Ivermectin

Aucamp Z, et al. Journal of Drug Delivery Science and Technology, 2024, 101(A), 106174.

Ivermectin Emulgel Formulation: Emulgels were prepared using 2% ivermectin with varying ratios of surfactants (Tween 80 and Span 60) and gelling agent (Carbopol Ultrez 20). The oil phase (Span 60 and ivermectin) and the water phase (Carbopol Ultrez 20 and Tween 80) were heated separately to ~80 °C. The oil phase was incrementally added to the water phase, homogenized at 13,500 rpm for 5 minutes, and subsequently cooled to room temperature. pH adjustments using NaOH facilitated gel formation, resulting in the optimized emulgel formulation, EG, alongside a placebo control (PEG).
Ivermectin Cream Formulation: The creams, containing 2% ivermectin, were designed with surfactant blends and cetyl alcohol as a thickening agent. The oil phase (Span 60, EPO, and cetyl alcohol) and water phase (Tween® 80 and water) were heated separately before being combined. Emulsification and pH adjustments yielded a stable cream formulation (CR) and a placebo (PCR) for comparative analysis.
Ivermectin Ointment Formulation: Ointments were formulated using polyethylene glycol (PEG 400 and PEG 4000) as the base. The components were melted, and ivermectin was incorporated with continuous stirring until dissolved. The mixture was cooled under stirring, resulting in an optimized ointment (OM) and a placebo counterpart (POM).

Aboelhadid SM, et al. Veterinary Parasitology, 2024, 332, 110335.

This study investigated the efficacy of ivermectin in combination with essential oil components (EOCs)-carvacrol, cinnamaldehyde, D-limonene, trans-anethole, and thymol-for controlling Rhipicephalus annulatus ticks from Egyptian isolates.
Using a larval immersion test, ivermectin was prepared in a 1% EthTX solution at concentrations ranging from 3 mg/mL to 0.0125 mg/mL. EOCs were diluted in a similar medium to final concentrations of 20, 10, 5, and 2.5 mg/mL. Both ivermectin and each EOC were tested individually and in 1:1 LC50 combinations.
The results demonstrated significant toxicity of all EOCs against R. annulatus larvae. While carvacrol and thymol increased mortality when combined with ivermectin, their combination indices (CIs) exceeded one, indicating no synergism. Conversely, D-limonene, cinnamaldehyde, and trans-anethole achieved high mortality rates (up to 100%) and exhibited CIs close to one, suggesting an additive effect. These findings highlight the potential of combining ivermectin with certain EOCs, particularly D-limonene, cinnamaldehyde, and trans-anethole, to manage cattle tick infestations effectively.

Ma B, et al. International Immunopharmacology, 2024, 143(1), 113360.

This study explores ivermectin's therapeutic potential in alleviating psoriasis-like lesions by targeting karyopherin subunit alpha 2 (KPNA2), a nuclear transport protein implicated in cell proliferation and differentiation. KPNA2 was found to be significantly upregulated in psoriatic lesions of patients and in imiquimod (IMQ)-induced psoriasis mouse models. In vivo studies demonstrated that ivermectin, a potent KPNA2 inhibitor, effectively reduced psoriasis symptoms, including erythema, desquamation, and epidermal thickening. Histopathological analysis confirmed reduced KPNA2 expression alongside decreased markers of abnormal keratinocyte proliferation and differentiation, such as K17 and Ki67.
Further transcriptomic and molecular analyses revealed that ivermectin's inhibition of KPNA2 disrupts the nuclear translocation of E2F transcription factor 1 (E2F1), a critical regulator of keratinocyte proliferation. This mechanism was supported by in vitro experiments, where KPNA2 downregulation in HaCaT cells suppressed epidermal growth factor (EGF)-induced activation of the AKT/STAT3 signaling pathway, thereby attenuating keratinocyte proliferation.