title: In vitro and in vivo evaluation of functionalized chitosan-Pluronic micelles loaded with myricetin on glioblastoma cancer.
abstract: This study aimed to develop a novel polymeric carrier based on chitosan-functionalized Pluronic P123/F68 micelles loaded with myricetin (MYR) to improve the therapeutic index of chemotherapy for glioblastoma cancer. Following characterization and assessment of the cellular uptake and antitumor effects of MYR-loaded micelles (MYR-MCs) in vitro, the acute toxicity, blood-brain barrier (BBB) translocation, brain uptake and biodistribution in vivo were assessed. The results demonstrated that MYR-MCs exhibited improved cellular uptake and antitumor activity compared to free MYR in vitro, with a significantly enhanced anticancer effect in vivo following efficient transport across the BBB. However, MYR-MCs did not affect the brain endothelial, barrier function, the liver, heart or kidneys. Furthermore, MYR-MCs altered the expression of apoptotic proteins, such as Bcl-2, BAD and BAX, in mice. In conclusion, MYR-MCs may be considered an effective and promising drug delivery system for glioblastoma treatment.
authors.affiliation: Department of Pharmaceutics, Shanghai Eighth People's Hospital, Jiangsu University, Shanghai, China; Hubei University of Medicine, Shiyan City, Hubei Province, China. Electronic address: wangan139@163.com.
authors.forename: Gang
authors.initials: G
authors.lastname: Wang
authors.affiliation: Department of Pharmaceutics, Shanghai Eighth People's Hospital, Jiangsu University, Shanghai, China.
authors.forename: Jun-Jie
authors.initials: JJ
authors.lastname: Wang
authors.affiliation: Hubei University of Medicine, Shiyan City, Hubei Province, China.
authors.forename: Xiang-Jun
authors.initials: XJ
authors.lastname: Tang
authors.affiliation: Department of Pharmaceutics, Shanghai Eighth People's Hospital, Jiangsu University, Shanghai, China.
authors.forename: Li
authors.initials: L
authors.lastname: Du
authors.affiliation: Department of Pharmaceutics, Shanghai Eighth People's Hospital, Jiangsu University, Shanghai, China.
authors.forename: Fei
authors.initials: F
authors.lastname: Li
mesh_terms: D000818:Animals; D001932:Brain Neoplasms / Q000188:drug therapy*; D045744:Cell Line, Tumor; D048271:Chitosan; D016503:Drug Delivery Systems; D005419:Flavonoids / Q000008:administration & dosage*; D005909:Glioblastoma / Q000188:drug therapy*; D051379:Mice; D008823:Micelles; D020442:Poloxamer; D014018:Tissue Distribution
chemical_list: D005419:Flavonoids; D008823:Micelles; D020442:Poloxamer; C040015:myricetin; D048271:Chitosan
keywords: Anti-cancer; Drug delivery; Glioblastoma; Mixed micelles; Myricetin