Taxol-loaded block copolymer nanospheres composed of methoxy poly(ethylene glycol) and poly(ε-caprolactone) as novel anticancer drug carriers

We prepared the methoxy poly(ethylene glycol) (MePEG)/poly(epsilon -caprolactone) (PCL) amphiphilic block copolymeric nanospheres containing taxol which has promising anticancer activity. MePEG/PCL block copolymeric nanospheres (MEP50) showed a narrow size distribution and an average diameter of less than 100 nm. When the initial weight ratio of taxol to polymer was 0.5: 1.0, we could obtain the nanospheres having a relatively high drug-loading of more than about 20%. The size of the MePEG/PCL nanospheres also increased according to the taxol loading. However, the nanospheres did not exhibit a significant change in the size distribution and also showed a size of less than 100 nm for even that with drug-loading content (DLC) of about 20%. From the H-1 NMR analysis, we identified that the MePEG/PCL nanospheres prepared by dialysis procedure have core-shell structure consisting of the hydrophilic outer shell of MePEG and the hydrophobic inner core of PCL. We confirmed the low toxicity of MePEG/PCL nanospheres (MEP70) in the acute toxicity study using male ICR mice. In addition, considering the extremely lipophilic characteristics of taxol, this MePEG/PCL, nanosphere system with high taxol loading content and suspended properties in water could be useful for the delivery of taxol. (C) 2001 Elsevier Science Ltd. All rights reserved.