Preparation of cisplatin liposomes and their in vitro and in vivo evaluation
Objective To prepare cisplatin lipid complex liposomes in order to reduce the toxic and side effects of cisplatin and maintain the efficacy of the drug.Methods Cisplatin lipid complex liposomes were prepared by reverse phase evaporation;SD rats were used as experimental animals to investigate the pharmacokinetics of cisplatin liposomes in vivo;H22 tumor bearing mice were used as models,and cisplatin for injection was used as a reference to investigate the efficacy and side effects of cisplatin liposomes.Results The average particle size of the prepared cisplatin lipid complex liposomes were 109.8 nm,and the entrapment efficiency was as high as 90％.The pharmacokinetics results in rats showed that compared with cisplatin for injection,cisplatin complex liposome ρmax was significantly increased by 2.93 times(P＜0.001),t1/2α 65.50 times longer(P＜0.01);AUC0-24 was significantly increased by 41.26 times(P＜0.01),and CDDP-MM significantly improved the pharmacokinetics of cisplatin for injection in vivo.The results of anti-tumor activity in mice showed that the tumor inhibition rate of CDDP-MM was as high as 82.5％,and the body weight increased significantly compared with cisplatin for injection(P＜0.000 1).Renal injury decreased significantly.Conclusion CDDP-MM can effectively inhibit tumor growth and significantly reduce gastrointestinal toxicity and nephrotoxicity compared with cisplatin for injection.
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