title: Preparation, optimization, characterization and cytotoxicity in vitro of Baicalin-loaded mixed micelles.
abstract: The aim of this study was to develop a Baicalin (BC)-loaded mixed micelle delivery system (BC-ST-P123-MMs) with sodium taurocholate (ST) and pluronic P123 block copolymer (P123) as carrier materials to improve the solubility of BC, a poorly soluble drug. In this study, the mixed micelle system was prepared using the method of thin-film dispersion and then optimized by the homogeneous design-response surface methodology with the entrapment efficiency and drug loading as indexes. The average size and the zeta potential of the BC-ST-P123-MMs were 15.60 nm and -5.26 mV, respectively. Drug loading (DL, 16.94%) and entrapment efficiency (EE, 90.67%) contributed to high solubility (10.20 mg/mL) of BC in water. The optimized BC-ST-P123-MMs appeared spherical with obvious core-shell structure and well dispersed without aggregation and adhesion under TEM. In addition, DSC result indicated that BC had been wrapped in BC-ST-P123-MMs and crystalline state of BC was changed. The release result in vitro showed that BC-ST-P123-MMs presented sustained release behavior compared to control group. The IC50 value of BC-ST-P123-MMs (46.18 μg/mL) was lower than that of BC solution (67.14 μg/mL) on Hep G2 cell lines. Cellular uptake tests illustrated that the ST-P123-MMs system as carrier could significantly enhance the uptake of drugs by tumor cells. The results demonstrated that the BC-loaded mixed micelles could improve solubility of BC and exhibited great potential for delivering drug into cancer cells.
authors.affiliation: Department of Pharmaceutics, College of Pharmacy, Shandong University, Jinan 250012, China.
authors.forename: Haiqun
authors.initials: H
authors.lastname: Zhang
authors.affiliation: Department of Pharmaceutics, College of Pharmacy, Shandong University, Jinan 250012, China.
authors.forename: Lili
authors.initials: L
authors.lastname: Zhao
authors.affiliation: College of Medicine and Nursing, Dezhou University, Dezhou 253023, China.
authors.forename: Lianjun
authors.initials: L
authors.lastname: Chu
authors.affiliation: College of Chemistry, Shandong University, Jinan 250100, China.
authors.forename: Xu
authors.initials: X
authors.lastname: Han
authors.affiliation: Department of Pharmaceutics, College of Pharmacy, Shandong University, Jinan 250012, China. Electronic address: professorgxzhai@126.com.
authors.forename: Guangxi
authors.initials: G
authors.lastname: Zhai
mesh_terms: D000970:Antineoplastic Agents / Q000008:administration & dosage* / Q000493:pharmacokinetics / Q000494:pharmacology; D002470:Cell Survival / Q000187:drug effects; D003692:Delayed-Action Preparations / Q000737:chemistry*; D005419:Flavonoids / Q000008:administration & dosage* / Q000493:pharmacokinetics / Q000494:pharmacology; D056945:Hep G2 Cells; D006801:Humans; D008823:Micelles; D009369:Neoplasms / Q000188:drug therapy; D011060:Poloxalene / Q000737:chemistry*; D013656:Taurocholic Acid / Q000737:chemistry*
chemical_list: D000970:Antineoplastic Agents; D003692:Delayed-Action Preparations; D005419:Flavonoids; D008823:Micelles; C464484:pluronic block copolymer P123; C038044:baicalin; D013656:Taurocholic Acid; D011060:Poloxalene
keywords: Baicalin; Entrapment efficacy; Mixed micelles; Pluronic P123 copolymer; Sodium taurocholate