMS tip were extracted using 1000 ml of acetonitrile containing 10 µg/ml of cilostazol as an internal standard. Analytical separation was performed on the C-18 column at 40 ℃ with a mobile phase mixture of 50 mmol ammonium acetate buffer pH 5.0-acetonitrile-methanol (40:30:30), flow rate 0.5 ml/min. The analysis was carried out with the calibration curve over a range of 1.0–30 µg/ml for rifampicin and 0.4-20 µg/ml for isoniazid.\u0000Results: Analyte analysis in 21 patients showed that the measured value of rifampicin was 3.39–16.77 µg/ml, and isoniazid was 2.63–10.43 µg/ml at 2 h post-dose. 52.38% of patients had low blood concentrations in at least one of the drugs, 28.57% of the patients were in the therapeutic range, and 23.81% had a high blood concentration of isoniazid alone.\u0000Conclusion: The concentration of rifampicin and isoniazid in 21 tuberculosis patients varied. Dose adjustment is needed because most patients had low blood concentrations of one of the drugs, and a limited number had a high blood isoniazid concentration alone. Only some patients simultaneously had plasma concentrations within the target range of the drugs. This method was valid and reliably utilized for therapeutic drug monitoring of antituberculosis.","PeriodicalId":13737,"journal":{"name":"International Journal of Applied Pharmaceutics","volume":null,"pages":null},"PeriodicalIF":0.0,"publicationDate":"2024-01-07","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"139448106","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}
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