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Tytuł:
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Nanoemulsion composed of 10-(4,5-dihydrothiazol-2-yl)thio)decan-1-ol), a synthetic analog of 3-alkylpiridine marine alkaloid: development, characterization, and antimalarial activity.
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Autorzy:
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Silva MGD; Federal University of São João del-Rei, Campus Centro Oeste Dona Lindu, Sebastião Gonçalves Coelho 400, Chanadour, 35.501-296, Divinópolis, Minas Gerais, Brazil.
Cardoso JF; School of Pharmacy, Federal University of Ouro Preto, Campus Morro do Cruzeiro w/n, Bauxita, 35.400-000, Ouro Preto, Minas Gerais, Brazil.
Perasoli FB; School of Pharmacy, Federal University of Ouro Preto, Campus Morro do Cruzeiro w/n, Bauxita, 35.400-000, Ouro Preto, Minas Gerais, Brazil.
Branquinho RT; School of Pharmacy, Federal University of Ouro Preto, Campus Morro do Cruzeiro w/n, Bauxita, 35.400-000, Ouro Preto, Minas Gerais, Brazil.
Mourão RS; School of Pharmacy, Federal University of Ouro Preto, Campus Morro do Cruzeiro w/n, Bauxita, 35.400-000, Ouro Preto, Minas Gerais, Brazil.
Tavares HDS; Federal University of São João del-Rei, Campus Centro Oeste Dona Lindu, Sebastião Gonçalves Coelho 400, Chanadour, 35.501-296, Divinópolis, Minas Gerais, Brazil.
Xocaira MLCT; Federal University of São João del-Rei, Campus Centro Oeste Dona Lindu, Sebastião Gonçalves Coelho 400, Chanadour, 35.501-296, Divinópolis, Minas Gerais, Brazil.
Guimarães DSM; Federal University of São João del-Rei, Campus Centro Oeste Dona Lindu, Sebastião Gonçalves Coelho 400, Chanadour, 35.501-296, Divinópolis, Minas Gerais, Brazil.
Viana GHR; Federal University of São João del-Rei, Campus Centro Oeste Dona Lindu, Sebastião Gonçalves Coelho 400, Chanadour, 35.501-296, Divinópolis, Minas Gerais, Brazil.
Varotti FP; Federal University of São João del-Rei, Campus Centro Oeste Dona Lindu, Sebastião Gonçalves Coelho 400, Chanadour, 35.501-296, Divinópolis, Minas Gerais, Brazil.
Silva GRD; School of Pharmacy, Federal University of Ouro Preto, Campus Morro do Cruzeiro w/n, Bauxita, 35.400-000, Ouro Preto, Minas Gerais, Brazil. Electronic address: .
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Źródło:
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European journal of pharmaceutical sciences : official journal of the European Federation for Pharmaceutical Sciences [Eur J Pharm Sci] 2020 Aug 01; Vol. 151, pp. 105382. Date of Electronic Publication: 2020 May 26.
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Typ publikacji:
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Journal Article
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Język:
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English
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Imprint Name(s):
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Publication: Amsterdam : Elsevier Science B.V
Original Publication: Amsterdam ; New York : Elsevier, c1993-
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MeSH Terms:
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Alkaloids*/pharmacology
Antimalarials*/pharmacology
Antimalarials*/therapeutic use
Malaria*/drug therapy
Animals ; Parasitemia/drug therapy ; Plasmodium berghei ; Plasmodium falciparum
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Contributed Indexing:
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Keywords: 10-(4,5-dihydrothiazol-2-yl)thio)decan-1-ol); 3-alkylpyridine marine alkaloid analogs; Malaria; Nanoemulsion; Plasmodium falciparum; Thiazole
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Substance Nomenclature:
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0 (Alkaloids)
0 (Antimalarials)
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Entry Date(s):
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Date Created: 20200530 Date Completed: 20210621 Latest Revision: 20210621
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Update Code:
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20240104
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DOI:
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10.1016/j.ejps.2020.105382
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PMID:
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32470575
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Malaria treatment is based on a reduced number of antimalarial drugs, and drug resistance has emerged, leading to the search for new antimalarial drugs incorporated into pharmaceutical formulations. In this study, 10-(4,5-dihydrothiazol-2-yl)thio)decan-1-ol) (thiazoline), a synthetic analog of 3-alkylpiridine marine alkaloid, and a potent antimalarial substance, was incorporated into O/W nanoemulsion. This formulation was prepared by a 2 3 factorial design. It was characterized by globule diameter, polydispersity index, zeta potential, encapsulation efficiency, in vitro thiazoline release at pH 2 and 6.86, and accelerated stability. In vitro and in vivo antimalarial activity was determined against P. falciparum and P. berghei, respectively. Thiazoline nanoemulsion showed 248.8 nm of globule diameter, 0.236 of polydispersity index, -38.5 mV of zeta potential, 96.92% encapsulation efficiency, and it was stable for 6 months. Thiazoline release profiles differed in acidic and neutral media, but in both cases, the nanoemulsion controlled and prolonged the thiazoline delivery. Thiazoline nanoemulsion exerted in vitro antimalarial activity against the parasite (IC 50 = 1.32 µM), and it significantly reduced the in vivo parasitemia for 8 days without increasing the survival time of animals. Therefore, the thiazoline nanoemulsion represents a strategy to treat malaria combining an antimalarial candidate and a new nanocarrier.
Competing Interests: Declarations of Competing Interest none.
(Copyright © 2020 Elsevier B.V. All rights reserved.)