期刊
MOLECULAR PHARMACEUTICS
卷 18, 期 9, 页码 3281-3289出版社
AMER CHEMICAL SOC
DOI: 10.1021/acs.molpharmaceut.1c00197
关键词
water insoluble drugs; pi-pi stacking; oral delivery; drug absorption; pharmaceutical solubilizer
资金
- Special Education and Research Expenses from the Japan Ministry of Education, Culture, Sports, Science and Technology (MEXT)
- Japan Society for the Promotion of Science (JSPS) [P19116]
The study investigated the use of a novel cinnamic acid-derived oil-like material (CAOM) in a SMEDDS for the oral delivery of fenofibrate. The results showed that the CAOM SMEDDS significantly improved fenofibrate bioavailability compared to traditional oils or enhancers. This suggests a strong potential for CAOM formulations in enhancing oral delivery of drugs with limited water solubility.
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.
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