{"title":"通过微流控和喷雾干燥技术设计的维达列汀负载聚合物纳米颗粒可增强抗糖尿病活性","authors":"Eknath Kole, Krishna Jadhav, Zia Khan, Rahul Kumar Verma, Aniruddha Chatterjee, Arun Mujumdar, Jitendra Naik","doi":"10.1186/s43094-024-00736-9","DOIUrl":null,"url":null,"abstract":"<div><h3>Background</h3><p>Vildagliptin (VLG), an antidiabetic agent, presents a potential solution to this widespread affliction. It exhibits notable attributes, such as a high solubility and a shorter elimination half-life. The current study uses a microreactor to fabricate sustained-release VLG-encapsulated cross-linked chitosan–dextran sulfate nanoparticles (VLG-CDNPs). The fabrication was systematically optimized using the design of experiment approach.</p><h3>Results</h3><p>The optimized VLG-CDNPs had an average particle size of 217.4 ± 12.3 nm and an encapsulation efficiency of 78.25 ± 3.0%. Scanning electron microscopy revealed that the nanoparticles had a smooth spherical shape. Spray drying was used for drying, and the reconstitution ability was close to ideal (~ 1.33). In vitro studies revealed sustained VLG release over 12 h, with ~ 58% in acidic and ~ 83% in basic conditions. Cell viability remained at 80% even at 100 μg/mL, and glucose uptake in L6 cells was significantly enhanced with VLG-CDNPs (78.34%) compared to pure VLG (60.91%). VLG-CDNPs also showed moderate inhibitory activity against α-amylase (41.57%) and α-glucosidase (63.48%) compared to pure VLG, which had higher inhibition levels.</p><h3>Conclusion</h3><p>The study’s outcome suggested that the optimized VLG-CDNPs may serve as an effective and promising nanoformulation for managing diabetes mellitus.</p></div>","PeriodicalId":577,"journal":{"name":"Future Journal of Pharmaceutical Sciences","volume":"10 1","pages":""},"PeriodicalIF":3.4000,"publicationDate":"2024-11-12","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://fjps.springeropen.com/counter/pdf/10.1186/s43094-024-00736-9","citationCount":"0","resultStr":"{\"title\":\"Engineered vildagliptin-loaded polymeric nanoparticles via microfluidic and spray drying for enhanced antidiabetic activity\",\"authors\":\"Eknath Kole, Krishna Jadhav, Zia Khan, Rahul Kumar Verma, Aniruddha Chatterjee, Arun Mujumdar, Jitendra Naik\",\"doi\":\"10.1186/s43094-024-00736-9\",\"DOIUrl\":null,\"url\":null,\"abstract\":\"<div><h3>Background</h3><p>Vildagliptin (VLG), an antidiabetic agent, presents a potential solution to this widespread affliction. It exhibits notable attributes, such as a high solubility and a shorter elimination half-life. The current study uses a microreactor to fabricate sustained-release VLG-encapsulated cross-linked chitosan–dextran sulfate nanoparticles (VLG-CDNPs). The fabrication was systematically optimized using the design of experiment approach.</p><h3>Results</h3><p>The optimized VLG-CDNPs had an average particle size of 217.4 ± 12.3 nm and an encapsulation efficiency of 78.25 ± 3.0%. Scanning electron microscopy revealed that the nanoparticles had a smooth spherical shape. Spray drying was used for drying, and the reconstitution ability was close to ideal (~ 1.33). In vitro studies revealed sustained VLG release over 12 h, with ~ 58% in acidic and ~ 83% in basic conditions. Cell viability remained at 80% even at 100 μg/mL, and glucose uptake in L6 cells was significantly enhanced with VLG-CDNPs (78.34%) compared to pure VLG (60.91%). VLG-CDNPs also showed moderate inhibitory activity against α-amylase (41.57%) and α-glucosidase (63.48%) compared to pure VLG, which had higher inhibition levels.</p><h3>Conclusion</h3><p>The study’s outcome suggested that the optimized VLG-CDNPs may serve as an effective and promising nanoformulation for managing diabetes mellitus.