Food protein-stabilized nanoemulsions as potential delivery systems for poorly water-soluble drugs: preparation, in vitro characterization, and pharmacokinetics in rats

被引:149
作者
He, Wei [1 ]
Tan, Yanan [1 ]
Tian, Zhiqiang [1 ]
Chen, Lingyun [2 ]
Hu, Fuqiang [3 ]
Wu, Wei [1 ]
机构
[1] Fudan Univ, Dept Pharmaceut, Sch Pharm, Shanghai 201203, Peoples R China
[2] Univ Alberta, Dept Agr Food & Nutr Sci, Edmonton, AB T6G 2M7, Canada
[3] Zhejiang Univ, Sch Pharm, Dept Pharmaceut, Hangzhou, Zhejiang, Peoples R China
关键词
oil in water nanoemulsions; food proteins; poorly water-soluble drugs; biocompatibility; in vivo absorption; BOVINE BETA-LACTOGLOBULIN; LIPID-BASED FORMULATIONS; ORAL DELIVERY; LIPOPHILIC DRUGS; RELEASE KINETICS; EMULSIONS; CARRIERS; ALGINATE; NANOPARTICLES; MICROCAPSULES;
D O I
10.2147/IJN.S17282
中图分类号
TB3 [工程材料学];
学科分类号
082905 [生物质能源与材料];
摘要
Nanoemulsions stabilized by traditional emulsifiers raise toxicological concerns for long-term treatment. The present work investigates the potential of food proteins as safer stabilizers for nanoemulsions to deliver hydrophobic drugs. Nanoemulsions stabilized by food proteins (soybean protein isolate, whey protein isolate, beta-lactoglobulin) were prepared by high-pressure homogenization. The toxicity of the nanoemulsions was tested in Caco-2 cells using the 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazoliumbromide viability assay. In vivo absorption in rats was also evaluated. Food protein-stabilized nanoemulsions, with small particle size and good size distribution, exhibited better stability and biocompatibility compared with nanoemulsions stabilized by traditional emulsifiers. Moreover, beta-lactoglobulin had a better emulsifying capacity and biocompatibility than the other two food proteins. The pancreatic degradation of the proteins accelerated drug release. It is concluded that an oil/water nanoemulsion system with good biocompatibility can be prepared by using food proteins as emulsifiers, allowing better and more rapid absorption of lipophilic drugs.
引用
收藏
页码:521 / 533
页数:13
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