title: Formulation and in vitro evaluation of quercetin loaded polymeric micelles composed of pluronic P123 and D-a-tocopheryl polyethylene glycol succinate.
abstract: The objective of this study was to develop a polymeric delivery system to improve the solubility and biological activity of Quercetin (QT). QT loaded mixed micelles, composed of Pluronic P123 (P123) and D-a-tocopheryl polyethylene glycol succinate (TPGS) with proportion of 7:3 (QT-P/T), were prepared by thin-film hydration method. The average size of the mixed micelles was 18.43 nm, and the encapsulating efficiency for QT was 88.94 +/- 3.71%, drug-loading was 10.59 +/- 0.38%. The solubility of QT in QT-P/T was 5.56 mg/mL, which was about 2738-fold that of crude QT in water. Compared with the QT propylene glycol solution, the in vitro release of QT from QT-P/T presented the sustained-release property. The in vitro cytotoxicity assay showed that the IC50 values on MCF-7 cells for QT-P/T and QT loaded P123 micelles (QT-P123) were 7.13 microg/mL and 10.73 microg/mL, respectively, while 7.23 microg/mL and 14.47 microg/mL on MCF-7/ADR cells. From the results, it can be concluded that, P123/TPGS mixed micelles may serve as a pharmaceutical nano carrier with improved solubility and biological activity for QT.
authors.affiliation: Department of Pharmaceutics, College of Pharmacy, Shandong University, Jinan 250012, China.
authors.forename: Liyan
authors.initials: L
authors.lastname: Zhao
authors.forename: Yikang
authors.initials: Y
authors.lastname: Shi
authors.forename: Shaohua
authors.initials: S
authors.lastname: Zou
authors.forename: Min
authors.initials: M
authors.lastname: Sun
authors.forename: Lingbing
authors.initials: L
authors.lastname: Lil
authors.forename: Guangxi
authors.initials: G
authors.lastname: Zhail
mesh_terms: D000970:Antineoplastic Agents / Q000494:pharmacology*; D001943:Breast Neoplasms / Q000188:drug therapy; D045744:Cell Line, Tumor; D002470:Cell Survival / Q000187:drug effects; D002626:Chemistry, Pharmaceutical; D016503:Drug Delivery Systems; D005260:Female; D006801:Humans; D020128:Inhibitory Concentration 50; D008823:Micelles; D046529:Microscopy, Electron, Transmission; D015394:Molecular Structure; D010316:Particle Size; D011060:Poloxalene / Q000737:chemistry; D011095:Polyethylenes / Q000737:chemistry; D011794:Quercetin / Q000494:pharmacology*; D013386:Succinates / Q000737:chemistry; D024505:Tocopherols / Q000494:pharmacology*
chemical_list: D000970:Antineoplastic Agents; D008823:Micelles; D011095:Polyethylenes; D013386:Succinates; C443715:poly(ethylene succinate); C464484:pluronic block copolymer P123; D011060:Poloxalene; D011794:Quercetin; D024505:Tocopherols