-
Tytuł:
-
Hydroxypropyl-β-cyclodextrin-complexed naringenin by solvent change precipitation for improving anti-inflammatory effect in vivo.
-
Autorzy:
-
Gratieri T; Laboratory of Food, Drug, and Cosmetics (LTMAC), School of Health Sciences, University of Brasilia, 70.910-900, Brasília, DF, Brazil.
Pinho LAG; Laboratory of Food, Drug, and Cosmetics (LTMAC), School of Health Sciences, University of Brasilia, 70.910-900, Brasília, DF, Brazil.
Oliveira MA; Laboratory of Neurosciences and Pharmacological Trials, Department of Physiology, Federal University of Sergipe, SE, Brazil.
Sa-Barreto LL; Laboratory of Food, Drug, and Cosmetics (LTMAC), School of Health Sciences, University of Brasilia, 70.910-900, Brasília, DF, Brazil; Faculty of Ceilândia, University of Brasília (UnB), 72220-900, Brasília, DF, Brazil.
Marreto RN; Laboratory of Nanosystems and Drug Delivery Devices (NanoSYS), School of Pharmacy, Federal University of Goias, 74605-170, Goiânia, GO, Brazil.
Silva IC; Faculty of Ceilândia, University of Brasília (UnB), 72220-900, Brasília, DF, Brazil.
Gelfuso GM; Laboratory of Food, Drug, and Cosmetics (LTMAC), School of Health Sciences, University of Brasilia, 70.910-900, Brasília, DF, Brazil.
de Souza Siqueira Quintans J; Laboratory of Neurosciences and Pharmacological Trials, Department of Physiology, Federal University of Sergipe, SE, Brazil.
Quintans-Junior LJ; Laboratory of Neurosciences and Pharmacological Trials, Department of Physiology, Federal University of Sergipe, SE, Brazil.
Cunha-Filho M; Laboratory of Food, Drug, and Cosmetics (LTMAC), School of Health Sciences, University of Brasilia, 70.910-900, Brasília, DF, Brazil. Electronic address: .
-
Źródło:
-
Carbohydrate polymers [Carbohydr Polym] 2020 Mar 01; Vol. 231, pp. 115769. Date of Electronic Publication: 2019 Dec 19.
-
Typ publikacji:
-
Journal Article
-
Język:
-
English
-
Imprint Name(s):
-
Publication: <1992-> : Barking : Elsevier Applied Science Publishers
Original Publication: London [Eng.] : Applied Science Publishers, c1981-
-
MeSH Terms:
-
2-Hydroxypropyl-beta-cyclodextrin/*chemistry
Anti-Inflammatory Agents/*chemistry
Flavanones/*chemistry
Flavonoids/*chemistry
2-Hydroxypropyl-beta-cyclodextrin/pharmacology ; Anti-Inflammatory Agents/pharmacology ; Calorimetry, Differential Scanning ; Flavanones/pharmacology ; Flavonoids/pharmacology ; Gene Expression Regulation/drug effects ; Humans ; Inflammation/drug therapy ; Models, Molecular ; Solubility ; Solvents/chemistry ; Spectroscopy, Fourier Transform Infrared ; Tumor Necrosis Factor-alpha/genetics ; X-Ray Diffraction
-
Contributed Indexing:
-
Keywords: Anti-inflammatory effect; Cyclodextrin; Naringenin; Solid-state inclusion complex; Solvent change precipitation
-
Substance Nomenclature:
-
0 (Anti-Inflammatory Agents)
0 (Flavanones)
0 (Flavonoids)
0 (Solvents)
0 (Tumor Necrosis Factor-alpha)
1I96OHX6EK (2-Hydroxypropyl-beta-cyclodextrin)
HN5425SBF2 (naringenin)
-
Entry Date(s):
-
Date Created: 20200101 Date Completed: 20200608 Latest Revision: 20200608
-
Update Code:
-
20240104
-
DOI:
-
10.1016/j.carbpol.2019.115769
-
PMID:
-
31888829
-
The flavonoid naringenin (NAR) exhibits an outstanding anti-inflammatory potential; however, stability problems and reduced solubility hinder its commercial insertion. This work aimed to obtain solid-state hydroxypropyl-β-cyclodextrin (CD) inclusion complexes with NAR using, for the first time, the solvent change precipitation method. For this, molecular modeling and physicochemical characterizations were conducted, followed by in vitro and in vivo assays. The complexation method showed thermal and spectroscopic evidence of NAR inclusion complexes formation, suggesting an improvement of its stability. Additionally, 30 min-dissolution efficiency of the complex was 57.2 %, whereas NAR, as supplied, showed only 14.3 %, a four-fold enhancement. In vitro and in vivo performance attested the potent anti-inflammatory and antinociceptive profile of NAR with significant suppression of TNF-α production. Moreover, NAR complexation with CD improved its therapeutic effect, which showed similar activity to that achieved with NAR as supplied but employing only 1/5 of its dose.
(Copyright © 2019 Elsevier Ltd. All rights reserved.)
