Thiol-mediated transportation pathway:an approach for improving tumor penetration of nanomedicines in vivo  

作　　者：Junjie Zhang Weican Sun Xing Wang Senyan Chen Jingying Li Huanghao Yang 

机构地区：[1]New Cornerstone Science Laboratory,Key Laboratory for Analytical Science of Food Safety and Biology(Ministry of Education),College of Chemistry,Fuzhou University,Fuzhou 350116,China [2]Department of Chemistry and College of Biological Science and Engineering,Fuzhou University,Fuzhou 350116,China

出　　处：《Science China Chemistry》2024年第1期383-389,共7页中国科学（化学英文版）

基　　金：supported by the National Key R&D Program of China(2020YFA0210800);the National Natural Science Foundation of China(21974022,22027805);the Major Project of Science and Technology of Fujian Province(2020HZ06006)。

摘　　要：Abnormal tumor microenvironment imposes barriers to tumor penetration of nanomedicine,which remains a major challenge for effective anti-tumor.Herein,we present disulfide-based nanoparticles that actively penetrate deep tumors in vivo through a thiol-mediated transportation pathway.To achieve active tumor accumulation in vivo,disulfide-based nanoparticles are modified with folic acid units(FA-DBNPs).It is gratifying that FA-DBNPs still enter cells via the thiol-mediated pathway,which facilitates transcellular transportation and tumor penetration both in vitro and in vivo.Besides,FA-DBNPs exhibit GSH concentration-dependent depolymerization characterization,indicating that the GSH level in tumor tissues regulates the penetration depth of FA-DBNPs.Benefiting from these advantages,FA-DBNPs showed potent anti-tumor activity in mouse models,leading to the significant regression of tumors.The current study lays a foundation that thiol-mediated transportation is a promising approach in nanomedicine design for solid tumor therapy.

关 键 词：deep penetration thiol-mediated pathway transcellular transportation solid tumor 

分 类 号：TQ460.1[化学工程—制药化工] TB383.1[一般工业技术—材料科学与工程] R91[医药卫生—药学]