Premium
Functionalized Nanoscale Micelles with Brain Targeting Ability and Intercellular Microenvironment Biosensitivity for Anti‐Intracranial Infection Applications
Author(s) -
Shao Kun,
Zhang Yu,
Ding Ning,
Huang Shixian,
Wu Jiqin,
Li Jianfeng,
Yang Chunfu,
Leng Qibin,
Ye Liya,
Lou Jinning,
Zhu Liping,
Jiang Chen
Publication year - 2015
Publication title -
advanced healthcare materials
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 2.288
H-Index - 90
eISSN - 2192-2659
pISSN - 2192-2640
DOI - 10.1002/adhm.201400214
Subject(s) - nanocarriers , blood–brain barrier , micelle , drug delivery , glut1 , targeted drug delivery , drug , materials science , chemistry , biophysics , nanotechnology , pharmacology , glucose transporter , medicine , biology , central nervous system , aqueous solution , insulin
Due to complication factors such as blood‐brain barrier (BBB), integrating high efficiency of brain target ability with specific cargo releasing into one nanocarrier seems more important. A brain targeting nanoscale system is developed using dehydroascorbic acid (DHA) as targeting moiety. DHA has high affinity with GLUT1 on BBB. More importantly, the GLUT1 transportation of DHA represents a “one‐way” accumulative priority from blood into brain. The artificial micelles are fabricated by a disulfide linkage, forming a bio‐responsive inner barrier, which can maintain micelles highly stable in circulation and shield the leakage of entrapped drug before reaching the targeting cells. The designed micelles can cross BBB and be further internalized by brain cells. Once within the cells, the drug release can be triggered by high intracellular level of glutathione (GSH). Itraconazole (ITZ) is selected as the model drug because of its poor brain permeability and low stability in blood. It demonstrates that the functionalized nanoscale micelles can achieve highly effective direct drug delivery to targeting site. Based on the markedly increased stability in blood circulation and improved brain delivery efficiency of ITZ, DHA‐modified micelles show highly effective in anti‐intracranial infection. Therefore, this smart nanodevice shows a promising application for the treatment of brain diseases.