PRODUCTION AND EVALUATION OF THE RELEASE PROFILE AND BIOSAFETY OF LINSEED OIL MICROEMULSION FOR IVERMECTIN DELIVERY
Nanotechnology; microemulsion; antiparasitic; topical; biosafety.
Ivermectin (IVM) is a widely used antiparasitic drug. However, its low aqueous solubility and limited permeability may compromise its therapeutic efficacy, especially in topical delivery. Thus, microemulsions represent a promising strategy to improve drug solubilization, stability, and skin permeation. Therefore, this study aimed to develop and characterize a linseed oil (LO) microemulsion containing IVM (IVM-MeLO) for topical use. The formulation was prepared using, Kolliphor® RH40, Span 80®, LO, purified water, and IVM, and characterized regarding hydrodynamic diameter, polydispersity index (PdI), pH, electrical conductivity, entrapment efficiency (EE) and Fourier-transform infrared spectroscopy (FTIR). IVM’s chemical stability studies were performed for 30 days at room temperature (25 ± 2 ºC) using High Performance Liquid Chromatography. In addition, IVM-MeLO in vitro release assays using Franz diffusion cells and hemolysis tests for biosafety evaluation were performed. IVM-MeLO presented a hydrodynamic diameter of 21.70 ± 0.20 nm, PdI of 0.09 ± 0.01, pH of 5.33 ± 0.05, conductivity of 318.0 ± 2.00 µS.cm⁻¹, and EE of 93.22 ± 5.60%. The formulation maintained 93.22 ± 5.60% compared to initial IVM concentration after 30 days. FTIR analysis demonstrated preservation of the characteristic bands of IVM-MeLO’s components, indicating chemical compatibility and IVM incorporation in the system. In vitro release assays showed a slow-release profile for IVM-MeLO, reaching approximately 64% drug release after 24 h. The Weibull model provided adequate kinetic fit (R² = 0.9374). Furthermore, IVM-MeLO showed hemolytic activity lower than 2%, indicating hemocompatibility. Overall, IVM-MeLO demonstrated potential as a nanotechnological platform for topical controlled IVM delivery.