关键词: 药剂学, 透明质酸, 阿霉素, 聚合物胶束, 抗肿瘤

Abstract: In order to enchance the efficacy of antineoplastic drugs targeting and antitumor activity,hyaluronic acid-g-octadecyl conjugates were synthesized and used as vehicles for anti-cancer drugs.Doxorubicin(DOX)-loaded hyaluronic acid-g-octadecyl copolymeric micelles were prepared with ultrasonic method.The pharmaceutical properties of the micelles were investigated.The particle sizes of blank micelles and drug-loaded micelles were(180.7±1.25)nm and(178.3±2.24)nm; zeta potentials were(-21.3±0.25)mV and(-18.1±0.31)mV,respectively.The encapsulation efficiency and drug loading of drug-loaded micelles were(96.1%±0.72%) and(16.1%±1.18%),respectively.In vitro drug release study demonstrated that the cumulative release of DOX was merely about 40% at 72h,indicating that the copolymer micelles presented obvious sustained-release behavior.In vitro cytotoxicity assays showed that the blank micelles were nontoxic against all MCF-7 cells.However,DOX-loaded micelles presented significantly inhibitory effect on the tumor cells in a dose manner.Therefore,hyaluronic acid-g-octadecyl copolymeric micelles exhibited the characteristics of high drug envelopment rate,sustained-release behavior and potent antitumor effect.

Key words: pharmaceutics, hyaluronic acid, doxorubicin, copolymeric micelles, antitumor