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Inclusion complexes and self-assembled cyclodextrin aggregates for increasing the solubility of benzimidazoles BJPS
Rodrigues,Leticia Norma Carpentieri; Tavares,Anna Carollina Moraes; Ferreira,Beatriz Tavares; Reis,Adriana Karla Cardoso Amorim; Katiki,Luciana Morita.
Albendazole and fenbendazole are imidazole derivatives that exhibit broad spectrum activity against parasites, but the low solubility of these drugs considerably reduces their effectiveness. Complexation of albendazole and fenbendazole with cyclodextrins (β-cyclodextrin and hydroxypropyl-β-cyclodextrin) in both water and an aqueous solution of polyvinylpyrrolidone (PVP-k30) was studied to determine if it could increase the solubility and dissolution rate of the drugs. In an aqueous solution, β-cyclodextrin increased the solubility of albendazole from 0.4188 to ~93.47 µg mL-1 (223×), and of fenbendazole from 0.1054 to 45.56 µg mL-1 (432×); hydroxypropyl-β-cyclodextrin, on the other hand, increased solubility to ~443.06 µg mL-1 (1058×) for albendazole and...
Tipo: Info:eu-repo/semantics/article Palavras-chave: Cyclodextrins/pharmacokinetics Benzimidazoles/administration & Dosage Inclusion complexes Cyclodextrin aggregates Drug liberation/drug effects Antiparasitic agents/analysis Albendazole/analysis Fenbendazole/analysis.
Ano: 2019 URL: http://www.scielo.br/scielo.php?script=sci_arttext&pid=S1984-82502019000100551
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