Nanobiotechnology Division, Bio-X Center, State Key Laboratory of Urban Water Resources and Environment, School of Sciences, Harbin Institute of Technology, Harbin, 150001, China.
Langmuir. 2009 Nov 17;25(22):13114-9. doi: 10.1021/la9034112.
A novel polymerized vesicular carrier loaded with paclitaxel was developed by introducing the ultraviolet (UV) cross-linkable 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 PCDA/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.
一种新型聚合囊泡载体被开发出来，该载体装载有紫杉醇，通过将紫外（UV）可交联的 10,12-二十五碳二炔酸（PCDA）引入双层磷脂囊泡中，目的是提高脂质体的物理化学稳定性和控制释放性能。动态光散射（DLS）和透射电子显微镜（TEM）结果表明，PCDA 聚合囊泡对 Triton X-100 具有增强的稳定性。特别是，改变 PCDA/磷脂的比例和 UV 照射时间可以调节紫杉醇的累积释放。例如，仅由磷脂组成的囊泡在 24 小时内释放了 98.0 +/- 2.1%的紫杉醇。在相同的时间内，摩尔比为 1:3、1:1 和 3:1 的聚合 PCDA/磷脂囊泡分别释放了 72.0 +/- 5.8%、43.9 +/- 6.5%和 20.1 +/- 5.4%的紫杉醇。同样，通过将 UV 照射时间从 20 分钟增加到 40 分钟，摩尔比为 1:1 的聚合 PCDA/磷脂囊泡在 24 小时的实验观察时间内，紫杉醇的累积释放量从 90.5 +/- 3.7%减少到 37.6 +/- 2.3%。通过使用 Abaqus 进行有限元（FE）分析，进一步研究了囊泡组成（即 PCDA/磷脂比例）和 UV 照射时间对紫杉醇释放速率的影响。我们的结果表明，已经开发出了能够调节紫杉醇等抗癌药物释放的新型聚合囊泡。
