Formulation and evaluation of ivermectin-loaded dissolving microarray patches for rosacea disease
Abstract
Purpose
This investigation aims to develop and characterise dissolving microarray patches (MAPs) loaded with ivermectin (IVM) for rosacea therapy.
Methods
Tween® 80 and Soluplus® were evaluated to enhance the water solubility of IVM powder. Three dissolving MAPs were fabricated using a two-layer casting method, pure IVM-loaded (F1), IVM-Tween® 80 (F2), and IVM-Soluplus® (F3) loaded patches. Formulations were evaluated for drug content, in vitro and ex vivo mechanical performances, ex vivo skin dissolution time, dermatokinetics, in vitro biocompatibility and activity against rosacea.
Results
IVM solubility in water was improved with surfactants, reaching 1206.42 ± 53.78 and 130.78 ± 12.78 µg/mL in Tween® 80 and Soluplus® solutions, respectively. The MAPs, featuring bubble-free, perfectly shaped pyramidal needles of approximately 800 μm, exhibited considerably higher IVM content in F2 and F3 than in F1 (2.31 ± 0.26 mg for F1, 3.58 ± 0.15 mg for F2, and 3.19 ± 0.22 mg for F3). All formulations demonstrated mechanical robustness and penetrated the skin to a depth of 650 μm. The highest IVM deposition in the skin at 24 h was achieved by F2, selected as the lead formulation (F1 = 1456.35 ± 266.90 µg; F2 = 2165.24 ± 130.13 µg; F3 = 1684.74 ± 212.09 µg). Furthermore, F2 and F3 provided faster IVM deposition, most likely due to the quicker dissolution rate of microneedles in the skin. F2 proved biocompatible to skin cells in vitro and effectively inhibited the inflammatory cascade associated with rosacea diseases.
Conclusion
This study encourages further investigation into IVM-loaded dissolving MAPs formulated with Tween® 80 for rosacea therapy.
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Materials
Ivermectin (IVM) (purity, 95%) and Tween® 80 were purchased from Tokyo Chemical (Oxford, UK). Soluplus® was generously provided by BASF (Ludwigshafen, Germany). Polyvinylpyrrolidone (PVP) 90 kDa (Plasdone™ K-29/32) was obtained from Ashland (Kidderminster, UK). Dulbecco’s Modified Eagle’s medium (DMEM), fetal bovine serum (FBS), and the 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide (MTT) assay kit, along with dimethyl sulfoxide (DMSO), were sourced from Sigma Aldrich (St. Louis, MO, USA). The human epidermal keratinocytes (HaCaT) cell line was acquired from ATCC. The enzyme-linked immunosorbent assay (ELISA) analysis kit was procured from R&D Systems (Minneapolis, MN, USA). All other reagents, which were of analytical grade, were purchased from Sigma-Aldrich (Dorset, UK) or Fisher Scientific (Loughborough, UK). The full-thickness neonatal porcine skin used in the study was sourced from stillborn piglets within 24 h post-mortem and stored frozen at -20 °C before experimentation.
Anjani, Q.K., Demartis, S., Moreno-Castellanos, N. et al. Formulation and evaluation of ivermectin-loaded dissolving microarray patches for rosacea disease. J. Pharm. Investig. (2024). https://doi.org/10.1007/s40005-024-00682-x
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