洛匹那韦聚合物胶束的制备、开发与评价

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引用次数: 4

摘要

洛匹那韦是一种抗HIV药物,用于治疗HIV-1感染。在这项研究中,我们使用单洛匹那韦药物来制备聚合物胶束。本研究主要有两个目的:一是为了提高BCS IV类药物的溶解度和生物利用度,二是为了避免洛匹那韦和利托那韦合用,并使用单个洛匹那韦制备聚合物胶束,同时避免口服给药的缺点。方法:选择不同的pluronic (F188 & f127)和助溶剂(Tween80),用不同的药聚合物比制备胶束,并分别加入或不加入助溶剂和药物洛匹那韦。采用临界胶束浓度(CMC)值、胶束大小、DSC、XRD、载药率、载药率、稳定性等指标对配方进行表征。结果:经优化后得到的混合胶束(亲疏水)的包封率最高,为29%,囊泡大小为0.156µm。并对洛匹那韦和优化后的配方进行了DSC、FTIR、XRD研究。结论:与复配溶剂相比,复配溶剂的复配F68包封率和载药量均较高
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Formulation, Development and Evaluation of Lopinavir Loaded Polymeric Micelles
Lopinavir is the anti HIV drug which is used to treat the HIV-1 infection. In this study we used the single lopinavir drug to formulate the polymeric micelle. This study was done with the two main objectives as Objective:first to enhance the solubility and bioavailability of the BCS class IV drug and second to avoid the combination of lopinavir rand ritonavir and use single lopinavir to preparation of polymeric micelle also to avoid the disadvantages related to the oral administration. Method:The different pluronic (F188 &F127) and co-solvent (Tween80) were chosen & the micelles were prepared by using different Drug: polymer ratio with or without cosolvent and drug Lopinavir. Formulations were been characterized by critical micelle concentration(CMC) value, micellesize,DSC, XRD, loading efficiency, % drug loading and stability.Result:Mixed micelle (hydrophobic &hydrophilic) obtained from optimized batch shows the highest entrapment of 29%with the pluronic F68 with the use of co-solvent and the vesicle size of 0.156µm the DSC, FTIR, XRD study was also done for lopinavir and optimized formulation .Conclusion: The pluronic F68 with the co-solvent showed fairly high entrapment efficiency, loading capacity than the mixed Pluronic in combination
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