甘草次酸修饰的聚谷氨酸苄酯包载喜树碱纳米球的制备及评价

Preparation and Evaluation of Camptothecin-loaded Glycyrrhetinic Acid-modified Poly(γ-benzyl-L-glutamate) Nanospheres

利用甘草次酸(glycyrrhetinic acid,GA)修饰聚谷氨酸苄酯(PBLG),合成出聚合度为20和50的2种GA-NH-PBLG材料,通过核磁共振、红外光谱对其结构进行确认。利用这2种材料包载抗癌药物喜树碱,采用溶剂挥发法制备纳米球,采用扫描电镜对纳米球的理化性质进行表征,并通过体外释放实验评价了其体外释放性能。结果表明:纳米球粒径分布在50～300 nm之间,在电解质溶液中具有较高的稳定性。2种材料制得的纳米球包封率和载药量分别为77.3%、82.4%和1.4%、2.3%,在PBS缓冲溶液中具有较好缓释效果,8 d内药物的累计释放量达50%。该研究为具主动和被动双重肝靶向性纳米球的制备奠定了基础。

To study the preparation of nanospheres（NPs） surface-modified with glycyrrhetinic acid（GA） targeting to hepatocytes.The two GA-NH-PBLG material with the degree of polymerization of 20 and 50,were synthesized bypoly-glutamic acid benzyl ester（PBLG） with GA modified.Their structure was determined by nuclear magnetic resonance and infrared spectroscopy.The two materials were formed into NPs loaded the camptothecin via solvent evaporation method,the physical and chemical properties of the NPs were investigated by scanning electron microscopy,and the release in vitro was evaluated in vitro release study.Result shows the size of the NPs distributed between 50~300 nm and the NPs exhibited good stability against electrolyte solution.The entrapment efficiency and drug loading amount were 77.3%,82.4% and 1.4%,2.3%,respectively.The NPs had a good sustained release effect in PBS buffer solution,the drug cumulative release reached 50% in 8 days.The study laid the foundation for the preparation of NPs with active and passive double liver targeting property by the materials.