3种方法制备硫酸卷曲霉素脂质体及其药剂学性质考察

目的:制备硫酸卷曲霉素脂质体并对其性质进行考察。方法:分别采用pH梯度法、硫酸铵梯度法和醋酸钠梯度法3种主动载药法制备硫酸卷曲霉素脂质体并将其制成冻干制剂,通过测定包封率、粒径和ζ电位及考察稳定性等研究脂质体的性质。结果:3种方法制备硫酸卷曲霉素脂质体的包封率冻干前、后分别为65.7%、65.2%,20.1%、18.6%,34.6%、32.4%,粒径分别为136、145nm,144、153nm,142、159nm,ζ电位分别为—20.2、—19.5mV,—24.4、—22.9mV,—18.7、—17.8mV。稳定性考察各项指标均无明显改变。结论:3种方法中pH梯度法更适于制备硫酸卷曲霉素脂质体。

Study on Preparation and Pharmaceutical Character of Capreomycin Sulfate Liposomes by Three Kinds of Methods

OBJECTIVE： To prepare and characterize capreomycin sulfate liposomes（CSL） . METHODS： Capreomycin sulfate was entrapped into liposomes using active loading that pH gradient methods, ammonium sulfate gradient methods and sodium acetate gradient methods respectively followed by lyophilization technique. The liposome was characterized by entrapment efficiency, particle size, ξ potential and the stability. RESULTS： The entrapment efficiency of CSL pre- and post- lyophilization prepared by three methods were 65.7% and 65.2 %, 20.1% and 18.6%, 34.6% and 32.4%,with particle size of 136 and 145 nm, 144 and 153 nm, 142 and 159 nm, ξ potential of -20.2 and -19.5 mV,-24.4 and -22.9 mV,-18.7 and -17.8 mV respectively. No obvious changes were found in all the indexes in the stability test. CONCLUSIONS： The pH gradient technique is suitable for preparing CSL in 3 kinds of methods.