title: Development and Evaluation of a Novel Drug Delivery: Pluronics/SDS Mixed Micelle Loaded With Myricetin In Vitro and In Vivo.
abstract: This study is to prepare and evaluate Pluronics-modified mixed micelle (MM) to deliver polyphenolic myricetin (MYR) across the blood-brain barrier. MYR has been proven to be an effective anticancer agent against glioblastoma cells in our previous studies. However, the poor solubility of MYR limits its access to the brain. In this study, the feasibility of preparing lipid-based MM that combined sodium dodecyl sulphate (SDS) with Pluronic F68 (F68) and Labrasol was investigated. Furthermore, the nonionic surfactant coating technology for the protection of MYR against oxidation, and its attainment in oral bioavailability, was examined. On account of the altered biomaterial properties of F68/SDS-modified lipid-based micelles, myricetin-loaded mixed micelles (MYR-MMs) were prepared by solvent-evaporation method to self-assembly into MMs. The average size of MYR-MMs was 96.3 nm, with negatively charged potential and spherical in shape. The drug loading of MYR-MMs was high with the increased grafting ratio, the more prolonged drug release profile, and more effective killing glioblastoma cells in vitro. Moreover, MYR-MMs showed a higher preference for the brain than free MYR alone, suggesting the novel MMs loaded with MYR could promote absorption and increase relative bioavailability. Taken together, the F68/SDS-modified and Labrasol-modified lipid-based micelles may provide a promising method to deliver polyphenolic compounds across the brain to treat brain tumor.
authors.affiliation: Department of Pharmaceutics, Shanghai Eighth People's Hospital, Jiangsu University, Shanghai 200235, 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 200235, China; College of Pharmacy, Hubei University of Medicine, Shiyan City, Hubei 442000, China.
authors.forename: Jun-Jie
authors.initials: JJ
authors.lastname: Wang
authors.affiliation: Department of Pharmaceutics, Shanghai Eighth People's Hospital, Jiangsu University, Shanghai 200235, China.
authors.forename: Fei
authors.initials: F
authors.lastname: Li
authors.affiliation: Department of Health Technology and Informatics, The Hong Kong Polytechnic University, Hong Kong SAR, China.
authors.forename: Shing-Shun Tony
authors.initials: SS
authors.lastname: To
mesh_terms: D000818:Animals; D000970:Antineoplastic Agents / Q000008:administration & dosage* / Q000493:pharmacokinetics / Q000494:pharmacology; D001921:Brain / Q000187:drug effects / Q000378:metabolism; D001932:Brain Neoplasms / Q000188:drug therapy / Q000378:metabolism; D045744:Cell Line, Tumor; D004337:Drug Carriers / Q000737:chemistry*; D016503:Drug Delivery Systems; D005419:Flavonoids / Q000008:administration & dosage* / Q000493:pharmacokinetics / Q000494:pharmacology; D005909:Glioblastoma / Q000188:drug therapy / Q000378:metabolism; D006801:Humans; D008823:Micelles; D020442:Poloxamer / Q000737:chemistry*; D017207:Rats, Sprague-Dawley; D012967:Sodium Dodecyl Sulfate / Q000737:chemistry*
chemical_list: D000970:Antineoplastic Agents; D004337:Drug Carriers; D005419:Flavonoids; D008823:Micelles; D020442:Poloxamer; D012967:Sodium Dodecyl Sulfate; C040015:myricetin
keywords: F68/SDS; Labrasol; bioavailability; brain tumor; lipid-based micelles; myricetin (MYR)