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

以聚L-赖氨酸和聚L-丙交酯的AB型两亲性可生物降解二嵌段共聚物为聚合物胶束，通过聚离子络合物（PIC）的形成，制备了聚阴离子透明质酸（HA）包覆的可生物降解聚合物胶束。所得HA包被胶束在稀释条件下和血清存在下显示出极高的稳定性。此外，HA包被的胶束特异性结合肝窦内皮细胞。我们还制备了可生物降解的聚合物胶束与半乳糖轴承透明质酸（Gal-HA），并研究所获得的Gal-HA涂层胶束的细胞特异性识别。结果表明，半乳糖-透明质酸包被胶束通过半乳糖受体介导的机制表现出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.