Development of high stable biodegradable polyion complex-coated polymeric micelles as drug carriers

采用带正电荷的聚l -赖氨酸和聚l -丙交酯双嵌段共聚物胶束形成聚离子络合物（PIC），制备了可降解聚阴离子透明质酸（HA）包被聚合物胶束。得到的ha包被胶束在稀释条件下和血清存在下表现出极高的稳定性。此外，ha包被的胶束特异性地与肝窦内皮细胞结合。我们还制备了含有半乳糖透明质酸（Gal-HA）的可生物降解聚合物胶束，并研究了所获得的Gal-HA包被胶束的细胞特异性识别。结果表明，gal - ha包被的胶束通过半乳糖受体介导的机制被细胞特异性摄取到肝癌中。

We prepared biodegradable polymeric micelles coated with polyanionic hyaluronic acid (HA) by polyion complex (PIC) formation from positively charged polymeric micelles consisting of amphiphilic biodegradable AB-type diblock copolymers of poly(L-lysine) and poly(L-lactide). The obtained HA-coated micelles showed extremely higher stability under diluted condition and in the presence of serum. Moreover, the HA-coated micelles specifically bound to liver sinusoidal endothelial cells. We also prepared biodegradable polymeric micelles coated with galactose bearing hyaluronic acid (Gal-HA) and investigated cell-specific recognition of the obtained Gal-HA-coated micelles. The obtained results suggested that the Gal-HA-coated micelles showed cell-specific uptake into hepatoma via galactose receptor mediated mechanism.