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用于以极低浓度局部给药药物分子的水凝胶增稠微乳剂。

Hydrogel-thickened microemulsion for topical administration of drug molecule at an extremely low concentration.

作者信息

Chen Huabing, Mou Dongsheng, Du Danrong, Chang Xueling, Zhu Dandan, Liu Jie, Xu Huibi, Yang Xiangliang

机构信息

College of Life Science and Technology, Huazhong University of Science and Technology, 430074 Wuhan, China.

出版信息

Int J Pharm. 2007 Aug 16;341(1-2):78-84. doi: 10.1016/j.ijpharm.2007.03.052. Epub 2007 Apr 5.

Abstract

In this work, a hydrogel-thickened microemulsion (HTM) was investigated for delivering an extremely low concentration of drug molecule. The pseudo-ternary phase diagrams were constructed using isopropyl myristate (IPM), Tween 80, propylene glycol and water. The various HTM were prepared and characterized. We described that HTM has the combination of o/w microstructure of microemulsion and the three-dimensional gel network of hydrogel in continuous phase using transmission electron microscope. The stability tests showed that HTM had good stability. The influence of the addition of hydrogel into microemulsions on the viscosity and permeation ability is investigated. The abilities of HTM to deliver an extremely low concentration of triptolide as a model drug were evaluated using the in vitro permeation studies. The permeation rates of triptolide from various HTM were 2.2-3.6 times over that from the control hydrogel. The addition of 2% menthol into HTM consisting of 3% IPM, 30% Tween 80, 15% propylene glycol, 0.75% carbomer 940 resulted in the highest permeation rate of 0.105+/-0.006microcm(-2)h(-1), which was 5.8 times over control gel. The powerful permeation enhancing ability of HTM with a suitable viscosity makes it promising alternative carrier for transdermal administration of drug molecule at an extremely low concentration.

摘要

在本研究中,对一种水凝胶增稠微乳液(HTM)进行了研究,用于递送极低浓度的药物分子。使用肉豆蔻酸异丙酯(IPM)、吐温80、丙二醇和水构建了拟三元相图。制备并表征了各种HTM。我们使用透射电子显微镜描述了HTM在连续相中具有微乳液的水包油微观结构和水凝胶的三维凝胶网络的组合。稳定性测试表明HTM具有良好的稳定性。研究了向微乳液中添加水凝胶对粘度和渗透能力的影响。使用体外渗透研究评估了HTM作为模型药物递送极低浓度雷公藤内酯醇的能力。来自各种HTM的雷公藤内酯醇的渗透速率是对照水凝胶的2.2 - 3.6倍。在由3% IPM、30%吐温80、15%丙二醇、0.75%卡波姆940组成的HTM中添加2%薄荷醇,导致最高渗透速率为0.105±0.006微厘米⁻²小时⁻¹,是对照凝胶的5.8倍。具有合适粘度的HTM强大的渗透增强能力使其成为极低浓度药物分子经皮给药的有前景的替代载体。

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