Preparation and evaluation of nattokinaseloaded self-double-emulsifying drug delivery system  

作　　者：Xiaona Wang Sifan Jiang Xinyue Wang Jie Liao Zongning Yin 

机构地区：[1]Key Laboratory of Drug Targeting and Drug Delivery Systems,West China School of Pharmacy,Sichuan University,No.17,Block 3,Southern Renmin Road,Chengdu 610041,China

出　　处：《Asian Journal of Pharmaceutical Sciences》2015年第5期386-395,共10页亚洲药物制剂科学（英文）

基　　金：supported by National Natural Science Foundation of China(No.81373338).

摘　　要：In the present study,we prepared nattokinase-loaded self-double-emulsifying drug delivery system(SDEDDS)and investigated its preliminary pharmacodynamics.The type and concentration of oil phase,inner aqueous phase and emulsifier were screened to prepare optimum nattokinase-loaded SDEDDS.Next,the optimum formulations were characterized based on microstructure,volume-weighted mean droplet size,self-emulsifying rate,yield,storage stability,in vitro release and in vivo pharmacodynamics studies.The water/oil/watermultiple emulsions exhibited typicalmultiple structure,with relatively small volumeweighted mean droplet size 6.0±0.7μm and high self-emulsifying ability(self-emulsifying time<2 min).Encapsulation of nattokinase was up to 86.8±8.2%.The cumulative release of nattokinase within 8 h was about 30%,exhibiting a sustained release effect.The pharmacodynamics study indicated that nattokinase-loaded SDEDDS could significantly prolong the whole blood clotting time in mouse and effectively improve the carrageenan-induced tail thrombosis compared with nattokinase solution.Moreover,we showed that SDEDDS could successfully self-emulsify into water/oil/water multiple emulsions upon dilution in dispersion medium with gentle stirring and effectively protect nattokinase activity in gastric environment.Our findings suggested that SDEDDS could be a promising strategy for peptide and protein drugs by oral administration.

关 键 词：Self-double-emulsifying drug delivery system NATTOKINASE Yield Release in vitro Pharmacodynamics study 

分 类 号：S60[农业科学—园艺学]