title: Preparation and Characterization of Copolymer Micelles for the Solubilization and In Vitro Release of Luteolin and Luteoloside.
abstract: Luteolin (LUT) and luteoloside (LUS) belong to flavonoids with high anticancer potential and were loaded into biodegradable diblock copolymer micelles of methoxy polyethylene glycol-polycaprolactone (mPEG5K-PCL10K), methoxy polyethylene glycol-polylactide-co-glycolide (mPEG5K-PLGA10K), and methoxy polyethylene glycol-polylactide (mPEG5K-PDLLA10K) by a self-assembly method, creating water-soluble LUT and LUS copolymer micelles, respectively. The solubilization formulations of the copolymer micelles were optimized with response surface methodology (RSM). The obtained drug micelles are torispherical under transmission electron microscope (TEM) with an average diameter of about 70 nm. The mPEG5K-PLGA10Kexhibited higher loading capacity for LUS which was 4.33%, and LUT- (or LUS)-loaded mPEG5K-PCL10Kexhibited a better stability and encapsulation efficiency which was 65.1 and 55.8%, respectively. The in vitro drug release study showed above 47% of LUT was released from micelles at pH 7.4 PBS; however, no more than 35% of LUT was released at pH 6.4 PBS within 24 h. Meanwhile, no more than 30% of LUS was released from micelles whether at pH 6.4 or 7.4 PBS solution within 24 h.
authors.affiliation: Institute of Environmental and Analytical Sciences, College of Chemistry and Chemical Engineering, Henan University, Kaifeng, 475004, People's Republic of China.|Medical College, Henan University, Kaifeng, 475004, People's Republic of China.
authors.forename: Weixia
authors.initials: W
authors.lastname: Qing
authors.affiliation: Institute of Environmental and Analytical Sciences, College of Chemistry and Chemical Engineering, Henan University, Kaifeng, 475004, People's Republic of China.
authors.forename: Yong
authors.initials: Y
authors.lastname: Wang
authors.affiliation: Institute of Environmental and Analytical Sciences, College of Chemistry and Chemical Engineering, Henan University, Kaifeng, 475004, People's Republic of China.
authors.forename: Huan
authors.initials: H
authors.lastname: Li
authors.affiliation: Key Laboratory of Natural Medicine and Immune-Engineering of Henan Province, Henan University, Kaifeng, 475004, People's Republic of China.
authors.forename: Fanyi
authors.initials: F
authors.lastname: Ma
authors.affiliation: Institute of Environmental and Analytical Sciences, College of Chemistry and Chemical Engineering, Henan University, Kaifeng, 475004, People's Republic of China.
authors.forename: Jinhua
authors.initials: J
authors.lastname: Zhu
authors.affiliation: Institute of Environmental and Analytical Sciences, College of Chemistry and Chemical Engineering, Henan University, Kaifeng, 475004, People's Republic of China. ll514527@163.com.|Key Laboratory of Natural Medicine and Immune-Engineering of Henan Province, Henan University, Kaifeng, 475004, People's Republic of China. ll514527@163.com.
authors.forename: Xiuhua
authors.initials: X
authors.lastname: Liu
mesh_terms: D004337:Drug Carriers / Q000138:chemical synthesis / Q000493:pharmacokinetics; D065546:Drug Liberation; D004365:Drugs, Chinese Herbal / Q000138:chemical synthesis / Q000493:pharmacokinetics; D005960:Glucosides / Q000138:chemical synthesis* / Q000493:pharmacokinetics; D047311:Luteolin / Q000138:chemical synthesis* / Q000493:pharmacokinetics; D008823:Micelles; D011108:Polymers / Q000138:chemical synthesis* / Q000493:pharmacokinetics
chemical_list: D004337:Drug Carriers; D004365:Drugs, Chinese Herbal; D005960:Glucosides; D008823:Micelles; D011108:Polymers; C066408:luteolin-7-glucoside; D047311:Luteolin
keywords: diblock copolymer micelles; luteolin; luteoloside; release