ArticlePharmaceutical research2025
Cyclodextrin-mediated Enhancement of Haloperidol Solubility: Physicochemical Studies and In Vivo Investigation Using Planaria Worms.
Article in Pharmaceutical research, 2025. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 1 paper.
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Who cites it
1 citing paper in PubMed.
- Cyclodextrin-Grafted Polysaccharides as Sustainable Platforms for Biomedical and Environmental Applications.International journal of molecular sciences · 2026Review
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Authors and funding
3 authors.
Funding
Abstract
purposeThis study aims to evaluate the ability of various cyclodextrins (CDs) to enhance the aqueous solubility of haloperidol (HAL), through the formation of inclusion complexes. It also investigates the pharmacological activity of CD/HAL complexes using a planaria model.
methodsInclusion complexes were prepared using α-CD, β-CD, methyl-β-CD, hydroxypropyl-β-CD and γ-CD. The solubility of HAL in the presence of CDs was assessed, and the stoichiometry of the complexes was determined using Job's method. Physicochemical interactions between HAL and CDs were characterized by nuclear magnetic resonance (NMR), differential scanning calorimetry (DSC), and powder X-ray diffraction (PXRD). The in vivo pharmacological activity was tested in planaria worms following exposure to HAL in the presence or absence of CDs.
resultsHAL's aqueous solubility was significantly enhanced in the presence of α-CD, methyl-β-CD, and hydroxypropyl-β-CD, while γ-CD showed no effect. Only modest solubility improvements were observed with increasing β-CD concentrations up to 8 mg/mL. Stoichiometric analysis confirmed a 1:1 ratio of HAL to CD in the inclusion complexes. In vivo studies demonstrated that HAL reduced planaria mobility, mimicking cataleptic effects seen in mammals, whereas the presence of CDs reduced this pharmacological effect.
conclusionCyclodextrins, particularly α-CD, methyl-β-CD, and hydroxypropyl-β-CD, effectively enhance the solubility of haloperidol by forming 1:1 inclusion complexes. The reduction in haloperidol-induced behavioral changes in planaria by CDs suggests a potential impact on drug bioavailability and supports the use of planaria as a simple in vivo model for screening neuroactive compounds and formulations.
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