</p></div>\",\"PeriodicalId\":577,\"journal\":{\"name\":\"Future Journal of Pharmaceutical Sciences\",\"volume\":\"10 1\",\"pages\":\"\"},\"PeriodicalIF\":3.4000,\"publicationDate\":\"2024-11-12\",\"publicationTypes\":\"Journal Article\",\"fieldsOfStudy\":null,\"isOpenAccess\":false,\"openAccessPdf\":\"https://fjps.springeropen.com/counter/pdf/10.1186/s43094-024-00736-9\",\"citationCount\":\"0\",\"resultStr\":null,\"platform\":\"Semanticscholar\",\"paperid\":null,\"PeriodicalName\":\"Future Journal of Pharmaceutical Sciences\",\"FirstCategoryId\":\"1085\",\"ListUrlMain\":\"https://link.springer.com/article/10.1186/s43094-024-00736-9\",\"RegionNum\":0,\"RegionCategory\":null,\"ArticlePicture\":[],\"TitleCN\":null,\"AbstractTextCN\":null,\"PMCID\":null,\"EPubDate\":\"\",\"PubModel\":\"\",\"JCR\":\"Q2\",\"JCRName\":\"PHARMACOLOGY & PHARMACY\",\"Score\":null,\"Total\":0}","platform":"Semanticscholar","paperid":null,"PeriodicalName":"Future Journal of Pharmaceutical Sciences","FirstCategoryId":"1085","ListUrlMain":"https://link.springer.com/article/10.1186/s43094-024-00736-9","RegionNum":0,"RegionCategory":null,"ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":null,"EPubDate":"","PubModel":"","JCR":"Q2","JCRName":"PHARMACOLOGY & PHARMACY","Score":null,"Total":0}
Engineered vildagliptin-loaded polymeric nanoparticles via microfluidic and spray drying for enhanced antidiabetic activity
Background
Vildagliptin (VLG), an antidiabetic agent, presents a potential solution to this widespread affliction. It exhibits notable attributes, such as a high solubility and a shorter elimination half-life. The current study uses a microreactor to fabricate sustained-release VLG-encapsulated cross-linked chitosan–dextran sulfate nanoparticles (VLG-CDNPs). The fabrication was systematically optimized using the design of experiment approach.
Results
The optimized VLG-CDNPs had an average particle size of 217.4 ± 12.3 nm and an encapsulation efficiency of 78.25 ± 3.0%. Scanning electron microscopy revealed that the nanoparticles had a smooth spherical shape. Spray drying was used for drying, and the reconstitution ability was close to ideal (~ 1.33). In vitro studies revealed sustained VLG release over 12 h, with ~ 58% in acidic and ~ 83% in basic conditions. Cell viability remained at 80% even at 100 μg/mL, and glucose uptake in L6 cells was significantly enhanced with VLG-CDNPs (78.34%) compared to pure VLG (60.91%). VLG-CDNPs also showed moderate inhibitory activity against α-amylase (41.57%) and α-glucosidase (63.48%) compared to pure VLG, which had higher inhibition levels.
Conclusion
The study’s outcome suggested that the optimized VLG-CDNPs may serve as an effective and promising nanoformulation for managing diabetes mellitus.
期刊介绍:
Future Journal of Pharmaceutical Sciences (FJPS) is the official journal of the Future University in Egypt. It is a peer-reviewed, open access journal which publishes original research articles, review articles and case studies on all aspects of pharmaceutical sciences and technologies, pharmacy practice and related clinical aspects, and pharmacy education. The journal publishes articles covering developments in drug absorption and metabolism, pharmacokinetics and dynamics, drug delivery systems, drug targeting and nano-technology. It also covers development of new systems, methods and techniques in pharmacy education and practice. The scope of the journal also extends to cover advancements in toxicology, cell and molecular biology, biomedical research, clinical and pharmaceutical microbiology, pharmaceutical biotechnology, medicinal chemistry, phytochemistry and nutraceuticals.