Literature DB >> 34611857

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

Hemil S Patel1, Sofiya J Shaikh1, Debes Ray2, Vinod K Aswal2, Foram Vaidya3, Chandramani Pathak4, Rakesh K Sharma5.   

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.
© 2021. The Author(s), under exclusive licence to Springer Science+Business Media, LLC, part of Springer Nature.

Entities:  

Keywords:  In vitro cell proliferation activity; In vitro release; Mixed Pluronic micelles; Quercetin; Solubilization

Mesh:

Substances:

Year:  2021        PMID: 34611857     DOI: 10.1007/s12010-021-03691-w

Source DB:  PubMed          Journal:  Appl Biochem Biotechnol        ISSN: 0273-2289            Impact factor:   2.926


  33 in total

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Journal:  Wiley Interdiscip Rev Nanomed Nanobiotechnol       Date:  2015-02-13

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Journal:  Free Radic Res       Date:  2001-06

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Review 7.  Quercetin: a potential drug to reverse multidrug resistance.

Authors:  Chen Chen; Jane Zhou; Chunyan Ji
Journal:  Life Sci       Date:  2010-07-15       Impact factor: 5.037

8.  Study of freeze-dried quercetin-cyclodextrin binary systems by DSC, FT-IR, X-ray diffraction and SEM analysis.

Authors:  Tayade Pralhad; Kale Rajendrakumar
Journal:  J Pharm Biomed Anal       Date:  2004-02-04       Impact factor: 3.935

9.  Carotenoid content of fruits and vegetables: an evaluation of analytic data.

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Journal:  J Am Diet Assoc       Date:  1993-03

10.  The relative antioxidant activities of plant-derived polyphenolic flavonoids.

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Journal:  Free Radic Res       Date:  1995-04
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  1 in total

1.  TiO2 Nanoparticles Dispersion in Block-Copolymer Aqueous Solutions: Nanoarchitectonics for Self-Assembly and Aggregation.

Authors:  Valeria Conti Nibali; Giovanna D'Angelo; Antonella Arena; Carmine Ciofi; Graziella Scandurra; Caterina Branca
Journal:  J Funct Biomater       Date:  2022-04-09
  1 in total

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