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目的:研制羧甲基壳聚糖(CMC)包衣长春西汀(VIN)纳米脂质体,并对其进行体外释药考察。方法:采用薄膜分散法制备VIN脂质体,用不同取代度的CMC包衣,经高压均质机乳匀得到CMC包衣的VIN纳米脂质体。以包封率为指标,正交试验筛选最佳处方;激光粒度分析仪测定其Zeta电位,粒径大小及分布,并用透射电镜观察其形态;体外透析法考察其体外释药性质。结果:CMC包衣VIN脂质体的最佳处方为药脂比1∶20,胆固醇∶卵磷脂1∶6,甘露醇占总量的50%,CMC的取代度为50%。其形态圆整,包衣效果理想,平均包封率为(72.2±2.4)%,Zeta电位为(-11.6±2.1)mV,平均粒径为(94.8±5.93)nm(n=3);体外释药曲线符合Higuchi方程:Q=-0.35220+0.20628t1/2(r=0.9925)。结论:CMC包衣VIN纳米脂质体包封率较高,达纳米级,体外具显著缓释性质。
OBJECTIVE: To develop carboxymethyl chitosan (CMC) coated vinpocetine (VIN) nano-liposomes and study their release in vitro. Methods: VIN liposomes were prepared by membrane dispersion method and coated with CMC with different degrees of substitution. The CMC-coated VIN nanosomes were uniformly emulsified by high pressure homogenizer. The entrapment efficiency as an index, orthogonal test screening the best prescription; laser particle size analyzer Zeta potential, particle size and distribution, and observed by transmission electron microscopy morphological; in vitro dialysis method in vitro release properties. Results: The optimum formulation of VIN coating liposome was CMC: lipid 1:20, cholesterol: lecithin 1:6, mannitol 50% of the total and CMC substitution 50%. The average encapsulation efficiency was (72.2 ± 2.4)%, the Zeta potential was (-11.6 ± 2.1) mV and the average particle diameter was (94.8 ± 5.93) nm (n = 3) The drug release curve conformed to the Higuchi equation: Q = -0.35220 + 0.20628t1 / 2 (r = 0.9925). Conclusion: The encapsulation efficiency of CMC-coated VIN nano-liposomes is high, reaching nano-scale, with significant sustained-release properties in vitro.