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
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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.

用于西尼地平的创新型纳米结构脂质支架:提高高血压治疗潜力的设计与优化
高血压是心脏病、中风和慢性肾病患者死亡的首要原因。西尼地平(Cilnidipine, CLN)是第四代二氢吡啶类钙通道阻滞剂,在治疗心血管疾病方面显示出良好的效果,但其生物利用度(6-30%)对其疗效有负面影响。采用高压均质法合成西尼地平包封的纳米脂质载体,采用33 Box-Behnken设计优化。物理化学表征评估了捕获效率(%EE)、颗粒大小、zeta势、热行为、结晶度和化学相互作用。优化后的配方平均粒径为190.21±21.63 nm, PDI为0.27±0.12,Zeta为-29.25±0.31 mV,包封效率为79.35%±3.13%。DSC和XRD分析证实,在纳米结构脂质载体(nlc)内,药物的晶体形式转变为无定形形式,可能提高其溶解度和生物利用度。傅里叶变换红外光谱(FTIR)证实了西尼地平与制剂辅料的相容性。体外释放的研究表明,最初的释放激增,随后逐渐缓慢地从NLCs中释放药物,表现出双重释放模式。本研究旨在开发、优化和评估CLN - nlcs,以提高CLN的口服生物利用度,从而提高其治疗效果和患者依从性。
本文章由计算机程序翻译,如有差异,请以英文原文为准。
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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.
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