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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 N-trimethyl chitosan (TMC) coated insulin ophthalmic liposomes (INSL) and screen the optimal formulation. Methods: INSL was prepared by reverse evaporation and coated with TMC (TMC60) with a quaternization degree of 60%. Taking the entrapment efficiency as the main index, the optimal prescription was screened by orthogonal test and its related in vitro properties were investigated. Results: The optimum prescription of TMC60 coated INSL was 1:50 for cholesterol to lecithin, 1: 4 for cholesterol and lecithin, and 4 mg · ml -1 for TMC60. Rotation temperature is 15 ℃. The optimal prescription of the average entrapment efficiency was (59.17 ± 1.46)% (n = 3). The average particle size of uncoated INSL was (88.97 ± 0.46) nm and the zeta potential was (-30.5 ± 0.46) mV. After coated with TMC60, the mean particle size was (91.33 ± 0.06) nm and the Zeta potential was (29.47 ± 0.15) mV. CONCLUSION: The entrapment efficiency of TMC60 coated INSL is high and its surface has high positive potential, which lays the foundation for the study of its ocular drug delivery system.