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Quercetin-PVP K25 solid dispersions

Preparation, thermal characterization and antioxidant activity

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Abstract

Quercetin is a flavonoid very well studied and has already entered clinical trials emerging as prospective anticancer drug candidate. In addition, quercetin has being reported to its free-radical scavenging activity and suggests potential uses for the prevention and treatment of pathologies as atherosclerosis, chronic inflammation, and others. However, quercetin is sparingly soluble in water, which may be responsible for its limited absorption upon oral administration. The solid dispersion of quercetin with polyvinylpyrrolidone Kollidon® 25 (PVP K25) suggests an interesting way to increase quercetin solubility, antioxidant activity, and consequently bioavailability. Then, the purpose of this study was to prepare solid dispersions of quercetin with PVP K25 and evaluate their thermal characterization, antioxidant activity and quercetin improvement solubility. For this purpose, quercetin-PVP K25 solutions were dried and quercetin-PVP K25 solids were obtained. The formation of quercetin-PVP K25 solid dispersion was evaluated by solubility studies, powder X-ray diffraction (XRD), fourier transform infrared spectroscopy (FT-IR), differential scanning calorimetry (DSC), thermogravimetry (TG), and antioxidant activity. It was observed that PVP K25 was able to provide quercetin clear aqueous solutions and that quercetin solubility was increased in a PVP K25 concentration dependent manner, improving solubility even 436-fold the pure quercetin. The results obtained with XRD, FT-IR, DSC, and TG demonstrated possible quercetin-PVP K25 solid dispersion formation. Besides, the antioxidant activity of the quercetin-PVP K25 solid dispersions dissolved in aqueous solution and pure quercetin dissolved in methanol showed IC50 value of 0.61 ± 0.03 and 1.00 ± 0.02 μg/mL, respectively, demonstrating that the solid dispersions presented a significant increase in antioxidant activity (P < 0.05). Putting results together, it was possible to conclude there was the formation of quercetin-PVP K25 solid dispersion.

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Acknowledgements

The authors are grateful to APIS FLORA (Apis Flora Indl. Coml. Ltda.), CAPES (Coordenação de Aperfeiçoamento de Pessoal de Nível Superior), CNPQ-Brasil (Conselho Nacional de Desenvolvimento Científico e Tecnológico) and FAPESP (Fundação de Amparo à Pesquisa do Estado de São Paulo).

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Authors and Affiliations

  1. Apis Flora Industrial e Comercial LTDA, Rua Triunfo, Ribeirão Prêto-SP, 945 CEP 14020-670, Brazil

    Ana Rita de Mello Costa, Flávia Silva Marquiafável, Mirela Mara de Oliveira Lima Leite Vaz, Bruno Alves Rocha, Paula Carolina Pires Bueno & Andresa Ap. Berreta-Silva

  2. Instituto de Química UNESP/Araraquara—UNESP, Araraquara-SP, Brazil

    Pedro Luiz M. Amaral & Hernane da Silva Barud

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  1. Ana Rita de Mello Costa
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  2. Flávia Silva Marquiafável
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  3. Mirela Mara de Oliveira Lima Leite Vaz
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Correspondence to Ana Rita de Mello Costa.

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de Mello Costa, A.R., Marquiafável, F.S., de Oliveira Lima Leite Vaz, M.M. et al. Quercetin-PVP K25 solid dispersions. J Therm Anal Calorim 104, 273–278 (2011). https://doi.org/10.1007/s10973-010-1083-3

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