Assay and drug development technologies最新文献_第7页

Oral Gastroretentive Film of Lacidipine for the Treatment of Gastroparesis. 口服拉西地平胃保留膜治疗胃轻瘫。

IF 1.8 4区医学

Assay and drug development technologies Pub Date : 2023-04-01 DOI: 10.1089/adt.2022.091

Mrunali Navin Kantak, Lalit Kumar, Prashant Jivaji Bhide, Rupesh Kalidas Shirodkar

{"title":"Oral Gastroretentive Film of Lacidipine for the Treatment of Gastroparesis.","authors":"Mrunali Navin Kantak, Lalit Kumar, Prashant Jivaji Bhide, Rupesh Kalidas Shirodkar","doi":"10.1089/adt.2022.091","DOIUrl":"https://doi.org/10.1089/adt.2022.091","url":null,"abstract":"The research work was aimed to formulate and evaluate gastroretentive mucoadhesive film of calcium channel blocker, Lacidipine for treatment of gastroparesis. Box-Behnken design was used for preparation of optimized formulation using solvent casting method. In this design, different concentrations of mucoadhesive polymers HPMC E15, Eudragit RL100, and Eudragit RS100 were considered as independent variables and its effect on responses like percent drug release, swelling index at 12 h, and folding endurance of the film were examined. Drug and polymer compatibility studies were performed using Fourier transform infrared spectroscopy and differential scanning calorimetry. Optimized formulation was evaluated for organoleptic properties, weight variation, thickness, swelling index, folding endurance, drug content, tensile strength, percent elongation, drug release, and percent moisture loss. The results revealed that the film possessed considerable flexibility and smoothness, and in vitro drug release was found to be 95.22% ± 0.93% at the end of 12 h. Scanning electron microscopy imaging of film displayed smooth, uniform, and porous surface texture. The dissolution followed Higuchi's model and Hixson Crowell model displayed non-Fickian drug release mechanism. Furthermore, the film was incorporated in capsule and the presence of capsule showed no effect on the drug release profile. In addition, no change was observed in the appearance, drug content, swelling index, folding endurance, and drug release upon storage at 25°C ± 2°C and 60% ± 5% relative humidity for 3 months. Collectively, the study revealed that gastroretentive mucoadhesive film of Lacidipine could serve as an effective and alternate site-specific targeted delivery in the management of gastroparesis.","PeriodicalId":8586,"journal":{"name":"Assay and drug development technologies","volume":"21 3","pages":"97-109"},"PeriodicalIF":1.8,"publicationDate":"2023-04-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"9566760","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

引用次数: 0

Identification of Potent, Selective, and Peripherally Restricted Serotonin Receptor 2B Antagonists from a High-Throughput Screen. 通过高通量筛选鉴定强效、选择性和外周限制性羟色胺受体 2B 拮抗剂

IF 1.8 4区医学

Assay and drug development technologies Pub Date : 2023-04-01 Epub Date: 2023-03-17 DOI: 10.1089/adt.2022.116

Aaron M Bender, Michael S Valentine, Joshua A Bauer, Emily Days, Craig W Lindsley, W David Merryman

引用次数: 0

Pharmaceutical Methods for Enhancing the Dissolution of Poorly Water-Soluble Drugs. 提高难水溶性药物溶出度的药学方法。

IF 1.8 4区医学

Assay and drug development technologies Pub Date : 2023-02-01 DOI: 10.1089/adt.2022.119

Tahir Mahmood, Rai M Sarfraz, Asmara Ismail, Muhammad Ali, Abdur Rauf Khan

{"title":"Pharmaceutical Methods for Enhancing the Dissolution of Poorly Water-Soluble Drugs.","authors":"Tahir Mahmood, Rai M Sarfraz, Asmara Ismail, Muhammad Ali, Abdur Rauf Khan","doi":"10.1089/adt.2022.119","DOIUrl":"https://doi.org/10.1089/adt.2022.119","url":null,"abstract":"\u0000 Low water solubility is the main hindrance in the growth of pharmaceutical industry. Approximately 90% of newer molecules under investigation for drugs and 40% of novel drugs have been reported to have low water solubility. The key and thought-provoking task for the formulation scientists is the development of novel techniques to overcome the solubility-related issues of these drugs. The main intention of present review is to depict the conventional and novel strategies to overcome the solubility-related problems of Biopharmaceutical Classification System Class-II drugs. More than 100 articles published in the last 5 years were reviewed to have a look at the strategies used for solubility enhancement. pH modification, salt forms, amorphous forms, surfactant solubilization, cosolvency, solid dispersions, inclusion complexation, polymeric micelles, crystals, size reduction, nanonization, proliposomes, liposomes, solid lipid nanoparticles, microemulsions, and self-emulsifying drug delivery systems are the various techniques to yield better bioavailability of poorly soluble drugs. The selection of solubility enhancement technique is based on the dosage form and physiochemical characteristics of drug molecules.\u0000 ","PeriodicalId":8586,"journal":{"name":"Assay and drug development technologies","volume":"21 2","pages":"65-79"},"PeriodicalIF":1.8,"publicationDate":"2023-02-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"9512702","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

