Effect of copolymer composition on the physicochemical characteristics, in vitro stability, and biodistribution of PLGA-mPEG nanoparticles
Effect of copolymer composition on the physicochemical characteristics, in vitro stability, and biodistribution of PLGA-mPEG nanoparticles
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DOI：
10.1016/s0378-5173(03)00224-2
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发表时间：
2003-06-18
影响因子：
5.8
通讯作者：
Ithakissios, DS
中科院分区：
文献类型：
--
作者：
Avgoustakis, K;Beletsi, A;Ithakissios, DS
研究了不同聚乳酸 - 羟基乙酸共聚物 - 甲氧基聚乙二醇（PLGA - mPEG）纳米颗粒组成的理化性质、体外胶体稳定性以及在小鼠体内的生物分布特性。纳米颗粒通过沉淀 - 溶剂蒸发技术制备。用于制备纳米颗粒的PLGA - mPEG共聚物的组成显著影响PLGA - mPEG纳米颗粒的物理特性和胶体稳定性。由具有相对较高mPEG/PLGA比率的共聚物制备的PLGA - mPEG纳米颗粒比由具有相对较低mPEG/PLGA比率的共聚物制备的更小且稳定性更差。与传统的PLGA纳米颗粒相比，所有PLGA - mPEG纳米颗粒组成在血液中的停留时间都更长。PLGA - mPEG共聚物的组成显著影响PLGA - mPEG纳米颗粒在肝脏、脾脏和骨骼中的血液停留时间和生物分布。不同PLGA - mPEG纳米颗粒组成的体内行为似乎与其体外稳定性无关。似乎存在最佳的mPEG/PLGA比率，使得PLGA - mPEG纳米颗粒具有较长的血液循环时间。这可能与mPEG/PLGA比率对纳米颗粒表面PEG的密度以及纳米颗粒大小的影响有关。（C）2003爱思唯尔科学出版社。版权所有。
The physicochemical properties, the colloidal stability in vitro and the biodistribution properties in mice of different PLGA-mPEG nanoparticle compositions were investigated. The nanoparticles were prepared by a precipitation-solvent evaporation technique. The physical characteristics and the colloidal stability of the PLGA-mPEG nanoparticles were significantly influenced by the composition of the PLGA-mPEG copolymer used to prepare the nanoparticles. PLGA-mPEG nanoparticles prepared from copolymers having relatively high mPEG/PLGA ratios were smaller and less stable than those prepared from copolymers having relatively low mPEG/PLGA ratios. All PLGA-mPEG nanoparticle compositions exhibited prolonged residence in blood, compared to the conventional PLGA nanoparticles. The composition of the PLGA-mPEG copolymer affected significantly the blood residence time and the biodistribution of the PLGA-mPEG nanoparticles in liver, spleen and bones. The in vivo behavior of the different PLGA-mPEG nanoparticle compositions did not appear to correlate with their in vitro stability. Optimum mPEG/PLGA ratios appeared to exist leading to long blood circulation times of the PLGA-mPEG nanoparticles. This may be associated with the effects of the mPEG/PLGA ratio on the density of PEG on the surface of the nanoparticles and on the size of the nanoparticles. (C) 2003 Elsevier Science B.V. All rights reserved.