丹参酮传递体的制备及其变形性

目的考察丹参酮传递体的制备工艺,并评价其质量。方法用薄膜分散法制备丹参酮传递体,考察其形态、含量、包封率、粒径、多分散度及Zate电位;并对传递体的稳定性和变形性进行研究。结果丹参酮传递体球形圆整,大小较均匀,含量为(1.0192±0.075)mg/ml,包封率为(62.3±0.08)%,算术平均粒径110 nm,多分散度为0.19,Zate电位为-15 mV;丹参酮传递体分散于0.9%氯化钠注射用水中,4℃避光保存3个月稳定;证实了含有胆酸钠的传递体在外压作用下特定的变形性。结论丹参酮传递体的制备工艺对其质量有较大影响,选择薄膜分散法优化工艺制备得到的丹参酮传递体包封率较高,稳定性较好。表面活性剂胆酸钠的存在促进脂质体的变形,这种作用与胆酸钠在磷脂双分子层中所占比例及外压有关。

Preparation of tanshinone transfersome and its deformability

OBJECTIVE: To prepare tanshinone transfersome (TTs) and evaluate its deformability. METHODS: The transfersomes were prepared by film dispersion method followed by sonication, and their physical properties, morphology, content, entrapment efficiency, particle size, polydispersity, and Zeta potential were investigated. The stability and deformability of TTs were studied. Liposomes with different molar ratios of cholate and lecithin were compared for their permeability under external pressure. RESULTS: The prepared TF were spherical vesicles with content of 1.0192+/-0.075 mg/ml, entrapment efficiency of (62.3+/-0.08)%, particle size of 110 nm, polydispersity of 0.19 and Zate potential of -15.0 mV. The TTs remained stable during light-proof preservation for 3 months at 4 degrees C, and sodium cholate contributed to the flexibility of the lecithin vesicles. CONCLUSION: TTs prepared by film dispersion method has good entrapment efficiency and stability. The vesicles possess high deformability in relation to the molar ratio of sodium cholate to lecithin and the external pressure.