Taxol-loaded block copolymer nanospheres composed of methoxy poly(ethylene glycol) and poly(epsilon-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 1H 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.
Kim
S Y
SY
Department of Industrial Chemistry, College of Engineering, Hanyang University, Seoul, South Korea.
Lee
Y M
YM
D000818:Animals; D000972:Antineoplastic Agents, Phytogenic / Q000008:administration & dosage*; D004337:Drug Carriers; D007928:Lethal Dose 50; D008297:Male; D051379:Mice; D008813:Mice, Inbred ICR; D008855:Microscopy, Electron, Scanning; D008863:Microspheres; D017239:Paclitaxel / Q000008:administration & dosage*; D010316:Particle Size; D011091:Polyesters / Q000737:chemistry / Q000633:toxicity; D011092:Polyethylene Glycols / Q000737:chemistry / Q000633:toxicity; D011108:Polymers
D000972:Antineoplastic Agents, Phytogenic; D004337:Drug Carriers; D011091:Polyesters; D011108:Polymers; C016240:polycaprolactone; D011092:Polyethylene Glycols; C028210:monomethoxypolyethylene glycol; D017239:Paclitaxel