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载奈韦拉平的泊洛沙姆407/普朗尼克P123混合胶束:制剂优化及体外评价

Nevirapine loaded Poloxamer 407/Pluronic P123 mixed micelles: Optimization of formulation and in vitro evaluation.

作者信息

Jindal Neha, Mehta S K

机构信息

Department of Chemistry and Center of Advanced Studies in Chemistry, Panjab University, Chandigarh 160014, India.

Department of Chemistry and Center of Advanced Studies in Chemistry, Panjab University, Chandigarh 160014, India.

出版信息

Colloids Surf B Biointerfaces. 2015 May 1;129:100-6. doi: 10.1016/j.colsurfb.2015.03.030. Epub 2015 Mar 18.

DOI:10.1016/j.colsurfb.2015.03.030
PMID:25839908
Abstract

An attempt has been made to develop polymeric mixed micelle delivery system using Poloxamer 407 and Pluronic P123 for the encapsulation of an antiretroviral drug, Nevirapine. The stability of formulated mixed micellar system at different ratios (1:2, 1:1 and 2:1) and standard thermodynamic parameters of micellization have been determined from the temperature dependence of the critical micelle concentration. The process of micellization of Poloxamer 407/Pluronic P 123 system has been found to be entropy dominant at low temperatures and enthalpy driven at high temperatures. The amity of the different components of mixed micelles has been explored using Fourier transform infrared spectroscopy, Differential scanning calorimeter and X-ray diffraction studies, which rule out the possibility of any interactions between the drug and excipients. Micropolarity measurements infer that the drug is solubilized in the inner core of mixed micelles. In addition, dialysis method has been employed to determine the entrapment efficiency of all the three formulations. The formulation at 1:1 ratio exhibits high entrapment efficiency along with sustained release of the drug.

摘要

已尝试开发一种使用泊洛沙姆407和普朗尼克P123的聚合物混合胶束递送系统,用于包裹抗逆转录病毒药物奈韦拉平。通过临界胶束浓度的温度依赖性,确定了不同比例(1:2、1:1和2:1)下配制的混合胶束系统的稳定性以及胶束化的标准热力学参数。已发现泊洛沙姆407/普朗尼克P123系统的胶束化过程在低温下以熵为主导,在高温下由焓驱动。使用傅里叶变换红外光谱、差示扫描量热法和X射线衍射研究探索了混合胶束不同组分之间的亲和性,排除了药物与辅料之间发生任何相互作用的可能性。微极性测量推断药物溶解在混合胶束的内核中。此外,已采用透析法测定所有三种制剂的包封率。1:1比例的制剂表现出高包封率以及药物的持续释放。

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