Intestinal uptake and biodistribution of novel polymeric micelles after oral administration

被引：86
|
作者：
Mathot, F
van Beijsterveldt, L
Préat, V
Brewster, M
Ariën, A
机构：
[1] Catholic Univ Louvain, Dept Pharmaceut Technol, B-1200 Brussels, Belgium
[2] Johnson & Johnson Pharmaceut Res & Dev, Div Janssen Pharmaceut, B-2340 Beerse, Belgium
来源：
JOURNAL OF CONTROLLED RELEASE | 2006年 / 111卷 / 1-2期
关键词：
self-assembling polymeric micelles; Caco-2; risperidone; oral delivery; biodistribution; mmePEG(750)P(CL-co-TMC);
D O I：
10.1016/j.jconrel.2005.11.012
中图分类号：
O6 [化学];
学科分类号：
0703 ;
摘要：
To determine the fate of polymeric micelles after oral administration, we investigated the possible transport of polymeric micelles across Caco-2 monolayers and their biodistribution in rats after per os administration of [C-14]-labelled mmePEG(750)P(CL-co-TMC) micelles containing risperidone (BCS Class II drug). mmePEG(750)P(CL-co-TMC) was able to cross Caco-2 monolayer via a saturable transport mechanism. The oral bioavailability of the polymer was 40%. Polymeric micelles based on mmePEG(750)P(CL-co-TMC) showed very low clearance by the reticuloendothelial system (RES) and a renal excretion. A sustained release of risperidone was observed. (c) 2005 Elsevier B.V. All rights reserved.
引用
收藏
页码：47 / 55
页数：9
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