Polydiacetylene vesicles as a novel drug sustained-release system.
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.
Guo
Caixin
C
Instrumental Science and Technology, School Electrical Engineering and Automation, State Key Laboratory of Urban Water Resources and Environment, Harbin Institute of Technology, Harbin, China. 163gcx@sina.com
Liu
Shaoqin
S
Dai
Zhifei
Z
Jiang
Chang
C
Li
Wenyuan
W
D000972:Antineoplastic Agents, Phytogenic / Q000494:pharmacology; D055598:Chemical Phenomena; D003692:Delayed-Action Preparations; D004355:Drug Stability; D005231:Fatty Acids, Unsaturated / Q000737:chemistry*; D008051:Lipid Bilayers / Q000737:chemistry*; D046529:Microscopy, Electron, Transmission; D015394:Molecular Structure; D017239:Paclitaxel / Q000494:pharmacology; D010316:Particle Size; D010743:Phospholipids / Q000737:chemistry*
C493048:10, 12-pentacosadiynoic acid; D000972:Antineoplastic Agents, Phytogenic; D003692:Delayed-Action Preparations; D005231:Fatty Acids, Unsaturated; D008051:Lipid Bilayers; D010743:Phospholipids; D017239:Paclitaxel