Article ; Online: Physicochemical and in vitro biological evaluations of furazolidone-based β-cyclodextrin complexes in Leishmania amazonensis.
Research in veterinary science
2018 Volume 119, Page(s) 143–153
Abstract: Recently, there have been numerous cases of leishmaniasis reported in different Brazilian states. The use of furazolidone (FZD) to treat leishmaniasis has been previously described; however, the drug is associated with adverse effects such as anorexia, ... ...
Abstract | Recently, there have been numerous cases of leishmaniasis reported in different Brazilian states. The use of furazolidone (FZD) to treat leishmaniasis has been previously described; however, the drug is associated with adverse effects such as anorexia, weight loss, incoordination, and fatigue in dogs. Thus, in the present study, we prepared and evaluated inclusion complexes between FZD and β-cyclodextrin (β-CD) to guarantee increased drug solubility and reduce the toxicity associated with high doses. The FZD:β-CD complexes were prepared by two different techniques (kneading and lyophilization) prior to incorporation in an oral pharmaceutical dosage form. Formation of the complexes was confirmed using appropriate physicochemical methods. Antileishmanial activity against L. amazonensis was tested in vitro via a microplate assay using resazurin dye and cytotoxicity was determined using the fibroblast L929 lineage. Solubility studies showed the formation of complexes with complexation efficiencies lower than 100%. Physicochemical analysis revealed that FZD was inserted into the β-CD cavity after complexation by both methods. Biological in vitro evaluations demonstrated that free FZD and the FZD:β-CD complexes presented significant leishmanicidal activity against L. amazonensis with IC |
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MeSH term(s) | Animals ; Antiprotozoal Agents/adverse effects ; Antiprotozoal Agents/pharmacology ; Brazil ; Furazolidone/adverse effects ; Furazolidone/pharmacology ; Leishmania mexicana/drug effects ; Parasitic Sensitivity Tests ; Treatment Outcome ; beta-Cyclodextrins/adverse effects ; beta-Cyclodextrins/pharmacology |
Chemical Substances | Antiprotozoal Agents ; beta-Cyclodextrins ; Furazolidone (5J9CPU3RE0) |
Language | English |
Publishing date | 2018-06-15 |
Publishing country | England |
Document type | Journal Article |
ZDB-ID | 840961-4 |
ISSN | 1532-2661 ; 0034-5288 |
ISSN (online) | 1532-2661 |
ISSN | 0034-5288 |
DOI | 10.1016/j.rvsc.2018.06.013 |
Database | MEDical Literature Analysis and Retrieval System OnLINE |
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