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Related Experiment Video

Updated: Feb 9, 2026

Transport Properties of Ibuprofen Encapsulated in Cyclodextrin Nanosponge Hydrogels: A Proton HR-MAS NMR Spectroscopy Study

Transport Properties of Ibuprofen Encapsulated in Cyclodextrin Nanosponge Hydrogels: A Proton HR-MAS NMR Spectroscopy Study

Published on: August 15, 2016

Solving the Delivery Problems of Triclabendazole Using Cyclodextrins.

Daniel Real¹, Darío Leonardi^1,2, Robert O Williams³

¹Instituto de Química de Rosario, Consejo Nacional de Investigaciones Científicas y Tecnológicas, Suipacha 531, 2000, Rosario, Argentina.

AAPS Pharmscitech

|May 31, 2018

Summary

Triclabendazole solubility and dissolution were significantly enhanced by complexation with cyclodextrins (HP-β-CD and Me-β-CD). These novel triclabendazole-cyclodextrin complexes maintained amorphous solid-state properties after long-term storage.

Keywords:

amorphous nature cylodextrin dissolution profiles storage triclabendazole

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Area of Science:

Pharmaceutical Sciences
Drug Delivery
Physical Chemistry

Background:

Triclabendazole is a crucial treatment for fascioliasis, a neglected parasitic disease.
Its poor aqueous solubility (Biopharmaceutics Classification System Class II/IV) limits therapeutic efficacy.
Developing strategies to enhance triclabendazole's bioavailability is essential for effective disease control.

Purpose of the Study:

To improve the aqueous solubility and dissolution rate of triclabendazole.
To investigate complexation with 2-hydroxylpropyl-β-cyclodextrin (HP-β-CD) and methyl-β-cyclodextrin (Me-β-CD) at 1:1 and 1:2 molar ratios.
To assess the impact of storage on the physicochemical properties of the resulting complexes.

Main Methods:

Complexation of triclabendazole with HP-β-CD and Me-β-CD.
Solubility and dissolution rate measurements.
Solid-state characterization using infrared spectroscopy, differential scanning calorimetry, X-ray diffractometry, and scanning electron microscopy.
Stability studies under defined storage conditions (25°C, 60% RH for 24 months).

Main Results:

Solubility increased up to 256-fold with HP-β-CD and 341-fold with Me-β-CD.
Complexation significantly improved drug dissolution, with 1:2 molar ratios showing higher efficacy than 1:1 ratios.
Physicochemical analyses indicated the formation of inclusion complexes and/or amorphous phases.
Complexes remained amorphous after 24 months of storage, demonstrating good stability.

Conclusions:

Triclabendazole-cyclodextrin inclusion complex formation markedly enhances drug solubility and dissolution.
The 1:2 molar ratio complexes, particularly with Me-β-CD, offer superior improvements.
These findings support the development of novel triclabendazole formulations with improved biopharmaceutical characteristics and stability.