Paclitaxel-loaded PLGA nanoparticles: preparation, physicochemical characterization and in vitro anti-tumoral activity
Paclitaxel-loaded PLGA nanoparticles: preparation, physicochemical characterization and in vitro anti-tumoral activity
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DOI：
10.1016/s0168-3659(02)00212-2
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发表时间：
2002-10-04
影响因子：
10.8
通讯作者：
Gaspar, R
中科院分区：
文献类型：
--
作者：
Fonseca, C;Simoes, S;Gaspar, R
本研究的主要目的是开发一种用于紫杉醇的聚合物给药系统，该系统拟静脉给药，能够提高药物的治疗指数且无聚氧乙烯蓖麻油（Cremophor® EL）的不良反应。为实现这一目标，采用界面沉积法制备了载紫杉醇（Ptx）的聚乳酸 - 羟基乙酸共聚物（PLGA）纳米粒子（Ptx - PLGA - Nps）。评估了不同实验参数对紫杉醇在纳米粒子中包封率的影响。我们的结果表明，紫杉醇在纳米粒子中的包封率主要受有机相的制备方法以及有机相/水相比例的影响。我们的数据显示，所采用的制备方法能够形成球形纳米级（
The main objective of this study was to develop a polymeric drug delivery system for paclitaxel, intended to be intravenously administered, capable of improving the therapeutic index of the drug and devoid of the adverse effects of Cremophor(R) EL. To achieve this goal paclitaxel (Ptx)-loaded poly(lactic-co-glycolic acid) (PLGA) nanoparticles (Ptx-PLGA-Nps) were prepared by the interfacial deposition method. The influence of different experimental parameters on the incorporation efficiency of paclitaxel in the nanoparticles was evaluated. Our results demonstrate that the incorporation efficiency of paclitaxel in nanoparticles was mostly affected by the method of preparation of the organic phase and also by the organic phase/aqueous phase ratio. Our data indicate that the methodology of preparation allowed the formation of spherical nanometric (