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疏水药物在 Pluronic F127 胶束中的包封:药物疏水性、溶液温度和 pH 值的影响。

Encapsulation of hydrophobic drugs in Pluronic F127 micelles: effects of drug hydrophobicity, solution temperature, and pH.

机构信息

Raman Research Institute, Bangalore, India.

出版信息

Langmuir. 2013 Apr 2;29(13):4350-6. doi: 10.1021/la304836e. Epub 2013 Mar 19.

DOI:10.1021/la304836e
PMID:23472840
Abstract

Three drugs, ibuprofen, aspirin, and erythromycin, are encapsulated in spherical Pluronic F127 micelles. The shapes and the size distributions of the micelles in dilute, aqueous solutions, with and without drugs, are ascertained using cryo-scanning electron microscopy and dynamic light scattering (DLS) experiments, respectively. Uptake of drugs above a threshold concentration is seen to reduce the critical micellization temperature of the solution. The mean hydrodynamic radii and polydispersities of the micelles are found to increase with decrease in temperature and in the presence of drug molecules. The hydration of the micellar core at lower temperatures is verified using fluorescence measurements. Increasing solution pH leads to the ionization of the drugs incorporated in the micellar cores. This causes rupture of the micelles and release of the drugs into the solution at the highest solution pH value of 11.36 investigated here and is studied using DLS and fluorescence spectrocopy.

摘要

三种药物(布洛芬、阿司匹林和红霉素)被包裹在球形的 Pluronic F127 胶束中。使用 cryo-scanning 电子显微镜和动态光散射(DLS)实验分别确定了药物存在和不存在时,胶束在稀水溶液中的形状和粒径分布。发现超过阈值浓度的药物摄取会降低溶液的临界胶束化温度。发现胶束的平均水动力半径和多分散性随温度降低和药物分子的存在而增加。使用荧光测量验证了较低温度下胶束核的水合作用。增加溶液 pH 值会导致掺入胶束核的药物发生离解。这会导致胶束破裂,并将药物释放到溶液中,在本文研究的最高溶液 pH 值 11.36 下会发生这种情况,并使用 DLS 和荧光光谱法进行研究。

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