Solving the Delivery Problems of Triclabendazole Using Cyclodextrins

AAPS PharmSciTech
Daniel RealClaudio J Salomon

Abstract

Triclabendazole is the first-line drug of choice to treat and control fasciolasis, a neglected parasitic human disease. It is a class II/IV compound according to the Biopharmaceutics Classification System. Thus, the aim of this study was to improve aqueous solubility and dissolution rate of triclabendazole complexed with 2-hydroxylpropyl-β-cyclodextrin (HP-β-CD) and methyl-β-cyclodextrin (Me-β-CD) at 1:1 and 1:2 M ratio. The impact of storage on the solubility, dissolution profile, and solid-state properties of such complexes was also investigated. Drug-carrier interactions were characterized by infrared spectroscopy, differential scanning calorimetry, X-ray diffractometry, and scanning electron microscopy. The solubility of triclabendazole improved up to 256- and 341-fold using HP-β-CD and Me-β-CD, respectively. In particular, the drug complexed with Me-β-CD showed a positive deviation from linearity, suggesting that its solubility increases with an increasing concentration of Me-β-CD concentration in a nonlinear manner. The drug dissolution was found to be improved through complex formation with HP-β-CD and Me-β-CD. In particular, the 1:2 M ratio complexes exhibited higher dissolution than the corresponding 1:1 M ratio comple...Continue Reading

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Citations

May 8, 2019·Wiley Interdisciplinary Reviews. Nanomedicine and Nanobiotechnology·Soeun GimMartina Delbianco
Jun 5, 2021·Biomaterials·Youssef W NaguibAliasger K Salem

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Methods Mentioned

BETA
differential
X-ray
scanning electron microscopy
Infrared Spectroscopy
NMR

Software Mentioned

Statgraphics Graphics System
Stoe Visual - Xpow package

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