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Physical and pharmacokinetic characterization of Soluvec™, a novel, solvent-free aqueous ivermectin formulation
Richa Mandalaywala1, Azhar Rana1, Aubrey L Ramos1
1Mountain Valley MD, 260 Edgeley Blvd - Unit 4, Concord, Ontario, L4K 3Y4, Canada.
Abstract:
Purpose: To describe application of the Quicksol™ solvent-free approach to solubilize ivermectin (IVM). Methods: Lyophilized IVM complexed with hydroxypropyl-β-cyclodextrin (HP-β-CD) was resolubilized in aqueous polysorbate-80, generating Soluvec™. Lyophilizate was examined by Fourier-transform infrared spectroscopy and differential scanning calorimetry; Soluvec, by dynamic light scattering. Pharmacokinetics was evaluated in dogs allocated to subcutaneous (SC) or intramuscular (IM) Soluvec or oral IVM. Results: IVM in Soluvec was tightly bound by HPβCD, forming nearly monodisperse 28 nm particles with solubility ∼2500-times that of free IVM. SC and IM Soluvec increased IVM exposure, peak IVM and extended duration of IVM exposure, versus oral dosing. Conclusion: The Quicksol method generated Soluvec, a concentrated aqueous parenteral IVM formulation with pharmacokinetic properties suitable for veterinary or human use.
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