Oral delivery of polyester nanoparticles for brain-targeting: Challenges and opportunities

作     者：Ping Wang Yue Wang Ping Li Chen Chen Siman Ma Linxuan Zhao Haibing He Tian Yin Yu Zhang Xing Tang Jingxin Gou Ping Wang;Yue Wang;Ping Li;Chen Chen;Siman Ma;Linxuan Zhao;Haibing He;Tian Yin;Yu Zhang;Xing Tang;Jingxin Gou

作者机构：Department of PharmaceuticsShenyang Pharmaceutical UniversityShenyang 110016China School of PharmacyJilin UniversityChangchun 130021China School of Functional Food and WineShenyang Pharmaceutical UniversityShenyang 110016China 

出 版 物：《Chinese Chemical Letters》 (中国化学快报（英文版）)

年 卷 期：2023年第34卷第4期

页      面：99-109页

核心收录：

学科分类：1002[医学-临床医学] 0703[理学-化学] 100204[医学-神经病学] 10[医学] 

基　　金：supported by the National Key R&D Program of China (No. 2020YFE0201700) the National Mega-project for Innovative Drugs (No. 2019ZX09721001) the National Natural Science Foundation of China (No. 81673378) the Liaoning Revitalization Talents Program (No. XLYC1908031) the Project of Liaoning Provincial Department of Education (No. 2019LQN07) the PhD Research Startup Foundation of Liaoning Province (No. 2020-BS-128)。 

主　　题：Polyester nanoparticles Oral brain drugs Brain-targeted delivery Physiological barrier Absorption enhancement 

摘      要：Efficient oral delivery of drugs treating brain diseases has long been a challenging topic faced by the drug delivery community. Fortunately, polyester nanoparticles offer certain solutions to this problem. This review article firstly describes the main obstacles faced by oral administered brain targeting, including:(1)instability in the gastrointestinal tract;(2) poor penetration of the intestinal mucosa and epithelium;(3)blood clearance;and(4) restriction by the BBB. Then the key factors influencing brain-targeting efficiency of orally administered polyester nanoparticles are also discussed, such as size, shape and surface properties. Finally, recent brain-targeting delivery strategies using oral polyester nanoparticles as carriers and their effects on brain drugs transport are reviewed, and the delivery ‘as a whole’ strategy of polyester nanoparticles will provide new insight for oral brain-targeting delivery. And by combination of multiple strategies, both the stability and permeability of polyester nanoparticles can be greatly improved for oral brain drug delivery.