國家衛生研究院 NHRI:Item 3990099045/11744
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    题名: Phase-changeable nanoemulsions for oral delivery of a therapeutic peptide: Toward targeting the pancreas for antidiabetic treatments using lymphatic transport
    作者: Lin, PY;Chen, KH;Miao, YB;Chen, HL;Lin, KJ;Chen, CT;Yeh, CN;Chang, Y;Sung, HW
    贡献者: Institute of Biotechnology and Pharmaceutical Research
    摘要: The oral absorption of a therapeutic peptide (such as exenatide; EXT) that can improve glycemic control in the treatment of type 2 diabetes is limited by multiple barriers of the intestinal epithelium. This work presents an oil-structured nanoemulsion system that consists of a phase-changeable fatty acid that allows EXT (EXT@PC/NEMs) to be delivered orally and absorbed efficiently in the small intestine. To construct an appropriate vehicle to encapsulate EXT, an oil-in-water single emulsion is generated at 37 °C, which is well above the melting point of the fatty acid but below the denaturation temperature of the peptide drug. The as-prepared EXT@PC/NEMs are physically stable when stored at 4 °C, as they form a solid core, which prevents drug leakage. Upon their oral delivery at body temperature, the deformable liquid EXT@PC/NEMs may undergo effective cellular uptake, enhancing their permeability across the intestinal epithelium. The orally administered PC/NEMs significantly improve the bioavailability of EXT via intestinal lymphatic transport, ultimately accumulating in the pancreas, suggesting the possibility of orally delivering labile peptide drugs. The delivered EXT may act on pancreatic β- and α-cells to stimulate insulin release and suppress glucagon secretion, respectively, reducing the blood glucose level, eventually having antidiabetic effects.
    日期: 2019-03-28
    關聯: Advanced Functional Materials. 2019 Mar 28;29(13): Article number 1809015.
    Link to: http://dx.doi.org/10.1002/adfm.201809015
    JIF/Ranking 2023: http://gateway.webofknowledge.com/gateway/Gateway.cgi?GWVersion=2&SrcAuth=NHRI&SrcApp=NHRI_IR&KeyISSN=1616-301X&DestApp=IC2JCR
    Cited Times(WOS): https://www.webofscience.com/wos/woscc/full-record/WOS:000463732400024
    Cited Times(Scopus): https://www.scopus.com/inward/record.url?partnerID=HzOxMe3b&scp=85061257443
    显示于类别:[陳炯東] 期刊論文

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