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

Biomaterials. 2001 Jul;22(13):1697-704. doi: 10.1016/s0142-9612(00)00292-1.

Abstract

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.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Animals
  • Antineoplastic Agents, Phytogenic / administration & dosage*
  • Drug Carriers
  • Lethal Dose 50
  • Male
  • Mice
  • Mice, Inbred ICR
  • Microscopy, Electron, Scanning
  • Microspheres
  • Paclitaxel / administration & dosage*
  • Particle Size
  • Polyesters* / chemistry
  • Polyesters* / toxicity
  • Polyethylene Glycols* / chemistry
  • Polyethylene Glycols* / toxicity
  • Polymers*

Substances

  • Antineoplastic Agents, Phytogenic
  • Drug Carriers
  • Polyesters
  • Polymers
  • polycaprolactone
  • Polyethylene Glycols
  • monomethoxypolyethylene glycol
  • Paclitaxel