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维甲酸固体脂质纳米粒:局部给药的潜力。

Solid lipid nanoparticles (SLN) of tretinoin: potential in topical delivery.

作者信息

Shah Kumar A, Date Abhijit A, Joshi Medha D, Patravale Vandana B

机构信息

Department of Pharmaceutical Sciences and Technology, University Institute of Chemical Technology, Matunga, Mumbai 400019, India.

出版信息

Int J Pharm. 2007 Dec 10;345(1-2):163-71. doi: 10.1016/j.ijpharm.2007.05.061. Epub 2007 Jun 2.

Abstract

The objective of this investigation was to develop solid lipid nanoparticles (SLN) of tretinoin (TRE) with the help of facile and simple emulsification-solvent diffusion (ESD) technique and to evaluate the viability of an SLN based gel in improving topical delivery of TRE. The feasibility of fabricating SLN of TRE by the ESD method was successfully demonstrated in this investigation. The developed SLN were characterized for particle size, polydispersity index, entrapment efficiency of TRE and morphology. Studies were carried out to evaluate the ability of SLN in improving the photostability of TRE as compared to TRE in methanol. Encapsulation of TRE in SLN resulted in a significant improvement in its photostability in comparison to methanolic TRE solution and also prevented its isomerization. Furthermore, the skin irritation studies carried out on rabbits showed that SLN based TRE gel is significantly less irritating to skin as compared to marketed TRE cream and clearly indicated its potential in improving the skin tolerability of TRE. In vitro permeation studies through rat skin indicated that an SLN based TRE gel has permeation profile comparable to that of the marketed TRE cream.

摘要

本研究的目的是借助简便的乳化-溶剂扩散(ESD)技术制备维甲酸(TRE)固体脂质纳米粒(SLN),并评估基于SLN的凝胶在改善TRE局部给药方面的可行性。本研究成功证明了通过ESD法制备TRE-SLN的可行性。对所制备的SLN进行了粒径、多分散指数、TRE包封率和形态表征。开展研究以评估SLN与甲醇中的TRE相比在提高TRE光稳定性方面的能力。与甲醇中的TRE溶液相比,TRE包封于SLN中使其光稳定性显著提高,并且还防止了其异构化。此外,在兔子身上进行的皮肤刺激性研究表明,与市售TRE乳膏相比,基于SLN的TRE凝胶对皮肤的刺激性明显更小,这清楚地表明了其在改善TRE皮肤耐受性方面的潜力。通过大鼠皮肤进行的体外渗透研究表明,基于SLN的TRE凝胶的渗透情况与市售TRE乳膏相当。

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