A simple method to achieve high doxorubicin loading in biodegradable polymersomes

J Control Release. 2010 Nov 1;147(3):428-35. doi: 10.1016/j.jconrel.2010.07.123. Epub 2010 Aug 6.

Abstract

Doxorubicin (Dox), an anthracycline anticancer drug, was successfully incorporated into block copolymer vesicles of poly(trimethylene carbonate)-b-poly(L-glutamic acid) (PTMC-b-PGA) by a solvent-displacement (nanoprecipitation) method. pH conditions were shown to have a strong influence on loading capacity and release profiles. Substantial drug loading (47% w/w) was achieved at pH 10.5. After pH neutralization, aqueous dispersions of drug-loaded vesicles were found stable for a prolonged period of time (at least 6months) without vesicle disruption or drug precipitation. Dox-loaded vesicles exhibited in vitro pH and temperature-dependent drug release profiles: release kinetics fastened in acid conditions or by increasing temperature. These features strongly support the interest of developing PTMC-b-PGA polymersomes as carriers for the controlled delivery of Dox.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Antibiotics, Antineoplastic / chemistry*
  • Chemical Precipitation
  • Chemistry, Pharmaceutical
  • Delayed-Action Preparations
  • Dioxanes / chemistry*
  • Doxorubicin / chemistry*
  • Drug Carriers*
  • Drug Compounding
  • Drug Stability
  • Hydrogen-Ion Concentration
  • Kinetics
  • Models, Chemical
  • Nanotechnology*
  • Polyglutamic Acid / chemistry*
  • Polymers / chemistry*
  • Solubility
  • Technology, Pharmaceutical / methods*
  • Temperature

Substances

  • Antibiotics, Antineoplastic
  • Delayed-Action Preparations
  • Dioxanes
  • Drug Carriers
  • Polymers
  • Polyglutamic Acid
  • polytrimethylene carbonate
  • Doxorubicin