Development of tacrolimus-loaded transfersomes for deeper skin penetration enhancement and therapeutic effect improvement in vivo  

作　　者：Wei Lei Chuqin Yu Huaqing Lin Xiaoyuan Zhou 

机构地区：[1]Department of Pharmacy,Guangdong Pharmaceutical University,Guangzhou 510006,China

出　　处：《Asian Journal of Pharmaceutical Sciences》2013年第6期336-345,共10页亚洲药物制剂科学（英文）

摘　　要：The aims of this study were to prepare novel transfersomes(TFs)for tacrolimus to treat atopic dermatitis,and to observe the therapeutic effects on mice atopic dermatitis,as compared to commercial tacrolimus ointment(Protopic
)and liposomes-gel.Different kinds of surfactantsdsodium cholate,Tween 80 and Span 80 were investigated to prepare TFs respectively.TFs-Tween 80 was selected as the optimal carrier owing to the best deformability and the highest drug retentions.Entrapment efficiency and diameter were also evaluated.The optimized TFs were further made into gel and in vitro drug release of TFs-gel after 24 h was higher than the commercial ointment.Cumulative drug release from TFs-gel after 12 h in vitro was 37.6%.The optimized TFs-gel illustrated remarkably highest drug skin retentions when compared with liposomes-gel and commercial ointment in vivo skin retention experiments.The amounts of tacrolimus in epidermis and dermis from TFsgel were 3.8 times and 4.2 times respectively as much as ointment,while liposomes-gel was only 1.7 times and 1.4 times respectively as compared to ointment.Topical application of TFs-gel displayed the best therapeutic effect on mice atopic dermatitis induced by repeated topical application of 2,4-dinitrofluorobenzene.Thus TFs displayed superior performance and effective skin target for topical delivery of tacrolimus.

关 键 词：TRANSFERSOMES TACROLIMUS TRANSDERMAL Deep skin layer target In vivo therapy 

分 类 号：Q73[生物学—分子生物学]