引用次数: 0

Drug Repurposing Patent Applications October-December 2022. 药物再利用专利申请2022年10月至12月。

IF 1.8 4区医学

Assay and drug development technologies Pub Date : 2023-02-01 DOI: 10.1089/adt.2023.008

Hermann A M Mucke

引用次数: 0

A Sojourn on Liposomal Delivery System: Recent Advances and Future Prospects. 脂质体递送系统的研究进展及未来展望。

IF 1.8 4区医学

Assay and drug development technologies Pub Date : 2023-02-01 DOI: 10.1089/adt.2022.089

Simranjeet Kaur, Dilpreet Singh

{"title":"A Sojourn on Liposomal Delivery System: Recent Advances and Future Prospects.","authors":"Simranjeet Kaur, Dilpreet Singh","doi":"10.1089/adt.2022.089","DOIUrl":"https://doi.org/10.1089/adt.2022.089","url":null,"abstract":"\u0000 Liposomes are unique novel drug delivery carriers that favor the effective transportation of pharmaceuticals. These vesicles acquire one or more phospholipid bilayer membranes, and an inner aqueous core can carry both aqueous and lipid drugs. While hydrophilic molecules can be confined in the aqueous core, hydrophobic molecules are injected into the bilayer membrane. Liposomes have many benefits as a drug delivery method, including biocompatibility, the capacity to carry large drug payloads, and a variety of physicochemical and biological parameters that can be altered to influence their biological characteristics. In addition, being a size of 10-100 nm range can have numerous additional benefits, including enhanced pharmacokinetics, clever escape from the reticuloendothelial system, greater in vivo stability, longer and site-specific administration, and increased internalization in tumor tissue (enhanced permeability and retention impact). The current review focuses on the structural composition of liposomes, formulation technologies, and suitable case studies for optimizing biopharmaceutical performance. Moreover, clinical trials and marketed formulations of liposomes have been also stated in the prior art.\u0000 ","PeriodicalId":8586,"journal":{"name":"Assay and drug development technologies","volume":"21 2","pages":"48-64"},"PeriodicalIF":1.8,"publicationDate":"2023-02-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"9517923","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

引用次数: 0

A Critical Sojourn of Polymeric Micelles: Technological Concepts, Recent Advances, and Future Prospects. 高分子胶束的关键逗留:技术概念、最新进展和未来展望。

IF 1.8 4区医学

Assay and drug development technologies Pub Date : 2023-02-01 DOI: 10.1089/adt.2022.079

Princi Verma, G D Gupta, Tanmay S Markandeywar, Dilpreet Singh

{"title":"A Critical Sojourn of Polymeric Micelles: Technological Concepts, Recent Advances, and Future Prospects.","authors":"Princi Verma, G D Gupta, Tanmay S Markandeywar, Dilpreet Singh","doi":"10.1089/adt.2022.079","DOIUrl":"https://doi.org/10.1089/adt.2022.079","url":null,"abstract":"Poorly soluble drug molecules/phytoconstituents are still a growing concern for biopharmaceutical delivery in the body. Polymeric micelles are the amphiphilic block copolymers and have been widely investigated as targeted nanocarriers for the treatment of various ailments. The versatility of nanocarriers is the self-assembling properties in the aqueous medium and forms a stable isotropic system in vivo. The hydrophobic core-hydrophilic shell configuration of the polymers used to the mixed micelles makes easy encapsulation of hydrophobic and hydrophilic drugs into the core. Polymeric micelles can also be combined with targeting ligands that increase their uptake by specific cells, decreasing off-target effects, and provide enhanced therapeutic effect. In the present review, we primarily focused on a critical appraisal of Polymeric micelles along with the method of preparation, mechanism of micelle formulation, and the ongoing formulations under clinical trials. In addition, the biological applications of this isotropic nanocarrier have been duly presented in each route of administration along with suitable case studies.","PeriodicalId":8586,"journal":{"name":"Assay and drug development technologies","volume":"21 2","pages":"31-47"},"PeriodicalIF":1.8,"publicationDate":"2023-02-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"9512679","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"医学","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 Optimization of Liposome Containing Thermosensitive In Situ Nasal Hydrogel System for Brain Delivery of Sumatriptan Succinate. 含热敏鼻腔水凝胶脂质体脑给药系统的制备与优化。

IF 1.8 4区医学

Assay and drug development technologies Pub Date : 2023-01-01 DOI: 10.1089/adt.2022.088

Dyandevi Mathure, Ashish Dilip Sutar, Hemantkumar Ranpise, Atmaram Pawar, Rajendra Awasthi

