期刊
DRUG DELIVERY
卷 23, 期 4, 页码 1469-1475出版社
TAYLOR & FRANCIS LTD
DOI: 10.3109/10717544.2016.1153744
关键词
Drug delivery; nanoparticles; nanostructured lipid carriers; oral bioavailability; sirolimus
资金
- Shanghai Commission of Science and Technology [14JC1490300]
- National Key Basic Research Program [2015CB931800]
The main purpose of this study was to improve the oral bioavailability of sirolimus (SRL), a poorly water-soluble immunosuppressant, by encapsulating into lipids-based nanostructured lipid carriers (NLCs). SRL-loaded NLCs (SRL-NLCs) were prepared by a high-pressure homogenization method with glycerol distearates (PRECIROL ATO-5) as the solid lipid, oleic acid as the liquid lipids, and Tween 80 as the emulsifier. The SRL-NLCs prepared under optimum conditions was spherical in shape with a mean particle size of about 108.3 nm and an entrapment efficiency of 99.81%. In vitro release of SRL-NLCs was very slow, about 2.15% at 12 h, while in vitro lipolysis test showed fast digestion of the NLCs within 1 h. Relative oral bioavailability of SRL-NLCs in Beagle dogs was 1.81-folds that of the commercial nanocrystalline sirolimus tablets Rapamune (R). In conclusion, the NLCs show potential to improve the oral bioavailability of SRL.
作者
我是这篇论文的作者
点击您的名字以认领此论文并将其添加到您的个人资料中。
推荐
暂无数据