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Intestinal OCTN2-and MCT1-targeted drug delivery to improve oral bioavailability

查看全文 作  者:Gang [1]Wang;Lichun [1,2]Zhao;Qikun [3]jiang;Yixin [3]Sun;Dongyang [3]Zhao;Mengchi [3]Sun;Zhonggui [3]He;Jin [3]sun;Yang [2]Wang 高影响力作者 机构地区:[1]Zhuang Yao Medicine Center of Engineering and Technology,Guang Xi University of Chinese Medicine,Nanning 530200,China;[2]School of Pharmacy,Guang Xi University of Chinese Medicine,Nanning 530200,China;[3]School of Pharmacy,Shenyang Pharmaceutical University,Shenyang 110016,China高影响力机构 出  处:《Asian Journal of Pharmaceutical Sciences》索引2020年第15卷第2期,共15页高影响力期刊 基  金:This work was financially supported by the Natural Science Foundation of Guangxi Province(Nos.2018JJB140325,2018JJB140377);Guangxi Scientific and Technology Base and Talents of Project(Nos.2018AD19035);Talents Project for Cultivating High-level Talent Teams in the Qi Huang Project of Guangxi University of Chinese Medicine(2018002);the specific subject of the dominant discipline construction of Chinese Pharmacy of Guangxi University of Chinese Medicine,Guang Xi Key Laboratory of Translational Medicine for Treating High-incidence Infectious Diseases with Integrative Medicine and School research projects(no.B170021,2018MS003);Scientific Research Projects of Guangxi University of Chinese Medicine(B170021,2018MS003). 摘  要:Various drug transporters are widely expressed throughout the intestine and play important roles in absorbing nutrients and drugs,thus providing high quality targets for the design of prodrugs or nanoparticles to facilitate oral drug delivery.In particular,intestinal carnitine/organic cation transporter 2(OCTN2)and mono-carboxylate transporter protein 1(MCT1)possess high transport capacities and complementary distributions.Therefore,we outline recent developments in transporter-targeted oral drug delivery with regard to the OCTN2 and MCT1 proteins in this review.First,basic information of the two transporters is reviewed,including their topological structures,characteristics and functions,expression and key features of their substrates.Furthermore,progress in transporter-targeting prodrugs and nanoparticles to increase oral drug delivery is discussed,including improvements in the oral absorption of anti-inflammatory drugs,antiepileptic drugs and anticancer drugs.Finally,the potential of a dual transporter-targeting strategy is discussed. 关 键 词:Carnitine/organic CATION TRANSPORTER 2(OCTN2) Monocarboxylate TRANSPORTER protein 1(MCT1) Transporter-targeting NANOPARTICLE PRODRUG
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