Maximizing the Oral Bioavailability of Poorly Water-Soluble Drugs Using Novel Oil-Like Materials in Lipid-Based Formulations

被引:8
|
作者
Abbasi, Saed [1 ]
Higashino, Haruki [2 ]
Sato, Yusuke [3 ]
Minami, Keiko [2 ]
Kataoka, Makoto [2 ]
Yamashita, Shinji [2 ]
Harashima, Hideyoshi [3 ]
机构
[1] Kawasaki Inst Ind Promot, Innovat Ctr NanoMed, Kawasaki, Kanagawa 2100821, Japan
[2] Setsunan Univ, Fac Pharmaceut Sci, Osaka 5730101, Japan
[3] Hokkaido Univ, Fac Pharmaceut Sci, Sapporo, Hokkaido 0600812, Japan
基金
日本学术振兴会;
关键词
water insoluble drugs; pi-pi stacking; oral delivery; drug absorption; pharmaceutical solubilizer; IN-VIVO EVALUATION; DELIVERY SYSTEM; PRECIPITATION INHIBITORS; VITRO; ABSORPTION; INTESTINE; DIGESTION; LIPOLYSIS; SMEDDS;
D O I
10.1021/acs.molpharmaceut.1c00197
中图分类号
R-3 [医学研究方法]; R3 [基础医学];
学科分类号
1001 ;
摘要
Lipid-based formulations, such as self-microemulsifying drug-delivery systems (SMEDDSs), are promising tools for the oral delivery of poorly water-soluble drugs. However, failure to maintain adequate aqueous solubility after coming into contact with gastrointestinal fluids is a major drawback. In this study, we examined the use of a novel cinnamic acid-derived oil-like material (CAOM) that binds drugs with a high affinity through pi-pi stacking and hydrophobic interactions, as an oil core in a SMEDDS for the oral delivery of fenofibrate in rats. The use of the CAOM in the SMEDDS resulted in an unprecedented enhancement in fenofibrate bioavailability, which exceeded the bioavailability values obtained using SMEDDSs based on corn oil, a conventional triglyceride oil, or Labrasol, an enhancer of intestinal permeation. Further characterization revealed that the CAOM SMEDDS does not alter the intestinal permeability and has no inhibitory activity on Pglycoprotein-mediated drug efflux. The results reported herein demonstrate the strong potential of CAOM formulations as new solubilizers for the efficient and safe oral delivery of drugs that have limited water solubility.
引用
收藏
页码:3281 / 3289
页数:9
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