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将姜黄素包封于两亲性嵌段共聚物胶束中用于药物传递应用。

Encapsulation of curcumin in Pluronic block copolymer micelles for drug delivery applications.

机构信息

Department of Biotechnology, Biomaterials and Tissue Engineering Laboratory, Indian Institute of Technology Guwahati, Guwahati-781039, Assam, India.

出版信息

J Biomater Appl. 2011 Feb;25(6):619-39. doi: 10.1177/0885328209357110. Epub 2010 Mar 5.

DOI:10.1177/0885328209357110
PMID:20207782
Abstract

We report here the potential of Pluronic tri-block copolymer micelles for the formulation of curcumin, a natural dietary compound having great therapeutic potential against many diseases including cancer. Two most commonly used Pluronic F127 and F68 were used for the formulation and analyzed for curcumin encapsulation efficiency and stability. The encapsulation of drug in micelle was highly dependent on drug-to-copolymer ratio. Pluronic F127 showed better encapsulation efficiency than Pluronic F68. In vitro release profile demonstrated slower and sustained release of curcumin from Pluronic micelles. The lyophilized form of the formulations exhibited good stability for long-term storage. The physical interaction of curcumin with Pluronic was evident by XRD analysis, UV-visible, fluorescence, and FT-IR spectroscopy. AFM study showed that the drug-encapsulated micelles were spherical in shape with diameters below 100 nm. The in vitro cytotoxicity of the drug formulations was investigated with HeLa cancer cells. Pluronic-encapsulated curcumin showed comparable anticancer activity with free curcumin.

摘要

我们在此报告了普朗尼克三嵌段共聚物胶束在姜黄素配方中的潜力,姜黄素是一种天然的膳食化合物,对许多疾病(包括癌症)具有巨大的治疗潜力。我们使用了两种最常用的普朗尼克 F127 和 F68 来进行配方,并分析了其对姜黄素的包封效率和稳定性。药物在胶束中的包封高度依赖于药物与共聚物的比例。普朗尼克 F127 显示出比普朗尼克 F68 更好的包封效率。体外释放曲线表明,姜黄素从普朗尼克胶束中的释放速度更慢,更持久。制剂的冻干形式在长期储存中表现出良好的稳定性。通过 X 射线衍射分析、紫外可见分光光度法、荧光分光光度法和傅里叶变换红外光谱法可以明显看出姜黄素与普朗尼克的物理相互作用。原子力显微镜研究表明,载药胶束呈球形,直径小于 100nm。我们用宫颈癌 HeLa 细胞研究了药物制剂的体外细胞毒性。普朗尼克包封的姜黄素显示出与游离姜黄素相当的抗癌活性。

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