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目的:制备羧甲基壳聚糖(CMC)包衣尼莫地平(NMD)纳米脂质体,并考察其在小鼠体内的组织分布。方法:采用薄膜分散法制备NMD脂质体,用CMC包衣后经高压均质机乳匀,得到CMC包衣NMD纳米脂质体。测定其包封率,Zeta电位,粒径大小及分布。对小鼠尾静脉注射普通NMD脂质体,CMC包衣脂质体(未乳匀),纳米脂质体(未包衣),CMC包衣纳米脂质体,于预定时间测定血浆及心,肝,脾,肺,肾,脑组织中的血药浓度,计算相关靶向参数。结果:包衣纳米脂质体的包封率为(71.2±4.8)%,Zeta电位为(-11.4±1.6)mV,平均粒径为(95.4±7.2)nm(n=3),与市售NMD注射液相比,脑组织中的TI,RTE分别为310.7%,58.25%。结论:本实验制备的CMC包衣NMD纳米脂质体包封率高,粒径达纳米级,并具有较好的脑靶向性。
OBJECTIVE: To prepare carboxymethyl chitosan (CMC) coated nimodipine (NMD) nanoliposomes and study their tissue distribution in mice. Methods: The NMD liposomes were prepared by the method of film dispersion. After coated with CMC and homogenized by high pressure homogenizer, the NMD liposomes were obtained. Determination of entrapment efficiency, Zeta potential, size and distribution of particle size. The mice were injected with normal NMD liposomes, CMC coating liposomes (non-uniform), nano-liposomes (uncoated) and CMC-coated nano-liposomes in the tail vein of mice. Plasma and heart were measured at a predetermined time, Liver, spleen, lung, kidney, brain tissue concentration of blood, calculate the relevant target parameters. Results: The encapsulation efficiency of the coated liposomes was (71.2 ± 4.8)% and the Zeta potential was (-11.4 ± 1.6) mV and the mean diameter was (95.4 ± 7.2) nm Compared with NMD injection, TI and RTE in brain tissue were 310.7% and 58.25%, respectively. CONCLUSION: The CMC-coated NMD nanoliposomes prepared in this experiment have high encapsulation efficiency, nanometer size, and good brain targeting.