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Formulation, Solubilization, and In Vitro Characterization of Quercetin-Incorporated Mixed Micelles of PEO-PPO-PEO Block Copolymers

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Abstract

Quercetin (QCN) is a plant polyphenol with a variety of medicinal effects. Poor water solubility, on the other hand, restricts its therapeutic effectiveness. The purpose of this study was to develop mixed micellar systems using two biocompatible amphiphilic PEO-PPO-PEO triblock copolymers, Pluronic P123 (EO20-PO70-EO20) and Pluronic F88 (EO104-PO39-EO104), in order to enhance the aqueous solubility and oral bioavailability of QCN drug. The critical micelle concentrations (CMCs) of mixed P123/F88 micellar solutions were investigated using UV–visible spectroscopy with pyrene as a probe. Mixed P123/F88 micelles have low CMCs, indicating that they have a stable micelle structure even when diluted. The solubility of QCN in aqueous mixed P123/F88 micellar solutions at different temperatures was investigated to better understand drug entrapment. The QCN solubility increased with increasing temperature in the mixed P123/F88 micellar system. The QCN-incorporated mixed P123/F88 micelles were prepared using the thin-film hydration method and were well characterized in terms of size and morphology, compatibility, in vitro release and antioxidant profile. In addition, the cell proliferation activity of the mixed micelles was evaluated in the MCF-7 cell line. The QCN-incorporated mixed P123/F88 micelles had a small particle size (< 25 nm) and a negative zeta potential with a spherical shape. The in vitro release behaviour of QCN from a mixed P123/F88 micellar system was slower and more sustained at physiological conditions. The oxidation resistance of QCN-incorporating mixed P123/F88 micelles was shown to be considerably higher than that of pure QCN. An in vitro cell proliferation study revealed that QCN-incorporated mixed micells were effective in inhibiting tumour cell growth. In conclusion, the QCN-incorporated mixed P123/F88 micelle may be a promising approach to increase QCN oral bioavailability, antioxidant activity, and cell viability.

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Acknowledgements

The corresponding author acknowledged Center of Excellence in Polymers (CoEP), Applied Chemistry Department, Faculty of Technology and Engineering for necessary lab facilities.

Funding

This work was supported by the UGC-DAE Research Project (CRS-M-205), Bhabha Atomic Research Centre, Mumbai, Maharashtra, India.

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Authors and Affiliations

  1. Applied Chemistry Department, Faculty of Technology and Engineering, The Maharaja Sayajirao University of Baroda, Vadodara, 390001, Gujarat, India

    Hemil S. Patel, Sofiya J. Shaikh & Rakesh K. Sharma

  2. Solid State Physics Division, Bhabha Atomic Research Centre (BARC), Mumbai, Maharashtra, India

    Debes Ray & Vinod K. Aswal

  3. Department of Cell Biology, School of Biological Sciences and Biotechnology, Indian Institute of Advanced Research, Gandhinagar, Gujarat, India

    Foram Vaidya

  4. Amity Institute of Biotechnology, Amity University, Gurgaon, Haryana, India

    Chandramani Pathak

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  1. Hemil S. Patel
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  3. Debes Ray
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  4. Vinod K. Aswal
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Contributions

Hemil S Patel, Sofiya J Shaikhand Rakesh K Sharma designed the study, analysed the data, and wrote the final manuscript. Debes Ray andVinod K Aswal contributed to the SANS measurments. Foram Vaidya and Chandramani Pathak carried out the molecular biology studies. All authors read and approved the final manuscript.

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Correspondence to Rakesh K. Sharma.

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Patel, H.S., Shaikh, S.J., Ray, D. et al. Formulation, Solubilization, and In Vitro Characterization of Quercetin-Incorporated Mixed Micelles of PEO-PPO-PEO Block Copolymers. Appl Biochem Biotechnol 194, 445–463 (2022). https://doi.org/10.1007/s12010-021-03691-w

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