Innovative Nanostructured Lipid Scaffolds for Cilnidipine: Design and Optimization to Elevate the Therapeutic Potential in Hypertensive Therapy

IF 2.7 4区 化学 Q2 CHEMISTRY, INORGANIC & NUCLEAR
Yogesh Mali, Rarchita Sharma, Yogeeta Agrawal, Kiran Patil
{"title":"Innovative Nanostructured Lipid Scaffolds for Cilnidipine: Design and Optimization to Elevate the Therapeutic Potential in Hypertensive Therapy","authors":"Yogesh Mali,&nbsp;Rarchita Sharma,&nbsp;Yogeeta Agrawal,&nbsp;Kiran Patil","doi":"10.1007/s10876-025-02792-4","DOIUrl":null,"url":null,"abstract":"<div><p>Hypertension is the foremost reason for death among patients with heart disease, stroke, and chronic kidney disease. Cilnidipine (CLN), a fourth–generation dihydropyridine calcium channel blocker, shows promising results for cardiovascular diseases, but its bioavailability (6–30%) negatively impacts its effectiveness. The synthesis of cilnidipine encapsulated Nanostructured Lipid Carriers was achieved through high–pressure homogenization and 3<sup>3</sup> Box–Behnken Design was utilized for optimization. The physicochemical characterization evaluated the entrapment efficiency (%EE), size of the particle, its zeta potential, thermal behavior, crystallinity, and chemical interactions. The optimized formulation presented 190.21 ± 21.63 nm (mean particle size), 0.27 ± 0.12 (PDI), -29.25 ± 0.31 mV (Zeta), and 79.35% ± 3.13% (Entrapment efficiency). Analysis using DSC and XRD confirmed the transition of the drug’s crystalline form to an amorphous form within the nanostructured lipid carriers (NLCs), potentially improving its solubility and bioavailability. Fourier–transform infrared spectroscopy (FTIR) affirmed compatibility between Cilnidipine and formulation excipients. The studies of <i>in–vitro</i> release showed an initial surge in release, followed by a gradual slow drug release from NLCs, exhibiting a dual–release pattern. This study aims to develop, optimize, and evaluate CLN–NLCs to boost the oral bioavailability of CLN, thereby improving its therapeutic effectiveness and patient compliance.</p></div>","PeriodicalId":618,"journal":{"name":"Journal of Cluster Science","volume":"36 3","pages":""},"PeriodicalIF":2.7000,"publicationDate":"2025-04-05","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":"0","resultStr":null,"platform":"Semanticscholar","paperid":null,"PeriodicalName":"Journal of Cluster Science","FirstCategoryId":"92","ListUrlMain":"https://link.springer.com/article/10.1007/s10876-025-02792-4","RegionNum":4,"RegionCategory":"化学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":null,"EPubDate":"","PubModel":"","JCR":"Q2","JCRName":"CHEMISTRY, INORGANIC & NUCLEAR","Score":null,"Total":0}
引用次数: 0

Abstract

Hypertension is the foremost reason for death among patients with heart disease, stroke, and chronic kidney disease. Cilnidipine (CLN), a fourth–generation dihydropyridine calcium channel blocker, shows promising results for cardiovascular diseases, but its bioavailability (6–30%) negatively impacts its effectiveness. The synthesis of cilnidipine encapsulated Nanostructured Lipid Carriers was achieved through high–pressure homogenization and 33 Box–Behnken Design was utilized for optimization. The physicochemical characterization evaluated the entrapment efficiency (%EE), size of the particle, its zeta potential, thermal behavior, crystallinity, and chemical interactions. The optimized formulation presented 190.21 ± 21.63 nm (mean particle size), 0.27 ± 0.12 (PDI), -29.25 ± 0.31 mV (Zeta), and 79.35% ± 3.13% (Entrapment efficiency). Analysis using DSC and XRD confirmed the transition of the drug’s crystalline form to an amorphous form within the nanostructured lipid carriers (NLCs), potentially improving its solubility and bioavailability. Fourier–transform infrared spectroscopy (FTIR) affirmed compatibility between Cilnidipine and formulation excipients. The studies of in–vitro release showed an initial surge in release, followed by a gradual slow drug release from NLCs, exhibiting a dual–release pattern. This study aims to develop, optimize, and evaluate CLN–NLCs to boost the oral bioavailability of CLN, thereby improving its therapeutic effectiveness and patient compliance.

求助全文
约1分钟内获得全文 求助全文
来源期刊
Journal of Cluster Science
Journal of Cluster Science 化学-无机化学与核化学
CiteScore
6.70
自引率
0.00%
发文量
166
审稿时长
3 months
期刊介绍: The journal publishes the following types of papers: (a) original and important research; (b) authoritative comprehensive reviews or short overviews of topics of current interest; (c) brief but urgent communications on new significant research; and (d) commentaries intended to foster the exchange of innovative or provocative ideas, and to encourage dialogue, amongst researchers working in different cluster disciplines.
×
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