Intestinal uptake and biodistribution of novel polymeric micelles after oral administration

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.