聚乙二醇对盐酸伊立替康脂质体体外释放及在不同稀释介质中稳定性的影响

目的:考察不同聚乙二醇含量对盐酸伊立替康脂质体体外释放特性及在不同稀释介质中稳定性的影响。方法:采用乙二胺四乙酸铵梯度法,以聚乙二醇2000含量分别为0、8、14、20、26 mg/ml的聚乙二醇2000-二硬脂酰磷脂酰乙醇胺(m PEG2000-DSPE)制备盐酸伊立替康脂质体,测定其包封率和粒径,评价其体外24 h内的累积释放度和在生理氯化钠溶液与5%葡萄糖注射液中的稳定性。结果:随着m PEG2000-DSPE含量的增加,盐酸伊立替康脂质体体外24 h累积释放度逐渐减小;以生理氯化钠溶液及5%葡萄糖注射液稀释后,随着m PEG2000-DSPE含量的增加,盐酸伊立替康脂质体的包封率和粒径变化均减小;当聚乙二醇2000质量浓度增加至20、26 mg/ml时,脂质体包封率和粒径基本不再变化。结论:m PEG2000-DSPE的加入可减慢盐酸伊立替康脂质体的体外释放,提高其在不同稀释介质中的稳定性。

Effects of Polyethylene Glycol on Drug Release and Stability of Irinotecan Hydrochloride Liposomes in vitro in Different Dilution Mediums

OBJECTIVE：To evaluate the effects of polyethylene glycol on drug release in vitro and stability of Irinotecan hydrochloride（CPT-11）liposomes in different dilution mediums. METHODS：The CPT-11 liposomes were prepared with PEG 2000-disteroylphosphoethanolamine（m PEG2000-DSPE）containing 0,8,14,20 and 26 mg/ml PEG2000 by ammonium ethylenediaminetetra acetate gradient method. The entrapment efficiencies and particle size of CPT-11 liposomes were determined. 24 h accumulative release rate in vitro and stability of the liposomes were evaluated in physiological solution of sodium chloride and 5% Glucose injection. RESULTS：With the increase of m PEG2000-DSPE content,24 h accumulative release rate in vitro of CPT-11 liposomes decreased gradually;the entrapment efficiencies and particle size of CPT-11 liposomes decreased after diluted by physiological solution of sodium chloride or 5% Glucose injection. When the concentration of PEG2000 reached 20 and 26 mg/ml,the entrapment efficiencies and particle size had almost no change. CONCLUSIONS：m PEG2000-DSPE can decrease drug release of CPT-11 liposomes in vitro,and improve stability of it in different mediums.