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Investigation of hydroxypropyl-β-cyclodextrin inclusion complexation of two poorly soluble model drugs and their taste-sensation - Effect of electrolytes, freeze-drying and incorporation into oral film formulations

The goal for any formulation design of poorly soluble drugs is to increase the solubility. However, increased solubility is a challenge when the drug is administered to the oral cavity as rapidly dispersing or mucoadhesive buccal films. Most drugs are bitter and increased solubility may correlate wi...

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Published in:Journal of drug delivery science and technology 2021-02, Vol.61, p.102245, Article 102245
Main Authors: Alopaeus, Julia F., Göbel, Anja, Breitkreutz, Jörg, Sande, Sverre Arne, Tho, Ingunn
Format: Article
Language:English
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Summary:The goal for any formulation design of poorly soluble drugs is to increase the solubility. However, increased solubility is a challenge when the drug is administered to the oral cavity as rapidly dispersing or mucoadhesive buccal films. Most drugs are bitter and increased solubility may correlate with perceived worsening of the taste profile. The aim of the present work was to investigate the dual effect of inclusion complex formation, namely solubilization of two lipophilic model drugs (indomethacin and furosemide) in the hydrophobic cavity of hydroxypropyl-β-cyclodextrin with the aim of increasing the solubility in different electrolyte solutions, and at the same time hinder the taste sensation of the solubilized drug. Taste perception investigations were performed using an electronic tongue on simple solutions, inclusion complexes and on multi-component formulations such as orodispersible films and buccal films. The electrolyte media was found to have an effect on solubilization, association constant and complexation efficiency of both model drugs. Buffers containing phosphate ions were generally better than other electrolyte media with respect to the solubility parameters, and freeze-drying had a favorable effect on all the desirable properties. This work demonstrated that freeze-dried drug-hydropxypropyl-β-cyclodextrin complexes in solution, or added to orodispersible or buccal film, exhibit different taste sensation as compared to the plain drug in solution or reference films without complexes, indicating a successful taste-masking. [Display omitted]
ISSN:1773-2247
DOI:10.1016/j.jddst.2020.102245