热聚合法自交联共轭亚油酸囊泡的制备与释药性能

Preparation and Drug Release Properties of the Self-crosslinked Conjugated Linoleic Acid Ufasomes by Thermal Polymerization

摘要:

以可聚合单体共轭亚油酸(CLA)及其钠盐混合物为原材料，在水溶液中经pH响应自组装得到共轭亚油酸囊泡(CLA-Ufasome)，再通过热聚合法对高浓度CLA-Ufasome自交联进行化学绑定，制备稳定的自交联共轭亚油酸囊泡(CLA-FAV)。采用透射电子显微镜(TEM)和动态激光光散射(DLS)对其进行表征，结果表明在pH 8.6条件下，经简单的热聚合法制备的CLA-FAV形貌与紫外法基本一致，在3-100 mmol?L-1 (500倍cvc)的浓度范围内均得到粒径为10-20 nm的CLA-FAV。该热聚合法CLA-FAV对五氟尿嘧啶具有良好的包载缓释效果。

Abstract:

Polymerizable monomer conjugated linoleic acid (CLA) and its ionized species (soap) were employed as raw materials to construct CLA-Ufasomes through pH-induced self-assembling in aqueous solution. Subsequently, CLA-Ufasomes self-assembled at high concentration were chemically tethered by intra-ufasomal self-crosslinking of conjugated double bonds in the CLA molecules through thermal polymerization to obtain the stable CLA-FAV. The morphologies and size distribution were characterized by transmission electron microscopy (TEM) and dynamic light scattering (DLS). The experimental results indicated that the morphology of the CLA-FAV prepared through thermal polymerization was consistent with that of the CLA-FAV obtained by UV irradiation at pH 8.6. Moreover, the CLA-FAV with diameter of 10-20 nm were always obtained in a wide concentration range of 3-100 mmol?L-1 (500 times of critical vesicular concentration of CLA). Finally, the in vitro release results of 5-fluorouracil (5-FU) showed that the CLA-FAV self-crosslinked through thermal polymerization possessed a good effect on encapsulation and release of 5-FU.