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

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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-PLGA10K exhibited higher loading capacity for LUS which was 4.33%, and LUT- (or LUS)-loaded mPEG5K-PCL10K 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.

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ACKNOWLEDGEMENTS

This work was supported by the Support Plan of Science and Technology Innovation team in Universities and Colleges in Henan Province of China (No. 14IRTSTHN030), Key Project of Science and Technology Research in Education Department of Henan Province in China (No. 14A150011), and Key Technology Research Program of Henan Province in China (No. 152102210257).

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Authors and Affiliations

  1. Institute of Environmental and Analytical Sciences, College of Chemistry and Chemical Engineering, Henan University, Kaifeng, 475004, People’s Republic of China

    Weixia Qing, Yong Wang, Huan Li, Jinhua Zhu & Xiuhua Liu

  2. Medical College, Henan University, Kaifeng, 475004, People’s Republic of China

    Weixia Qing

  3. Key Laboratory of Natural Medicine and Immune-Engineering of Henan Province, Henan University, Kaifeng, 475004, People’s Republic of China

    Fanyi Ma & Xiuhua Liu

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  1. Weixia Qing
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  2. Yong Wang
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  3. Huan Li
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Correspondence to Xiuhua Liu.

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Qing, W., Wang, Y., Li, H. et al. Preparation and Characterization of Copolymer Micelles for the Solubilization and In Vitro Release of Luteolin and Luteoloside. AAPS PharmSciTech 18, 2095–2101 (2017). https://doi.org/10.1208/s12249-016-0692-y

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