N-三甲基壳聚糖包衣胰岛素眼用纳米脂质体的研制

Study on the Preparation of Insulin Nanoliposomes Coated by N-trimethyl Chitosan

目的:制备N-三甲基壳聚糖(TMC)包衣胰岛素眼用纳米脂质体(INSL),筛选最优处方。方法:采用逆向蒸发法制备INSL,并用季铵化程度为60%的TMC(TMC60)对其进行包衣。以包封率为主要指标,用正交试验筛选最优处方,并对其相关体外性质进行考察。结果:TMC60包衣INSL的最优处方组成为:药脂比为1:50,胆固醇与卵磷脂之比为1:4,TMC60的最佳浓度为4 mg·ml^(-1);最佳旋蒸温度为15℃。最优处方的平均包封率为(59.17±1.46)%(n=3)。未包衣的INSL的平均粒径为(88.97±0.46)nm,Zeta电位为(-30.5±0.46)mV。TMC60包衣后,平均粒径为(91.33±0.06)nm,Zeta电位为(29.47±0.15)mV。结论:TMC60包衣INSL的包封率较高,表面带有较高的正电位,为研究其眼部释药系统奠定了实验基础。

Objective：To prepare insulin nanoliposomes（INSL） coated by N-trimethyl chitosan（TMC） and screen the optimal formula.Method：INSL were prepared by the reverse evaporation method,and TMC with 60%degree of quarternization（DQ） （TMC60） was used as the coating material.The encapsulation efficiency as the index,the optimal formula of the preparation was screened using the orthogonal experiment,and the characteristics in vitro of the preparation were investigated.Result：The optimal formula of the TMC60-coated INSL was as follows：the ratio of drug and lipid was 1：50,the ratio of cholesterol and lecithin was 1：4,and the optimum concentration of TMC60 was 4 mg · ml^（-1） with 15℃as the rotary evaporation temperature.The mean entrapment efficiency of the optimal TMC60-coated INSL was（59.17±1.46）%（n = 3）.The mean diameter of INSL before the coating was（88.97±0.46） nm,and the Zeta potential was（-30.5±0.46） mV.The mean diameter of INSL after TMC60-coating was（91.33±0.06） nm,and the Zeta potential was（29.47±0.15） mV.Conclusion;The encapsulation efficiency and the positive Zeta potential of the preparation are promising,which can provide experimental foundation for the further study of the ophthalmic drug release system.