目的 制备cRGD介导的盐酸去氢骆驼蓬碱长循环脂质体,对其体外性质进行考察,建立cRGD介导的盐酸去氢骆驼蓬碱长循环脂质体的最终制备方法。方法 首先建立盐酸去氢骆驼蓬碱的含量测定方法,采用逆相蒸发法制备脂质体,并采用主动载药法和被动载药法两种方法包裹盐酸去氢骆驼蓬碱。在此基础上,利用cRGD-DSPE-2000取代部分磷脂成分,制备cRGD修饰的盐酸去氢骆驼蓬碱长循环脂质体,并对不同方法制得的脂质体的粒径、电位和包封率进行测定,从而最终确定cRGD修饰的盐酸去氢骆驼蓬长循环脂质体的制备方法。在此基础上,进行了脂质体的释放度考察。结果 除体积分数100%甲醇外,各标准曲线相关性均较好。被动载药法、主动载药法以及cRGD修饰的长循环脂质体的粒径分别为227.2、246.3、241.9 nm,ξ电位均在20~30 mV左右,包封率分别为(36.78±6.82)%、(81.77±7.61)%、(80.02±1.27)%。cRGD修饰长循环脂质体与普通脂质体和原料相比,释放更加缓慢平稳。结论 采用主动载药法制备cRGD修饰的盐酸去氢骆驼蓬碱脂质体具备一定的可行性。
Abstract
OBJECTIVE To prepare cRGD-modified harmine hydrochloride long circulating liposomes, investigate its characteristics in vitro, and finally establish its best preparation method. METHODS Firstly the content determination method was established, and secondly harmine hydrochloride liposomes were prepared through reverse phase evaporation method. Both active and passive drug loading methods were investigated to entrap the drug. Thirdly, cRGD-DSPE-2000 was prepared by conjugation method, and then cRGD modified harmine hydrochloride long circulating liposomes were prepared. Finally the particle sizes, Zeta potential and the entrapment efficiency were determined. The release of the liposomes in vitro was measured. RESULTS The standard curves all had good linearities except for the one using 100% methanol as solvent. The particle sizes of the liposomes prepared by passive loading method, active loading method, and long circulating cRGD modified liposomes were 227.2, 246.3 and 241.9 nm, respectively, and the Zeta potentials were about 20-30 mV. The entrapment efficiency were (36.78?6.82)%, (81.77?7.61)%, and (80.02?1.27)%, respectively. The release of cRGD liposomes was slower than the liposomes without cRGD and HM solution. CONCLUSION cRGD-modified long circulating harmine hydrochloride liposomes can be made through reverse phase evaporation method and active loading method.
关键词
盐酸去氢骆驼蓬碱 /
脂质体 /
包封率 /
粒径
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Key words
harmine hydrochloride /
liposome /
entrapment efficiency /
particle size
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中图分类号：
R944
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参考文献
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