Evaluation of long-circulating nanoparticles using biodegradable ABA triblock copolymers containing of poly(L-lactic acid) A-blocks attached to central poly(oxyethylene) B-blocks in vivo
Evaluation of long-circulating nanoparticles using biodegradable ABA triblock copolymers containing of poly(L-lactic acid) A-blocks attached to central poly(oxyethylene) B-blocks in vivo
复制标题
DOI：
10.1016/s0378-5173(98)00280-4
复制
发表时间：
1998-11-26
影响因子：
5.8
通讯作者：
Takahashi, Y
中科院分区：
文献类型：
--
作者：
Nakada, Y;Tudomi, R;Takahashi, Y
纳米颗粒（平均直径152-377 nm），由阿坝三嵌段共聚物组成（分子量29000-147000）含聚乙烯（L-乳酸）（PLA）A-嵌段连接到中心聚（oxidase）（PEG）B-嵌段（PEG M-w 6600，20000）制备了聚乳酸-聚乙二醇-聚乳酸（PLA-PEG-PLA）纳米粒，研究了聚合物性质对纳米粒药动学和体内分布的影响。Progesterone被用作模型药物。我们可以使用三嵌段共聚物来制造长循环纳米颗粒。通过Co值（0时的孕酮浓度）估计的早期突释程度和循环时间受总M-w、PEG含量、PEG M-w和M-w/M-n（M-n：其中M-n为数均分子量）比的影响。聚合物的纯化是控制突发的重要因素。这些三嵌段共聚物纳米颗粒诱导肝脏和脾脏对纳米颗粒的吸收减少。这些现象可能是由于PEG在颗粒表面上的取向而避免了调理素吸附到颗粒上。(C)1998 Elsevier Science B. V.保留所有权利。
The nanoparticles (mean diameter 152-377 nm) ,consisting of the ABA triblock copolymers (M-w 29000-147000) containing poly(L-lactic acid) (PLA) A-blocks attached to central poly(oxyethylene) (PEG) B-blocks (PEG M-w 6600, 20000) (PLA-PEG-PLA) were prepared, and the effects of the polymer characteristics on the pharmacokinetics of the nanoparticles and the biodistribution of the nanoparticles were studied. Progesterone was used as a model drug. We could make the long-circulating nanoparticles using the triblock copolymer. The degree of burst in early phase, which was estimated by the Co values (Progesterone concentration at time 0) and the circulating-time were affected by the total M-w, the PEG content, the PEG M-w and the M-w/M-n (M-n: where M-n is the number average molecular weight) ratio. The purification of the polymer was an important factor for the control of the burst. These triblock copolymer nanoparticles induced reduction in the liver and spleen uptake of the nonoparticles. These phenomena are probably explained by the avoidence of adsorption of opsonin to the particles as a result of the orientation of PEG on the surface of the particles. (C) 1998 Elsevier Science B.V. All rights reserved.