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

IF 3.4 Q2 PHARMACOLOGY & PHARMACY
Eknath Kole, Krishna Jadhav, Zia Khan, Rahul Kumar Verma, Aniruddha Chatterjee, Arun Mujumdar, Jitendra Naik
{"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,&nbsp;Krishna Jadhav,&nbsp;Zia Khan,&nbsp;Rahul Kumar Verma,&nbsp;Aniruddha Chatterjee,&nbsp;Arun Mujumdar,&nbsp;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,&nbsp;Krishna Jadhav,&nbsp;Zia Khan,&nbsp;Rahul Kumar Verma,&nbsp;Aniruddha Chatterjee,&nbsp;Arun Mujumdar,&nbsp;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}
引用次数: 0

摘要

背景维达列汀(VLG)是一种抗糖尿病药物,为解决这一普遍存在的问题提供了一种潜在的解决方案。它具有高溶解度和较短的消除半衰期等显著特性。目前的研究使用微反应器来制造包封交联壳聚糖-硫酸葡聚糖的缓释 VLG 纳米粒子(VLG-CDNPs)。结果优化后的 VLG-CDNPs 平均粒径为 217.4 ± 12.3 nm,封装效率为 78.25 ± 3.0%。扫描电子显微镜显示,纳米颗粒呈光滑球形。干燥采用喷雾干燥法,重组能力接近理想水平(~ 1.33)。体外研究显示,VLG 可在 12 小时内持续释放,酸性条件下为 58%,碱性条件下为 83%。与纯 VLG(60.91%)相比,VLG-CDNPs 显著提高了 L6 细胞的葡萄糖摄取率(78.34%)。与抑制水平较高的纯 VLG 相比,VLG-CDNPs 对 α 淀粉酶(41.57%)和 α 葡萄糖苷酶(63.48%)也表现出中等程度的抑制活性。
本文章由计算机程序翻译,如有差异,请以英文原文为准。
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.

求助全文
通过发布文献求助,成功后即可免费获取论文全文。 去求助
来源期刊
自引率
0.00%
发文量
44
审稿时长
23 weeks
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.
×
引用
GB/T 7714-2015
复制
MLA
复制
APA
复制
导出至
BibTeX EndNote RefMan NoteFirst NoteExpress
×
提示
您的信息不完整,为了账户安全,请先补充。
现在去补充
×
提示
您因"违规操作"
具体请查看互助需知
我知道了
×
提示
确定
请完成安全验证×
copy
已复制链接
快去分享给好友吧!
我知道了
右上角分享
点击右上角分享
0
联系我们:info@booksci.cn Book学术提供免费学术资源搜索服务,方便国内外学者检索中英文文献。致力于提供最便捷和优质的服务体验。 Copyright © 2023 布克学术 All rights reserved.
京ICP备2023020795号-1
ghs 京公网安备 11010802042870号
Book学术文献互助
Book学术文献互助群
群 号:481959085
Book学术官方微信