Polydiacetylene vesicles as a novel drug sustained-release system

Colloids Surf B Biointerfaces. 2010 Mar 1;76(1):362-5. doi: 10.1016/j.colsurfb.2009.10.009. Epub 2009 Nov 7.

Abstract

Aiming at the enhancement of the physicochemical stability as well as the sustained-release property of conventional liposomes, a novel polymerized vesicular carrier, 10,12-pentacosadiynoic acid (PCDA) vesicles, loaded with paclitaxel as a model hydrophobic drug has been successfully constituted by incorporation of a polymerizable diacetylene into the lipid bilayer vesicles. The polymerized vesicles have been characterized in terms of particle size distribution and zeta-potential. Altering their lipid composition causes the zeta-potential to change from -3+/-1mV to more than -25mV, with a concomitant change in particle size distribution from 29+/-4nm to 149+/-18nm. Dynamic light scattering (DLS) showed that the stability of polymerized vesicles against Triton X-100 was improved greatly compared with the conventional liposomes. In vitro drug release studies show that PCDA-incorporating vesicles reduce the paclitaxel release over the conventional phospholipids vesicles. 69+/-6% paclitaxel is released within 24h from the conventional vesicles, but the insertion of 50% and 75% molar ratio of PCDA changes the amount to 57+/-1% and 32+/-4%, respectively. Our results demonstrate that such novel polymerized vesicles have very good prospect as an anticancer drug carrier.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Antineoplastic Agents, Phytogenic / pharmacology
  • Chemical Phenomena
  • Delayed-Action Preparations*
  • Drug Stability
  • Fatty Acids, Unsaturated / chemistry*
  • Lipid Bilayers / chemistry*
  • Microscopy, Electron, Transmission
  • Molecular Structure
  • Paclitaxel / pharmacology
  • Particle Size
  • Phospholipids / chemistry*

Substances

  • 10, 12-pentacosadiynoic acid
  • Antineoplastic Agents, Phytogenic
  • Delayed-Action Preparations
  • Fatty Acids, Unsaturated
  • Lipid Bilayers
  • Phospholipids
  • Paclitaxel