{"title":"Preparation and Optimization of Liposome Containing Thermosensitive In Situ Nasal Hydrogel System for Brain Delivery of Sumatriptan Succinate.","authors":"Dyandevi Mathure, Ashish Dilip Sutar, Hemantkumar Ranpise, Atmaram Pawar, Rajendra Awasthi","doi":"10.1089/adt.2022.088","DOIUrl":"https://doi.org/10.1089/adt.2022.088","url":null,"abstract":"Drug absorption is improved by the intranasal route's wide surface area and avoidance of first-pass metabolism. For the treatment of central nervous system diseases such as migraine, intranasal administration delivers the medication to the brain. The study's purpose was to develop an in situ nasal hydrogel that contained liposomes that were loaded with sumatriptan succinate (SS). A thin-film hydration approach was used to create liposomes, and a 32 factorial design was used to optimize them. The optimized liposomes had a spherical shape, a 171.31 nm particle size, a high drug encapsulation efficiency of 83.54%, and an 8-h drug release of 86.11%. To achieve in situ gel formation, SS-loaded liposomes were added to the liquid gelling system of poloxamer-407, poloxamer-188, and sodium alginate. The final product was tested for mucoadhesive strength, viscosity, drug content, gelation temperature, and gelation time. Following intranasal delivery, in vivo pharmacokinetic investigations showed a significant therapeutic concentration of the medication in the brain with a Cmax value of 167 ± 78 ng/mL and an area under the curve value of 502 ± 63 ng/min·mL. For SS-loaded liposomal thermosensitive nasal hydrogel, significantly higher values of the nose-to-brain targeting parameters, that is, drug targeting index (2.61) and nose-to-brain drug direct transport (57.01%), confirmed drug targeting to the brain through the nasal route. Liposomes containing thermosensitive in situ hydrogel demonstrated potential for intranasal administration of SS.","PeriodicalId":8586,"journal":{"name":"Assay and drug development technologies","volume":"21 1","pages":"3-16"},"PeriodicalIF":1.8,"publicationDate":"2023-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"9301249","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

引用次数: 3

On the Recent Changes to Animal Protection Measures in United States Food and Drug Administration Policy. 论美国食品和药物管理局政策中动物保护措施的最新变化。

IF 1.8 4区医学

Assay and drug development technologies Pub Date : 2023-01-01 DOI: 10.1089/adt.2023.29103.bjm

Bruce J Melancon

引用次数: 0

Design, Synthesis, and Biological Evaluation of Novel Dihydropyrimidinone Derivatives as Potential Anticancer Agents and Tubulin Polymerization Inhibitors. 新型二氢嘧啶衍生物抗癌和微管蛋白聚合抑制剂的设计、合成和生物学评价。

IF 1.8 4区医学

Assay and drug development technologies Pub Date : 2023-01-01 DOI: 10.1089/adt.2022.085

Ramkaran Rawal, Praveen K Gupta, Bhupinder Kumar, Rohit Bhatia

{"title":"Design, Synthesis, and Biological Evaluation of Novel Dihydropyrimidinone Derivatives as Potential Anticancer Agents and Tubulin Polymerization Inhibitors.","authors":"Ramkaran Rawal, Praveen K Gupta, Bhupinder Kumar, Rohit Bhatia","doi":"10.1089/adt.2022.085","DOIUrl":"https://doi.org/10.1089/adt.2022.085","url":null,"abstract":"The severity and prevalence of cancer in modern time are a huge global health burden. Continuous efforts are being made toward the development of newer therapeutic candidates to treat and manage this ailment. The dihydropyrimidinone scaffold is one of the key nuclei that have been highly explored and investigated against cancer. It has the potential to combat the consequences of cancer by interacting with several biological targets. Tubulin polymerization inhibition is one such strategy to prevent the progression of cancer. In the presented work, we have synthesized a series of sixteen dihydropyrimidinone derivatives by following a rational drug design. The synthesized compounds have been characterized by 1H NMR and 13C NMR and were further evaluated for cytotoxic activity against breast cancer cell lines (MCF-7 and MDA-MB-231), lung cancer cell lines (A549), and colon cancer cell lines (HCT-116). Compounds 5D and 5P were found most potent and revealed a better cytotoxic activity compared with the standard drug colchicine. Furthermore, the tubulin polymerization inhibition assay revealed that compound 5D showed better inhibition than colchicines, whereas compound 5P revealed an almost equal inhibition to that of colchicine. Furthermore, to investigate the possible mode of action and binding patterns, compounds 5P and 5D were subjected to molecular docking against tubulin (Protein Data Bank ID: ISA0). The results showed that compounds revealed significant interactions and were well occupied inside the cavity of tubulin. The compounds 5D and 5P may serve as new leads in drug development against cancer.","PeriodicalId":8586,"journal":{"name":"Assay and drug development technologies","volume":"21 1","pages":"17-28"},"PeriodicalIF":1.8,"publicationDate":"2023-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"10741939","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

引用次数: 0

Acknowledgment of Reviewers 2022. 审稿人致谢2022。

IF 1.8 4区医学

Assay and drug development technologies Pub Date : 2023-01-01 DOI: 10.1089/adt.2022.29102.ack

引用次数: 0