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含吡喹酮的聚乳酸-羟基乙酸共聚物纳米颗粒:制剂变量对粒径分布的影响

PLGA nanoparticles containing praziquantel: effect of formulation variables on size distribution.

作者信息

Mainardes Rubiana M, Evangelista Raul C

机构信息

Programa de Pós-Graduação em Ciências Farmacêuticas, UNESP, Rod. Araraquara-Jaú km 1, CEP 14802-902, Araraquara, SP, Brazil.

出版信息

Int J Pharm. 2005 Feb 16;290(1-2):137-44. doi: 10.1016/j.ijpharm.2004.11.027. Epub 2005 Jan 13.

DOI:10.1016/j.ijpharm.2004.11.027
PMID:15664139
Abstract

Praziquantel has been shown to be highly effective against all known species of Schistosoma infecting humans. Spherical nanoparticulate drug carriers made of poly(D,L-lactide-co-glycolide) acid with controlled size were designed. Praziquantel, a hydrophobic molecule, was entrapped into the nanoparticles with theoretical loading varying from 10 to 30% (w/w). This study investigates the effects of some process variables on the size distribution of nanoparticles prepared by emulsion-solvent evaporation method. The results show that sonication time, PLGA and drug amounts, PVA concentration, ratio between aqueous and organic phases, and the method of solvent evaporation have a significant influence on size distribution of the nanoparticles.

摘要

吡喹酮已被证明对所有已知感染人类的血吸虫物种都非常有效。设计了由聚(D,L-丙交酯-共-乙交酯)酸制成的具有可控尺寸的球形纳米颗粒药物载体。吡喹酮是一种疏水分子,被包裹在纳米颗粒中,理论载药量在10%至30%(w/w)之间变化。本研究考察了一些工艺变量对通过乳液-溶剂蒸发法制备的纳米颗粒尺寸分布的影响。结果表明,超声处理时间、聚乳酸-羟基乙酸共聚物(PLGA)和药物用量、聚乙烯醇(PVA)浓度、水相和有机相的比例以及溶剂蒸发方法对纳米颗粒的尺寸分布有显著影响。

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