载阿霉素混合胶束的制备及制剂工艺优化
Fujian Journal of Traditional Chinese Medicine（2020）
Abstract
目的 制备载阿霉素(DOX)的混合胶束,并优化其冻干制剂工艺.方法 以TPGS-甘草次酸偶联物(TG偶联物)和TPGS修饰的羧甲基壳聚糖-大黄酸偶联物(TCR偶联物)为混合胶束载体材料(TCR-TG),利用透析法制备载DOX的混合胶束(DOX/TCR-TG胶束),以载药量、包封率、粒径为评价指标,考察TG偶联物和TCR偶联物的投料比、DOX与TCR-TG的投料比,确定DOX/TCR-TG胶束最佳制备工艺.考察冻干保护剂的种类及用量,确定DOX/TCR-TG胶束的最佳冻干工艺.结果 DOX/TCR-TG胶束平均粒径为(121.3±8.49)nm,PDI为(0.21±0.02),Zeta电位为(-21.9±0.2)mV,载药量为(31.22±3.19)％,包封率为(62.59±6.39)％,其中TG偶联物和TCR偶联物最佳投料比为1:2,DOX和TCR-TG的最佳投料比为1:1.7,DOX/TCR-TG混合胶束冻干制剂的最佳保护剂为0.1％甘露醇.结论 TG偶联物与TCR偶联物形成的混合载体材料包载DOX,可制备成载药量和包封率较好,粒径分布均匀,形态圆整的聚合物胶束制剂.
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