一种用于延长药物释放的载环孢素A固体脂质纳米粒的新型制剂。

A novel preparation of solid lipid nanoparticles with cyclosporin A for prolonged drug release.

作者信息

Hu F Q, Wu M Zh, Yuan H, Zhang H H

机构信息

School of Pharmaceutical Science, Zhejiang University, Hangzhou, PR China.

出版信息

Pharmazie. 2004 Sep;59(9):683-5.

DOI:
Abstract

Solid lipid nanoparticles were prepared by a novel solvent diffusion method in an aqueous system. The lipophilic model drug cyclosporin A was incorporated into SLN to study encapsulation efficiency, zeta potential (charge) and drug delivery. Stearylamine and cyclosporin A were dissolved in ethanol and acetone and the resultant organic solution was dropped into water at 60 degrees C. The drug-loaded SLN suspension quickly formed with an azury color. After burst drug release with 18% of the drug over the first 12 hours, a distinctly prolonged release over a monitored period of 16 days was observed, with nearly 4% of the drug being released each day. These results demonstrate the suitability of SLN produced with the proposed method as a prolonged release formulation for lipophilic drugs.

摘要

采用一种新型的水相溶剂扩散法制备了固体脂质纳米粒。将亲脂性模型药物环孢素A包封于固体脂质纳米粒中,以研究其包封率、ζ电位(电荷)及药物递送情况。将硬脂胺和环孢素A溶解于乙醇和丙酮中,所得有机溶液于60℃滴入水相中。载药固体脂质纳米粒混悬液迅速形成,呈天蓝色。在最初12小时内有18%的药物发生突释后,在16天的监测期内观察到明显的缓释现象,每天约有4%的药物释放。这些结果表明,用所提出的方法制备的固体脂质纳米粒作为亲脂性药物的缓释制剂是合适的。

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