期刊
JOURNAL OF CONTROLLED RELEASE
卷 167, 期 3, 页码 301-314出版社
ELSEVIER SCIENCE BV
DOI: 10.1016/j.jconrel.2013.02.011
关键词
Co-encapsulation; Nanostructured lipid carriers; Two-step factorial design; Permeation enhancement; Molecular dynamics; Transdermal administration
资金
- FCT (Fundacao para a Ciencia e Tecnologia, Portugal) [SFRH/BD/41536/2007]
- Fundação para a Ciência e a Tecnologia [SFRH/BD/41536/2007] Funding Source: FCT
Co-encapsulation of drugs directed at commonly associated diseases provides a convenient means for administration, especially if transdermally delivered. In this work, a comprehensive study for the co-encapsulation of drugs with a differential lipophilicity, olanzapine and simvastatin, and their transdermal delivery in a formulation containing nanostructured lipid carriers (NLC) is presented. Focus is given to the evaluation of a strategy in which NLC and chemical permeation enhancers are combined. It comprises in vitro, in silico and cellular viability approaches. The optimization and rationalization of the systems are carried out using a two-step factorial design. It is shown that the external medium in the NLC dispersion strongly influences permeation. It is also seen that the use of NLC determines a synergistic effect with selected permeation enhancers, thus promoting marked flux enhancement ratios (48 and 21, respectively for olanzapine and simvastatin) relative to the drugs in solution. The developed formulations can be considered non-irritant. A correlation between enhancer positioning in a lipid bilayer, partially governed by a H-bonding phenomenon, and enhancement effect is suggested from molecular dynamics studies and experimental observations. (C) 2013 Elsevier B. V. All rights reserved.
作者
我是这篇论文的作者
点击您的名字以认领此论文并将其添加到您的个人资料中。
推荐
暂无数据