cRGD介导的盐酸去氢骆驼蓬碱长循环脂质体的制备研究

发布时间：2018-04-14 18:45

  本文选题：盐酸去氢骆驼蓬碱 + 脂质体　； 参考：《中国药学杂志》2015年08期

【摘要】：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 m V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 mediated long circulating liposome of deshlorophorine hydrochloride and to study its properties in vitro and to establish the final preparation method of cRGD mediated long circulating liposome of dehydrolampine hydrochloride.Methods at first, a method was established for the determination of dehydrolampine hydrochloride. Liposomes were prepared by reverse phase evaporation, and the active drug loading method and passive drug loading method were used to encapsulate the dehydrolordine hydrochloride.On this basis, cRGD-DSPE-2000 was used to replace some phospholipid components to prepare long-circulating liposomes modified with cRGD. The particle size, potential and entrapment efficiency of the liposomes prepared by different methods were determined.Finally, the preparation method of long circulating liposomes modified by cRGD was determined.On this basis, the release of liposome was investigated.Results except 100% methanol, the correlation of standard curves was good.The particle size of long-cycle liposomes modified by passive drug loading, active drug loading and cRGD modification were 227.2246.3nm, 尉 potential were about 200.30mV, and the entrapment efficiency were 36.78 卤6.82 卤80.02 卤80.02 卤80.02 卤1.27)%.cRGD, respectively, and the release was slower and more stable than that of ordinary liposomes and raw materials.Conclusion it is feasible to prepare cRGD modified liposome of dehydrolampine hydrochloride by active drug loading method.
【作者单位】： 新疆医科大学;
【分类号】：R943
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本文编号：1750549