盐酸博安霉素脂质体的制备及表征

Preparation and characterization of boanmycin liposomes

目的探讨制备方法对博安霉素脂质体包封率的影响,考察其制备的影响因素,优化处方工艺,并对其特性进行表征。方法分别采用乙醇注入法和逆向蒸发法制备博安霉素脂质体(boanmycin liposomes,BAM-Ls),确定最终工艺及处方。并对其包封率、粒径、Zeta电位和形态进行综合评价。结果逆向蒸发法制备BAM-Ls时药物包封率明显高于乙醇注入法,最终处方磷脂浓度为10mg/mL、磷脂胆固醇比为4:1(W/W)、水/乙醚比为1:3(V/V)时,所得脂质体包封率最高,约为30%。粒径为150nm,Zeta电位为-22.8mV,7d内脂质体稳定性良好。结论逆向蒸发法制备的BAM-Ls理化性质及稳定性良好。

Objective To prepare boanmycin loaded liposomes （BAM-Ls）, to study the influencing factors, to optimize their formulation and to characterize their properties. Methods BAM-Ls were prepared by ethanol injection and reverse evaporation method, the final process and prescription was determined. BAM-Ls were investigated using entrapment efficiency, particle size, and Zeta potential as indicators. Their physicochemical properties and stability were evaluated. Results BAM-Ls prepared using the optimal formulation, the concentration of EPCS was 1Omg/mL, the ratio of EPCS and Chol was 4： 1 （WIW） and the ratio of water and ether was 1：3 （V/V） showed a highest EE% of 30%, a particle size of 150nm, a Zeta potential of -22.8mV. There were no significant changes of the BAM-Ls in EE%, particle size and Zeta potential after treatment at 4℃ for 7 days. Conclusion BAM-Ls prepared with the optimized formulation by reverse evaporation method had good physicochemical properties and stability.