本发明涉及一种多疏水核心侧链聚合物、多疏水核心载药材料及FK506制剂。其中多疏水核心侧链聚合物为聚赖氨酸与γ-苄基-L-谷氨酸-N-环内酸酐进行开环聚合反应得到形成的以聚赖氨酸链为骨架,含多条疏水聚谷氨酸苄酯侧链的聚合物。本发明提供的多疏水核心侧链聚合物,在水相溶液中,多疏水侧链聚合物的疏水侧链能够自组装形成多个疏水核心,通过疏水相互作用可以实现对FK506高效负载。该多疏水核心载体与聚乙二醇-聚谷氨酸两性解离共聚物通过电荷驱动自组装能够形成稳定的纳米结构。

Tacrolimus (FK506) is an immunosuppressant. The purpose of this study is to construct an ophthalmic drug delivery system which can efficiently load FK506, improve the ocular bioavailability of FK506 and enhance the effect of inhibiting corneal graft rejection. A polymer with multi-hydrophobic side chain was synthesized using ring opening polymerization of γ-benzyl-L glutamate N-carboxy anhydride initiated from the side amino groups of poly-lysine. This polymer could self-assembled with a PEG-PGA forming a with multi-hydrophobic core drug carriers.