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目的:研制N-三甲基壳聚糖(TMC)包衣的盐酸阿霉素(ADM)脂质体。方法:采用硫酸铵梯度法制备ADM脂质体,以包封率为指标,筛选盐酸阿霉素脂质体最佳处方;合成不同季铵化程度的TMC,并对最佳ADM脂质体进行包衣。结果:未包衣ADM脂质体平均粒径为(378.6±5.2)nm,Zeta电位为(-62.08±2.5)mv,平均包封率为(62.27±1.75)%(n=3)。TMC包衣后,脂质体粒径增大,并随着TMC季铵化程度的增大,Zeta电位显著增大(P<0.05);TMC20、TMC40、TMC60包衣脂质体体外释药曲线符合Higuchi方程,分别为:Q=7.6315+3.7863t_(1/2)(r=0.929 2),Q=6.9647+3.5709t_(1/2)(r=0.9318),Q= 7.3451+2.7665t_(1/2)(r=0.935 7)。结论:TMC包衣ADM脂质体的制备工艺可行,其表面带有较高正电性,为下一步研究其血管靶向性打下基础。
Objective: To develop N-trimethyl chitosan (TMC) coated doxorubicin hydrochloride (ADM) liposomes. Methods: The ADM liposomes were prepared by ammonium sulfate gradient method. The entrapment efficiency was used as an index to screen the optimal formulation of doxorubicin hydrochloride liposomes. TMCs with different degrees of quaternization were synthesized and the optimal ADM liposomes Coating. RESULTS: The average diameter of uncoated ADM liposomes was (378.6 ± 5.2) nm and the Zeta potential was (-62.08 ± 2.5) mv. The average entrapment efficiency was 62.27 ± 1.75% (n = 3). After TMC coating, the liposome size increased, and the Zeta potential increased significantly with the increase of the quaternization degree of TMC (P <0.05). The in vitro release profiles of TMC20, TMC40 and TMC60 coated liposomes According to the Higuchi equation, Q = 7.6315 + 3.7863 t 1/2 (r = 0.929 2), Q = 6.9647 + 3.5709 t 1/2 (r = 0.9318), Q = 7.3451 + 2.7665 t -1 /2)(r=0.9357). CONCLUSION: The preparation of TMC-coated ADM liposomes is viable. The surface of the TMC-coated ADM liposomes possesses higher positive charge, which lays the foundation for further study of vascular targeting.