槐定碱/苦参碱二元醇脂质体不同制备方法的比较

Comparison of sophoridine/matrine binary ethosomes prepared by different methods

目的:以包封率、粒径分布和Zeta电位为指标,探讨槐定碱/苦参碱(sophoridine/matrine,S/M)二元醇脂质体3种不同制备方法的适宜性。方法:用被动载药法(Ⅰ法)、主动载药法(Ⅱ法)和被动加主动载药法(Ⅲ法)分别制备了S/M的二元醇脂质体,并考察了3种方法制备的不同药脂比二元醇脂质体的包封率、粒径分布和Zeta电位。结果:当药脂比为1∶1时,用Ⅰ法制备的S二元醇脂质体包封率最高,用Ⅲ法制备的M二元醇脂质体包封率最高;用Ⅱ法制备时,2种碱的包封率均随药脂比的减小而增大;而采用Ⅰ/Ⅲ法时2种碱的包封率均随药脂比的减小而减小。结论:制备S/M二元醇脂质体时,不同的方法和药脂比对其包封率有显著影响。S二元醇脂质体适宜用Ⅰ法制备,而M二元醇脂质体则适宜用Ⅲ法。

OBJECTIVE According to encapsulation efficiency, particle size, Zeta potential, to compare the three different methods of preparation Sophoridine/Matrine binary ethosomes. METHODS The passive drug-loading method （method I ）, active drug-loading method （method II ）, and passive plus active drug loading method （method III ） were applied in this research to prepare S/M binary ethosomes, respectively. The encapsulation efficiency, particle size, Zeta potential of S/M binary ethosomes with different drug/lipid ratio was characterized. RESULTS When the drug/lipid ratio was 1 ： 1, S binary etho- somes prepared by the method I were the highest encapsulation efficiency, and M binary ethosomes prepared by method m were the highest rate; using the methods II, the encapsulation efficiency of two alkaloids increased with the decrease of drug/ lipid ratio; whereas using method I or III, the encapsulation efficiency of two alkaloids decreased with the decrease of drug/ lipid ratio. CONCLUSION For preparation of S/M binary ethosomes, the appropriate methods and drug/lipid ratio are important impacts of their encapsulation efficiency. Method I is suitable for preparation of S binary ethosomes. Method III is suitable for preparation of M binary ethosomes.