以甲氧基肉桂酸辛酯为例,探讨使用固体脂质微球作为紫外线过滤剂载体的重要性。

Importance of using solid lipid microspheres as carriers for UV filters on the example octyl methoxy cinnamate.

作者信息

Yener Gülgün, Incegül Tuba, Yener Namýk

机构信息

Department of Pharmaceutical Technology, Cosmetics Section, Faculty of Pharmacy, Istanbul University, 34452, Istanbul, Turkey.

出版信息

Int J Pharm. 2003 Jun 4;258(1-2):203-7. doi: 10.1016/s0378-5173(03)00203-5.

Abstract

The aim of this study was to prepare solid lipid microspheres (SLM) of octyl methoxy cinnamate (2-ethylhexyl-p-methoxy cinnamate; OMC) to achieve controlled release, decrease penetration of this UV absorber from skin and improve its photostability. The influence of the carrier on the rate of release was studied in vitro with a cellulose acetate membrane and in vivo from excised rat skin with Franz diffusion cells. The release rate was decreased by up to 13-80% with the SLM formulation. In vivo, penetration of OMC into skin was investigated by HPLC method. It was found out that the rate of penetration is significantly dependent upon the formulation and could be decreased by up to 77% in SLM formulations. When different topical vehicles were compared, OMC was released and penetrated into rat skin more quickly and in greater amount from vehicles containing free OMC than in SLM form. Additionally, photostability was shown to be improved in SLM form.

摘要

本研究的目的是制备桂皮酸盐(2-乙基己基对甲氧基肉桂酸酯;OMC)的固体脂质微球(SLM),以实现控释,减少这种紫外线吸收剂从皮肤的渗透,并提高其光稳定性。用醋酸纤维素膜在体外研究了载体对释放速率的影响,并在体内用Franz扩散池从切除的大鼠皮肤研究了该影响。SLM制剂使释放速率降低了13%-80%。在体内,通过HPLC法研究了OMC在皮肤中的渗透情况。结果发现,渗透速率显著取决于制剂,在SLM制剂中可降低多达77%。当比较不同的局部给药载体时,与SLM形式相比,含有游离OMC的载体中OMC从大鼠皮肤释放和渗透得更快且量更大。此外,SLM形式的光稳定性得到了提高。

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