Click
here to close Hello! We notice that
you are using Internet Explorer, which is not supported by Echinobase
and may cause the site to display incorrectly. We suggest using a
current version of Chrome,
FireFox,
or Safari.
Parasitol Res
2018 Mar 01;1173:705-712. doi: 10.1007/s00436-017-5740-3.
Show Gene links
Show Anatomy links
Inclusion complex and nanoclusters of cyclodextrin to increase the solubility and efficacy of albendazole.
Pacheco PA
,
Rodrigues LNC
,
Ferreira JFS
,
Gomes ACP
,
Veríssimo CJ
,
Louvandini H
,
Costa RLD
,
Katiki LM
.
???displayArticle.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 β-cyclodextrin (βCD) or hydroxypropyl-β-cyclodextrin (HPβCD), 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/HPβCD had higher solubility than ABZ/βCD. The addition of PVP to the complexes increased solubility and dissolution rates more effectively for ABZ/HPβCD than for ABZ/βCD. In vivo, 48 lambs naturally infected with GIN were divided into six experimental groups: control, ABZ, ABZ/βCD, ABZ/βCD-PVP, ABZ/HPβCD, and ABZ/HPβCD-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/βCD (85.33%), ABZ/βCD-PVP (82.86%), ABZ/HPβCD (78.37%), and ABZ/HPβCD-PVP (43.79%). In vitro, ABZ/HPβCD and ABZ/HPβCD-PVP had high solubility and dissolution rates. In vivo, although the efficacies of ABZ/βCD, ABZ/βCD-PVP, and ABZ/HPβCD increased slightly when compared to pure ABZ, this increase was not significant (P > 0.05).
???displayArticle.pubmedLink???
29327323
???displayArticle.link???Parasitol Res ???displayArticle.grants???[+]
2013/15704-3 Fundação de Amparo à Pesquisa do Estado de São Paulo, 1476123 Coordenação de Aperfeiçoamento de Pessoal de Nível Superior
Ali,
The effect of reduced feed intake on the efficacy of oxfendazole against benzimidazole resistant Haemonchus contortus and Trichostrongylus colubriformis in sheep.
1995, Pubmed
Ali,
The effect of reduced feed intake on the efficacy of oxfendazole against benzimidazole resistant Haemonchus contortus and Trichostrongylus colubriformis in sheep.
1995,
Pubmed
Alvarez,
Drug transfer into target helminth parasites.
2007,
Pubmed
Aronson,
Correction factor for dissolution profile calculations.
1993,
Pubmed
Asbahr,
Binary and ternary inclusion complexes of finasteride in HPbetaCD and polymers: preparation and characterization.
2009,
Pubmed
Brewster,
Cyclodextrins as pharmaceutical solubilizers.
2007,
Pubmed
Cardia,
Immune response and performance of growing Santa Ines lambs to artificial Trichostrongylus colubriformis infections.
2011,
Pubmed
Carrier,
The utility of cyclodextrins for enhancing oral bioavailability.
2007,
Pubmed
Castillo,
Preparation and characterization of albendazole beta-cyclodextrin complexes.
1999,
Pubmed
Challa,
Cyclodextrins in drug delivery: an updated review.
2005,
Pubmed
Charkoftaki,
Biopharmaceutical classification based on solubility and dissolution: a reappraisal of criteria for hypothesis models in the light of the experimental observations.
2010,
Pubmed
Coles,
World Association for the Advancement of Veterinary Parasitology (W.A.A.V.P.) methods for the detection of anthelmintic resistance in nematodes of veterinary importance.
1992,
Pubmed
Daniel-Mwambete,
The effect of solubilization on the oral bioavailability of three benzimidazole carbamate drugs.
2004,
Pubmed
Delatour,
Netobimin (Totabin-SCH): preliminary investigations on metabolism and pharmacology.
1986,
Pubmed
Ehteda,
Complexation of albendazole with hydroxypropyl-β-cyclodextrin significantly improves its pharmacokinetic profile, cell cytotoxicity and antitumor efficacy in nude mice.
2012,
Pubmed
Evrard,
Oral bioavailability in sheep of albendazole from a suspension and from a solution containing hydroxypropyl-beta-cyclodextrin.
2002,
Pubmed
García,
Modified β-cyclodextrin inclusion complex to improve the physicochemical properties of albendazole. complete in vitro evaluation and characterization.
2014,
Pubmed
Gokbulut,
Comparative plasma disposition of fenbendazole, oxfendazole and albendazole in dogs.
2007,
Pubmed
Kawabata,
Formulation design for poorly water-soluble drugs based on biopharmaceutics classification system: basic approaches and practical applications.
2011,
Pubmed
Kurkov,
Cyclodextrins.
2013,
Pubmed
Lanusse,
Pharmacological knowledge and sustainable anthelmintic therapy in ruminants.
2014,
Pubmed
Loftsson,
Evaluation of cyclodextrin solubilization of drugs.
2005,
Pubmed
Martin,
Modes of action of anthelmintic drugs.
1997,
Pubmed
Martinez-Marcos,
A novel hot-melt extrusion formulation of albendazole for increasing dissolution properties.
2016,
Pubmed
Messner,
Self-assembled cyclodextrin aggregates and nanoparticles.
2010,
Pubmed
Moreno,
Dose-dependent activity of albendazole against benzimidazole-resistant nematodes in sheep: relationship between pharmacokinetics and efficacy.
2004,
Pubmed
Palomares-Alonso,
Two novel ternary albendazole-cyclodextrin-polymer systems: dissolution, bioavailability and efficacy against Taenia crassiceps cysts.
2010,
Pubmed
Pensel,
Enhanced chemoprophylactic and clinical efficacy of albendazole formulated as solid dispersions in experimental cystic echinococcosis.
2014,
Pubmed
Soares-Sobrinho,
Benznidazole drug delivery by binary and multicomponent inclusion complexes using cyclodextrins and polymers.
2012,
Pubmed
Sullivan,
Dissolving polymer microneedle patches for influenza vaccination.
2010,
Pubmed
Waller,
Anthelmintic resistance.
1997,
Pubmed
dos Santos,
Phase solubility studies and stability of cholesterol/β-cyclodextrin inclusion complexes.
2011,
Pubmed
