Department of Pharmaceutics, School of Pharmacy, Fudan University, Shanghai, People's Republic of China.
Int J Nanomedicine. 2011;6:521-33. doi: 10.2147/IJN.S17282. Epub 2011 Mar 11.
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, β-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, β-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.
由传统乳化剂稳定的纳米乳剂在长期治疗中引起了毒理学问题。本工作研究了将食品蛋白质用作更安全的纳米乳剂稳定剂以递送疏水性药物的可能性。通过高压均质法制备了由食品蛋白质(大豆蛋白分离物、乳清蛋白分离物、β-乳球蛋白)稳定的纳米乳剂。通过 3-(4,5-二甲基噻唑-2-基)-2,5-二苯基四氮唑溴化物活力测定法在 Caco-2 细胞中测试了纳米乳剂的毒性。还评估了在大鼠体内的吸收。与由传统乳化剂稳定的纳米乳剂相比,具有小粒径和良好粒径分布的食品蛋白稳定的纳米乳剂表现出更好的稳定性和生物相容性。此外,β-乳球蛋白比其他两种食品蛋白质具有更好的乳化能力和生物相容性。蛋白质的胰腺降解加速了药物释放。结论是,可以使用食品蛋白质作为乳化剂制备具有良好生物相容性的油/水纳米乳剂体系,从而使亲脂性药物更好、更快地吸收。