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

• 作者: Dongyang Zhao Gang Wang Jin sun Lichun Zhao Mengchi Sun Qikun jiang Yang Wang Yixin Sun Zhonggui He
• 来源期刊: 亚洲药物制剂科学(英文)
• 学科: 医学
• 关键词: Carnitine/organic CATION TRANSPORTER 2(OCTN2) Monocarboxylate TRANSPORTER protein 1(MCT1) Transporter-targeting NANOPARTICLE PRODRUG
• 年，卷（期）: 2020,（2）
• 页码范围: 158-172
• 页数: 15页
• 分类号: R57

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.