透明质酸-1-甲基色氨酸胶束的制备和表征  

Synthesis and characterization of hyaluronic acid-1-methyltryptophan micelle

作　　者：陈雪 胡英 黄丹丹 孙逊[1] 龚涛[1] 张志荣[1] 符垚[1] CHEN Xue;HU Ying;HUANG Dandan;SUN Xun;GONG Tao;ZHANG Zhirong;FU Yao(West China School of Pharmacy,Sichuan University,Chengdu,Sichuan,610041 P.R.China)

机构地区：[1]四川大学华西药学院,四川成都610041

出　　处：《华西药学杂志》2021年第3期237-240,共4页West China Journal of Pharmaceutical Sciences

基　　金：国家自然科学基金资助项目(批准号:81773654);四川省科技厅项目(2019YJ0019)。

摘　　要：目的制备载1-甲基色氨酸(MT)的透明质酸(HA)胶束。方法采用二碳酸二叔丁酯对MT的氨基进行保护,通过MT的羧基与HA的羟基反应形成酯键,对衍生物进行脱保护,获得透明质酸-1-甲基色氨酸(m-HA),并通过核磁共振氢谱进行结构表征。将m-HA溶解在PBS中自组装,形成聚合物胶束,并对胶束的粒径和电位进行表征。结果通过核磁共振氢谱表征证实m-HA制备成功,且其能自组装形成胶束,胶束的粒径均一。结论m-HA有望成为一种有效的靶向载体递送小分子药物MT到达肿瘤组织。OBJECTIVE To synthesize a hyaluronic acid derivative conjugated with 1-methyl tryptophan(MT).METHODS The amine group of MT was protected by dimethyl carbonate tert-butyl ester(Boc),and the carboxyl group of MT was reacted with the hydroxyl groups of hyaluronic acid(HA).Then hyaluronic acid-1-methyltryptophan conjugate(m-HA)was obtained through removing the Boc protection of the derivatives,and the structure of which was validated by proton nuclear magnetic resonance spectrum.Next,m-HA was self-assembled into polymeric micelles in phosphate buffer saline,and the particle size and Zeta potential of the micelles were characterized.RESULTS The results showed that m-HA was successfully synthesized and self-assembled into micelles with uniform particle size.CONCLUSION M-HA is expected to be an efficient carrier to deliver small molecule MT to tumor.

关 键 词：1-甲基色氨酸 吲哚胺-2 3-双加氧酶 透明质酸 CD44 透明质酸-1-甲基色氨酸 两亲性结构 聚合物胶束 靶向递送 免疫治疗 

分 类 号：R914[医药卫生—药物化学] R94[医药卫生—药学]