Physical and pharmacokinetic characterization of Soluvec™, a novel, solvent-free aqueous ivermectin formulation.

Purpose: To describe application of the Quicksol™ solvent-free approach to solubilize ivermectin (IVM). Methods: Lyophilized IVM complexed with hydroxypropyl-ß-cyclodextrin (HP-ß-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 HPßCD, 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.

Ivermectin (IVM) kills insects and worms that cause disease. Because it doesn't dissolve well, blood IVM can be low. We found a new way to dissolve IVM, using simple, common materials. Dogs receiving our IVM (Soluvec™) had high blood IVM levels for longer, compared with tablet IVM. Next, we hope to learn the best ways to dose Soluvec in animals and people.