Liposomes for systematic delivery of vancomycin hydrochloride to decrease nephrotoxicity:Characterization and evaluation  

作　　者：Junli Liu Zhonglan Wang Fubing Li Jinhua Gao Longmei Wang Guihua Huang 

机构地区：[1]The School of Pharmaceutical Science,Shandong University,Ji'nan,China [2]Research Institue of Orthopaedic Trauma of PLA,Kunming General Hospital of Chengdu Military Command,Kunming,China

出　　处：《Asian Journal of Pharmaceutical Sciences》2015年第3期212-222,共11页亚洲药物制剂科学（英文）

摘　　要：Vancomycin hydrochloride(VANH),the first glycopeptide antibiotic,is a water-soluble drug for the treatment of acute osteomyelitis.Liposomal formulations of VANH have already been manipulated and characterized,which was a mean of increasing their therapeutic index,reducing their toxicity and altering drug biodistribution.One of the challenges for preparing VANH-Lips is their low encapsulation efficiency(EE).In the present study,we aim to improve the liposomal formulation of VANH for higher EE,longer systemic circulation,reduced nephrotoxicity and enhanced antimicrobial activities.Vancomycin hydrochloride-loaded liposomes(VANH-Lips)were formulated by the method of modified reverse phase evaporation.Based on the optimization of formulation with orthogonal experimental design,the average drug encapsulation efficiency and the mean particle size of VANH-Lips were found to be 40.78±2.56%and 188.4±2.77 nm.In vitro drug release of VANH-Lips possessed a sustained release characteristic and their release behavior was in accordance with the Weibull equation.After intravenous injection to mice,the mean residence time(MRT)of VANH-Lips group was significantly prolonged in vivo and the AUC value was improved as well compared with the vancomycin hydrochloride solution(VANH-Sol)group.Furthermore,the biodistribution results in mice showed that VANH-Lips decreased the accumulation of VANH in kidney after intravenous injection.In conclusion,VANH-Lips may be a potential delivery system for VANH to decrease nephrotoxicity in the treatment of osteomyelitis.

关 键 词：BIODISTRIBUTION NEPHROTOXICITY PHARMACOKINETIC Systematic delivery Vancomycin hydrochloride LIPOSOME 

分 类 号：R96[医药卫生—药理学]