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Erschienen in:

10.01.2022 | Original Article

Curcumin and n-acetylcysteine cocrystal produced with supercritical solvent: characterization, solubility, and preclinical evaluation of antinociceptive and anti-inflammatory activities

verfasst von: Alessandro R. Paulazzi, Bianca O. Alves, Gabriela A. L. Zilli, Aline E. dos Santos, Fernanda Petry, Krissie D. Soares, Letícia J. Danielli, Jefferson Pedroso, Miriam A. Apel, Gean Pablo S. Aguiar, Anna M. Siebel, J. Vladimir Oliveira, Liz Girardi Müller

Erschienen in: Inflammopharmacology | Ausgabe 1/2022

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Abstract

Curcumin presents a promising anti-inflammatory potential, but its low water-solubility and bioavailability hinder its application. In this sense, cocrystallization represents a tool for improving physicochemical properties, solubility, permeability, and bioavailability of new drug candidates. Thus, the aim of this work was to produce curcumin cocrystals (with n-acetylcysteine as coformer, which possesses anti-inflammatory and antioxidant activities), by the anti-solvent gas technique using supercritical carbon dioxide, and to test its antinociceptive and anti-inflammatory potential. The cocrystal was characterized by differential scanning calorimetry, powder X-ray diffraction and scanning electron microscopy. The cocrystal solubility and antichemotaxic activity were also assessed in vitro. Antinociceptive and anti-inflammatory activities were carried out in vivo using the acetic acid-induced abdominal writhing and carrageenan-induced paw oedema assays in mice. The results demonstrated the formation of a new crystalline structure, thereby confirming the successful formation of the cocrystal. The higher solubility of the cocrystal compared to pure curcumin was verified in acidic and neutral pH, and the cocrystal inhibited the chemotaxis of neutrophils in vitro. In vivo assays showed that cocrystal presents increased antinociceptive and anti-inflammatory potency when compared to pure curcumin, which could be related to an improvement in its bioavailability.
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Metadaten
Titel
Curcumin and n-acetylcysteine cocrystal produced with supercritical solvent: characterization, solubility, and preclinical evaluation of antinociceptive and anti-inflammatory activities
verfasst von
Alessandro R. Paulazzi
Bianca O. Alves
Gabriela A. L. Zilli
Aline E. dos Santos
Fernanda Petry
Krissie D. Soares
Letícia J. Danielli
Jefferson Pedroso
Miriam A. Apel
Gean Pablo S. Aguiar
Anna M. Siebel
J. Vladimir Oliveira
Liz Girardi Müller
Publikationsdatum
10.01.2022
Verlag
Springer International Publishing
Erschienen in
Inflammopharmacology / Ausgabe 1/2022
Print ISSN: 0925-4692
Elektronische ISSN: 1568-5608
DOI
https://doi.org/10.1007/s10787-021-00917-5