DOI: 10.1002/ame2.12468
Endogenous Fe2+-triggered self-targeting nanomicelles for self-amplifying intracellular oxidative stress
Zhongxiong Fan1
Guoyu Xia1
Qingluo Wang1
Shiduan Chen2
Jianmin Li1
Zhenqing Hou3
Ziwen Jiang4
Juan Feng5
1.School of Pharmaceutical Sciences and Institute of Materia Medica,Xinjiang University,Urumqi,China2.College of Materials,Xiamen University,Xiamen,China3.School of Pharmaceutical Sciences and Institute of Materia Medica,Xinjiang University,Urumqi,China;College of Materials,Xiamen University,Xiamen,China4.Department of Gynecology,Beijing Obstetrics and Gynecology Hospital,Capital Medical University,Beijing Maternal and Child Health Care Hospital,Beijing,China5.Department of Hematology,The First Affiliated Hospital of Xiamen University and Institute of Hematology,School of Medicine,Xiamen University,Xiamen,China
摘要：Background:Artesunate(ASA)acts as an·O₂-source through the breakdown of en-doperoxide bridges catalyzed by Fe 2+,yet its efficacy in ASA-based nanodrugs is lim-ited by poor intracellular delivery.
Methods:ASA-hyaluronic acid(HA)conjugates were formed from hydrophobic ASA and hydrophilic HA by an esterification reaction first,and then self-targeting nanomi-celles(NM)were developed using the fact that the amphiphilic conjugates of ASA and HA are capable of self-assembling in aqueous environments.
Results:These ASA-HA NMs utilize CD44 receptor-mediated transcytosis to greatly enhance uptake by breast cancer cells.Subsequently,endogenous Fe 2+from the tumor catalyzes the released ASA to produce highly toxic·O₂-radicals to kill tumor cells,although sustained tumor growth inhibition can be achieved via in vivo experiments.
Conclusions:Self-targeting NMs represent a promising strategy for enhancing ASA-based treatments,leveraging clinically approved drugs to expedite drug development and clinical research in oncology.
机标关键词：stressendogenousfe2+-triggeredintracellularnanomicellesoxidativeself-amplifyingself-targeting
论文发表日期：2025-02-28
在线出版日期：2025-08-15（本平台首次上网日期，不代表文献的发表时间）
页数：15( 307-321 )
英文信息