Preparation and Properties of Afatinib Liposome Freeze-Dried Powder
A novel liposomal freeze-dried powder designed as an inhalation agent is expected to solve the problems such as severe gastrointestinal adverse effects of afatinib due to oral administration.The optimal lyophilization process is determined based on the appearance morphology,solubility,particle size,and encapsulation rate,and the properties of the prepared lyophilized powder are characterized.The experimental results show that afatinib lipo-somal freeze-dried powder prepared by freeze-drying method with mannitol+lactose as combined lyophilization pro-tectant is a fluffy white powder with good solubility,slight moisture attraction and good fluidity.The average parti-cle size after re-dissolution is(167.0±3.7)nm,the encapsulation rate is(91.3±1.2)％,and the stability is good.In vitro release experiments show that the preparation is released slowly in PBS and PBS containing 20％FBS at the initial stage,and its release rate is about 60％at 48 h.In vitro cytotoxicity test shows that the tumor cytotox-icity of the freeze-dried powder of afatinib liposome is similar to that of afatinib liposome,with the IC50 value of(4.9±0.6)µg/mL.
万方数据
维普
