猕猴桃根多糖脂质体的处方工艺研究

Process research of formulation and preparation on polysaccharide liposomes in Chinese actinidia root

目的:确定猕猴桃根多糖(APPS)脂质体的制备方法,考察处方组成和制备工艺的影响因素。方法:采用3种不同方法制备APPS脂质体,以包封率、载药量和稳定系数为指标,优选最佳制备方法以及考察各制备因素的影响。结果:逆相蒸发法制备的APPS脂质体包封率为(48.80±0.46)%、载药量为(4.79±0.04)%、稳定系数为(0.2558±0.1200)。以1/10离子强度的p H值7.4 PBS缓冲液为水合介质制备的APPS脂质体包封率为74.77%,稳定系数为0.1448;药脂比1∶20时制得的脂质体优于其他两种比例,其包封率为60.50%,稳定系数为0.087;以PEG2000为脂质膜成膜材料制备的脂质体的包封率为(59.80±1.83)%,稳定系数为(0.1188±0.0300);PEG与卵磷脂比例在0.25∶1时其包封率更佳,包封率为62.48%;转速60r/min制得的脂质体包封率为57.10%,稳定系数为0.1383;25℃下制备的脂质体其包封率为58.88%,稳定系数为0.0561;搅拌2min时得到的脂质体包封率为73.20%,均优于其他水平。结论:经综合考虑,采用逆相蒸发法,选用1/10离子强度的p H值7.4 PBS为水合介质,药脂比1∶20,PEG2000为脂质膜成膜材料,PEG与卵磷脂的比例为0.25∶1,转速60r/min,温度25℃,搅拌2min制备APPS脂质体工艺较优。

Objective： To determine the preparation technique of polysaccharide liposomes in Chinese actinidia root, and to observe the effect factors of the composition and preparation of prescription. Methods： Actinidia planch polysaccharide （APPS） was preparation in three different methods, and the optimum preparation method was selected by investigating the effect of preparation factors, the indexes included encapsulation ratio, drug loading and stability factor were studied by three different methods, Results： The encapsulation ratio of the reverse phase evaporation was （48.80±0.46）%, the drug loading was （4.79±0.04）%; and the stability factor was （0.2558±0.1200）. The PBS （pH=7.4） with 1/10 the ionic strength was prepared for hydration medium APPS liposomes, the encapsulation ratio was 74.77%, and the stability factor was 0.1448. The APPS liposomes obtained by 1：20 ratio of drug was better than the other two proportions, the encapsulation ratio was 60.50%, and the stability factor was 0.087. The lipid membrane of liposomes package APPS was prepared with PEG 2000 as the film-forming material, so the encapsulation ratio was （59.80±1.83）%, the stability factor was （0.1188±0.0300）, when the rate of PEG and lecithin was 0.25：1, the encapsulation ratio and stability factor were better, its encapsulation ratio was 62.48%, the encapsulation ratio was 57.10% at speed 60r/min, while the stability factor was 0.1383, the encapsulation ratio was 58.88% under 25℃, while the stability factor was 0.0561.When it mixed for 2min, the encapsulation ratio was 73.20%, arid much better than other levels. Conclusion： After comprehensive consideration, the preparation of APPS liposomes is used the reverse phase evaporation method, the choice of 1/10 of the ionic strength of pH=7.4 PBS as hydration medium, drug to lipid ratio of 1 ： 20, PEG2000 as the lipid membrane forming material, PEG and lecithin ratio of 0.25：1, speed 60r/min, temperature 25℃, homogenization time 2min,