A Promising Drug Controlled-Release System Based on Diacetylene/ Phospholipid Polymerized Vesicles

Caixin Guo, Shaoqin Liu, Chang Jiang, Wenyuan Li, and Zhifei Dai
Langmuir 2009, 25(22), 13114–13119

A novel polymerized vesicular carrier loaded with paclitaxel was developed by introducing the ultraviolet (UV) crosslinkable 10,12-pentacosadiynoic acid (PCDA) into bilayered phospholipid vesicles with the purpose of improving the physicochemical stability as well as the controlled-release property of liposomes. Dynamic light scattering (DLS) and transmission electron microscopy (TEM) results revealed the enhanced stability of PCDA-polymerized vesicles against Triton X-100. In particular, alteration in PCDA/phospholipids ratios and UV-irradiation time can modulate the cumulative paclitaxel released. For instance, vesicles composed of phospholipids only released 98.0(2.1% of paclitaxel within 24 h. Over the same time period, 72.0 ( 5.8%, 43.9 ( 6.5%, and 20.1 ( 5.4% of paclitaxel was released from polymerized PCDA/phospholipid vesicles at molar ratios of 1:3, 1:1, and 3:1, respectively. Likewise, by increasing the UV-irradiation time from 20 to 40 min, the cumulative release of paclitaxel from polymerized  CDA/phospholipid vesicles at molar ratio of 1:1 decreased from 90.5 ( 3.7% to 37.6 ( 2.3% over a time period of experimental observation of 24 h. The influences of vesicle composition (i.e., PCDA/phospholipids ratio) and UV-irradiation time on the release rates of paclitaxel were further examined by finite element (FE) analyzed using Abaqus. Our results demonstrate that novel polymerized vesicles capable of regulating the release of anticancer drugs such as paclitaxel have been developed.