Methoxy poly(ethylene glycol)-poly(lactide) (MPEG-PLA) nanoparticles for controlled delivery of anticancer drugs
Methoxy poly(ethylene glycol)-poly(lactide) (MPEG-PLA) nanoparticles for controlled delivery of anticancer drugs
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DOI：
10.1016/j.biomaterials.2003.09.055
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发表时间：
2004-06-01
期刊：
影响因子：
14
通讯作者：
Feng, SS
中科院分区：
文献类型：
--
作者：
Dong, YC;Feng, SS
合成了甲氧基聚乙二醇-聚乳酸共聚物（MPEG-PLA），并采用纳米沉淀法制备了纳米粒，用于临床给药。由于其出色的疗效和商业上的巨大成功，紫杉醇被用作原型药物。通过激光光散射、原子力显微镜、zeta电位分析仪和X射线光电子能谱（XPS）对紫杉醇纳米粒的粒径和粒径分布、表面形貌、表面电荷和表面化学进行了研究。采用高效液相色谱法测定包封率和体外释放度。评价了各种制剂参数的影响。发现所制备的纳米颗粒为球形，尺寸小于100 nm。Zeta电位测量和XPS分析证明了PEG层在颗粒表面上的存在。有机相的粘度被认为是粒度测定的主要工艺因素之一。发现EE受载药量的影响很大。药物释放模式是双相的快速释放速率，然后是缓慢的。该微粒悬浮液在体外表现出良好的空间稳定性。可以预期紫杉醇的这种纳米颗粒制剂在循环中具有长循环作用。(C)2003 Elsevier Ltd.保留所有权利。
Methoxy poly(ethylene glycol)-poly(lactide) copolymer (MPEG-PLA) was synthesized and used to make nanoparticles by the nanoprecipitation method for clinical administration of antineoplastic drugs. Paclitaxel was used as a prototype drug due to its excellent efficacy and commercially great success. The size and size distribution, surface morphology, surface charge and surface chemistry of the paclitaxel-loaded nanoparticles were then investigated by laser light scattering, atomic force microscopy, zeta-potential analyzer and X-ray photoelectron spectroscopy (XPS). The drug encapsulation efficiency (EE) and in vitro release profile were measured by high-performance liquid chromatography. The effects of various formulation parameters were evaluated. The prepared nanoparticles were found of spherical shape with size less than 100 nm. Zeta potential measurement and XPS analysis demonstrated the presence of PEG layer on the particle surface. Viscosity of the organic phase was found to be one of the main process factors for the size determination. The EE was found to be greatly influenced by the drug loading. The drug release pattern was biphasic with a fast release rate followed by a slow one. The particle suspension exhibited good steric stability in vitro. Such a nanoparticle formulation of paclitaxel can be expected to have long-circulating effects in circulation. (C) 2003 Elsevier Ltd. All rights reserved.