Inclusion complex and nanoclusters of cyclodextrin to increase the solubility and efficacy of albendazole

Show simple item record Pacheco, P. A. Rodrigues, Letícia Norma Carpentieri [UNIFESP] Ferreira, J. F. S. Gomes, A. C. P. Verissimo, C. J. Louvandini, H. Costa, R. L. D. Katiki, L. M. 2020-07-08T13:09:30Z 2020-07-08T13:09:30Z 2018
dc.identifier.citation Parasitology Research. New York, v. 117, n. 3, p. 705-712, 2018.
dc.identifier.issn 0932-0113
dc.description.abstract Albendazole (ABZ), a benzimidazole widely used to control gastrointestinal parasites, is poorly soluble in water, resulting in variable and incomplete bioavailability. This has favored the appearance ABZ-resistant nematodes and, consequently, an increase in its clinical ineffectiveness. Among the pharmaceutical techniques developed to increase drug efficacy, cyclodextrins (CDs) and other polymers have been extensively used with water-insoluble pharmaceutical drugs to increase their solubility and availability. Our objective was to prepare ABZ formulations, including beta-cyclodextrin (beta CD) or hydroxypropyl-beta-cyclodextrin (HP beta CD), associated or not to the water-soluble polymer polyvinylpyrrolidone (PVP). These formulations had their solubility and anthelmintic effect both evaluated in vitro. Also, their anthelmintic efficacy was evaluated in lambs naturally infected with gastrointestinal nematodes (GIN) through the fecal egg count (FEC) reduction test. In vitro, the complex ABZ/HP beta CD had higher solubility than ABZ/beta CD. The addition of PVP to the complexes increased solubility and dissolution rates more effectively for ABZ/HP beta CD than for ABZ/beta CD. In vivo, 48 lambs naturally infected with GIN were divided into six experimental groups: control, ABZ, ABZ/beta CD, ABZ/beta CD-PVP, ABZ/HP beta CD, and ABZ/HP beta CD-PVP. Each treated animal received 10 mg/kg of body weight (based on the ABZ dose) for three consecutive days. After 10 days of the last administered dose, treatment efficacy was calculated. The efficacy values were as follows: ABZ (70.33%), ABZ/beta CD (85.33%), ABZ/beta CD-PVP (82.86%), ABZ/HP beta CD (78.37%), and ABZ/HP beta CD-PVP (43.79%). In vitro, ABZ/HP beta CD and ABZ/HP beta CD-PVP had high solubility and dissolution rates. In vivo, although the efficacies of ABZ/beta CD, ABZ/beta CD-PVP, and ABZ/HP beta CD increased slightly when compared to pure ABZ, this increase was not significant (P > 0.05). en
dc.description.sponsorship Fundacao de Amparo a Pesquisa do Estado de Sao Paulo (FAPESP) |Coordenacao de Aperfeicoamento de Pessoal do Nivel Superior (CAPES)
dc.format.extent 705-712
dc.language.iso eng
dc.publisher Springer
dc.relation.ispartof Parasitology Research
dc.rights Acesso restrito
dc.subject Albendazole en
dc.subject Inclusion complex en
dc.subject Cyclodextrin en
dc.subject Solubility en
dc.subject Anthelmintic en
dc.subject Sheep en
dc.title Inclusion complex and nanoclusters of cyclodextrin to increase the solubility and efficacy of albendazole en
dc.type Artigo
dc.description.affiliation IZ APTA SAA, Inst Zootecnia, Rua Heitor Penteado 56, BR-13460000 Nova Odessa, SP, Brazil
dc.description.affiliation Univ Fed Sao Paulo, ICAQF UNIFESP, Diadema, SP, Brazil
dc.description.affiliation USDA ARS, US Salin Lab, 4500 Glenwood Dr, Riverside, CA 92501 USA
dc.description.affiliation Univ Sao Paulo, Ctr Energia Nucl Agr, Piracicaba, SP, Brazil
dc.description.affiliationUnifesp Univ Fed Sao Paulo, ICAQF UNIFESP, Diadema, SP, Brazil
dc.description.sponsorshipID FAPESP: 2013/15704-3
dc.description.sponsorshipID Coordenacao de Aperfeicoamento de Pessoal do Nivel Superior
dc.identifier.doi 10.1007/s00436-017-5740-3
dc.description.source Web of Science
dc.identifier.wos WOS:000426550800008
dc.coverage New York
dc.citation.volume 117
dc.citation.issue 3


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