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用于高血压管理的西洛他唑纳米胶束透皮贴剂的研发与优化

Development and Optimization of a Cilostazol-Loaded Nanomicelle Transdermal Patch for Hypertension Management.

作者信息

Thakkar Vaishali, Patel Prima, Parekh Khyati, Rana Hardik, Prajapati Bhupendra

机构信息

Department of Pharmaceutics, Anand Pharmacy College, Gujarat Technological University, Ahmedabad, Gujarat.

Department of Pharmaceutics and Pharmaceutical Technology, Shree S.K. Patel College of Pharmaceutical Education & Research, Ganpat University, Kherva, Gujarat.

出版信息

Pharm Nanotechnol. 2025 Jul 16. doi: 10.2174/0122117385362916250630053000.

DOI:10.2174/0122117385362916250630053000
PMID:40676784
Abstract

BACKGROUND

This study aimed to develop and optimize a cilostazol-loaded nanomicelle transdermal patch to enhance solubility, stability, and controlled drug release.

OBJECTIVE

To improve cilostazol bioavailability by formulating a stable, nanomicelle-loaded transdermal patch.

METHODS

Nanomicelles were prepared using the thin-film hydration method with Soluplus and Poloxamer 188 as the polymer and surfactant. The transdermal patch was fabricated using the solvent casting method and evaluated for tensile strength, folding endurance, and in vitro drug diffusion.

RESULTS

The optimized formulation showed 97.71% entrapment efficiency, 48.86% drug loading, a particle size of 129.07 nm, and a zeta potential of -21.5 mV. The patch exhibited a tensile strength of 141.83 MPa, folding endurance of over 300 folds, and sustained in vitro drug diffusion.

CONCLUSION

The developed transdermal patch offers a promising strategy to enhance cilostazol bioavailability by bypassing first-pass metabolism, promoting better penetration, and ensuring improved patient compliance.

摘要

背景

本研究旨在开发并优化载有西洛他唑的纳米胶束透皮贴剂,以提高其溶解度、稳定性及药物控释性能。

目的

通过制备稳定的载纳米胶束透皮贴剂提高西洛他唑的生物利用度。

方法

采用薄膜水化法,以固体分散体聚合物(Soluplus)和泊洛沙姆188为聚合物和表面活性剂制备纳米胶束。采用溶剂浇铸法制备透皮贴剂,并对其拉伸强度、耐折性及体外药物扩散进行评价。

结果

优化后的制剂包封率为97.71%,载药量为48.86%,粒径为129.07 nm,ζ电位为 -21.5 mV。该贴剂的拉伸强度为141.83 MPa,耐折性超过300次,并具有持续的体外药物扩散性能。

结论

所开发的透皮贴剂通过绕过首过代谢、促进更好的渗透并确保提高患者顺应性,为提高西洛他唑生物利用度提供了一种有前景的策略。

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