Preparation and Characterization of Copolymer Micelles for the Solubilization and In Vitro Release of Luteolin and Luteoloside

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 (mPEG 5K -PCL 10K ), methoxy polyethylene glycol-polylactide-co-glycolide (mPEG 5K -PLGA 10K ), and m...

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Published in:AAPS PharmSciTech 2017-08, Vol.18 (6), p.2095-2101
Main Authors: Qing, Weixia, Wang, Yong, Li, Huan, Ma, Fanyi, Zhu, Jinhua, Liu, Xiuhua
Format: Article
Language:English
Subjects:
Biochemistry
Biomedical and Life Sciences
Biomedicine
Biotechnology
Drug Carriers - chemical synthesis
Drug Carriers - pharmacokinetics
Drug Liberation
Drugs, Chinese Herbal - chemical synthesis
Drugs, Chinese Herbal - pharmacokinetics
Glucosides - chemical synthesis
Glucosides - pharmacokinetics
Luteolin - chemical synthesis
Luteolin - pharmacokinetics
Micelles
Pharmacology/Toxicology
Pharmacy
Polymers - chemical synthesis
Polymers - pharmacokinetics
Research Article
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Summary: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 (mPEG 5K -PCL 10K ), methoxy polyethylene glycol-polylactide-co-glycolide (mPEG 5K -PLGA 10K ), and methoxy polyethylene glycol-polylactide (mPEG 5K -PDLLA 10K ) 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 mPEG 5K -PLGA 10K exhibited higher loading capacity for LUS which was 4.33%, and LUT- (or LUS)-loaded mPEG 5K -PCL 10K exhibited 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.
ISSN:1530-9932
1530-9932
DOI:10.1208/s12249-016-0692-y