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姜黄素作为抗炎药物的透皮给药系统的设计与评价

Design and evaluation of transdermal drug delivery system for curcumin as an anti-inflammatory drug.

作者信息

Patel Nikunjana A, Patel Natvar J, Patel Rakesh P

机构信息

S. K. Patel College of Pharmaceutical Education and Research, Ganpat University, Gujarat, India.

出版信息

Drug Dev Ind Pharm. 2009 Feb;35(2):234-42. doi: 10.1080/03639040802266782.

Abstract

The purpose of this research was to develop a matrix-type transdermal therapeutic system containing herbal drug, curcumin (CUR), with different ratios of hydrophilic (hydroxyl propyl methyl cellulose K4M [HPMC K4M]) and hydrophobic (ethyl cellulose [EC]) polymeric systems by the solvent evaporation technique. Different concentrations of oleic acid (OA) were used to enhance the transdermal permeation of CUR. The physicochemical compatibility of the drug and the polymers was also studied by differential scanning calorimetry (DSC) and infrared (IR) spectroscopy. The results suggested no physicochemical incompatibility between the drug and the polymers. Formulated transdermal films were physically evaluated with regard to drug content, tensile strength, folding endurance, thickness, and weight variation. All prepared formulations indicated good physical stability. In vitro permeation studies of formulations were performed by using Franz diffusion cells. The results followed Higuchi kinetics, and the mechanism of release was diffusion-mediated. Formulation prepared with hydrophilic polymer containing permeation enhancer showed best in vitro skin permeation through rat skin as compared with all other formulations. This formulation demonstrated good anti-inflammatory activity against carrageenan-induced oedema in Wistar albino rats similar to standard formulation.

摘要

本研究的目的是通过溶剂蒸发技术开发一种含有草药药物姜黄素(CUR)的基质型透皮治疗系统,该系统由不同比例的亲水性(羟丙基甲基纤维素K4M [HPMC K4M])和疏水性(乙基纤维素[EC])聚合物体系组成。使用不同浓度的油酸(OA)来增强CUR的透皮渗透。还通过差示扫描量热法(DSC)和红外(IR)光谱研究了药物与聚合物的物理化学相容性。结果表明药物与聚合物之间不存在物理化学不相容性。对制备的透皮膜进行了药物含量、拉伸强度、耐折性、厚度和重量变化方面的物理评价。所有制备的制剂均显示出良好的物理稳定性。使用Franz扩散池对制剂进行体外渗透研究。结果符合Higuchi动力学,释放机制为扩散介导。与所有其他制剂相比,含有渗透促进剂的亲水性聚合物制备的制剂在体外通过大鼠皮肤的透皮性能最佳。该制剂对Wistar白化大鼠角叉菜胶诱导的水肿表现出良好的抗炎活性,与标准制剂相似。

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