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姜黄素通过微乳剂的透皮给药。

Transdermal delivery of curcumin via microemulsion.

作者信息

Sintov Amnon C

机构信息

Department of Biomedical Engineering, Faculty of Engineering Sciences, Ben Gurion University of the Negev, Be'er Sheva 84105, Israel.

出版信息

Int J Pharm. 2015 Mar 15;481(1-2):97-103. doi: 10.1016/j.ijpharm.2015.02.005. Epub 2015 Feb 2.

DOI:10.1016/j.ijpharm.2015.02.005
PMID:25655717
Abstract

The objective of this study was to evaluate the transdermal delivery potential of a new curcumin-containing microemulsion system. Three series of experiments were carried out to comprehend the system characteristics: (a) examining the influence of water content on curcumin permeation, (b) studying the effect of curcumin loading on its permeability, and (c) assessing the contribution of the vesicular nature of the microemulsion on permeability. The skin permeability of curcumin from microemulsions, which contained 5%, 10%, and 20% of water content (1% curcumin), was measured in vitro using excised rat skin. It has been shown that the permeability coefficient of CUR in a formulation containing 10% aqueous phase (ME-10) was twofold higher than the values obtained for formulations with 5% and 20% water (Papp=0.116 × 10(-3)± 0.052 × 10(-3)vs. 0.043 × 10(-3)± 0.022 × 10(-3) and 0.047 × 10(-3)± 0.025 × 10(-3)cm/h, respectively. A reasonable explanation for this phenomenon may be the reduction of both droplet size and droplets' concentration in the microemulsion as the aqueous phase decreased from 20% to 5%. It has also been shown that a linear correlation exists between the decrease in droplet size and the increase of curcumin loading in the microemulsion. In addition, it has been demonstrated that a micellar system, S/O-mix, and a plain solution of curcumin resulted in a significantly lower curcumin permeation relative to that presented by the microemulsion, Papp=0.018 × 10(-3)± 0.011 × 10(-3), 0.005 × 10(-3)± 0.002 × 10(-3), and 0.002 × 10(-3)± 0.000 × 10(-3)cm/h, respectively, vs. 0.110 × 10(-3)± 0.021 × 10(-3)cm/h for the microemulsion. The enhancement ratio (ER=Jss-ME/Jss-solution) of CUR permeated via 1% loaded microemulsion was 55.

摘要

本研究的目的是评估一种新型含姜黄素微乳体系的透皮给药潜力。进行了三组实验以了解该体系的特性:(a) 研究含水量对姜黄素渗透的影响;(b) 考察姜黄素载药量对其渗透性的作用;(c) 评估微乳的囊泡性质对渗透性的贡献。使用离体大鼠皮肤体外测定了含水量分别为5%、10%和20%(含1%姜黄素)的微乳中姜黄素的皮肤渗透性。结果表明,含10%水相的制剂(ME-10)中姜黄素的渗透系数比含5%和20%水的制剂高出两倍(Papp分别为0.116×10(-3)±0.052×10(-3)、0.043×10(-3)±0.022×10(-3)和0.047×10(-3)±0.025×10(-3)cm/h)。对此现象的一个合理解释可能是随着水相从20%降至5%,微乳中的液滴尺寸和液滴浓度均降低。还表明微乳中液滴尺寸的减小与姜黄素载药量的增加之间存在线性关系。此外,已证明与微乳相比,胶束体系S/O-mix和姜黄素的普通溶液导致姜黄素的渗透性显著降低,Papp分别为0.018×10(-3)±0.011×10(-3)、0.005×10(-3)±0.002×10(-3)和0.002×10(-3)±0.000×10(-3)cm/h,而微乳为0.110×10(-3)±0.021×10(-3)cm/h。通过1%载药量微乳渗透的姜黄素的增强比(ER=Jss-ME/Jss-solution)为55。

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