Soluplus®-based dissolving microarray patches loaded with colchicine: towards a minimally invasive treatment and management of gout

Considered as one of the most common inflammatory arthritis, gout is characterised by a sudden onset of severe joint pain. As the first-line drug of choice used in treating acute gout, colchicine (CLC) is hindered by poor gastrointestinal permeability as well as unfavourable gastrointestinal side effects. Herein, we present, for the first time, the preparation of microarray patches (MAPs) made of a polymeric solubiliser, Soluplus®, loaded with CLC for its systemic delivery. The fabricated MAPs displayed acceptable mechanical properties and were capable of being inserted into the skin to a depth of ≈500 μm in full thickness ex vivo neonatal porcine skin, as evidenced by optical coherence tomography.

In vitro dermatokinetic studies utilising full thickness neonatal porcine skin demonstrated that the CLC-loaded MAPs delivered CLC across all skin strata, resulting in a delivery efficiency of 73% after 24 hours. Furthermore, 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyl tetrazolium bromide (MTT) and cell proliferation assays along with LIVE/DEAD™ staining on the 3T3-L1 cell line showed that the MAP formulation displayed minimal toxicity, with acceptable biocompatibility. Lastly, the anti-inflammatory properties of the formulation were evaluated using a THP-1 macrophage cell line. It was shown that treatment of THP-1 macrophages that are exposed to lipopolysaccharide (LPS) with CLC-loaded MAPs caused a significant (p < 0.05) reduction of TNF-α production, a pro-inflammatory cytokine typically associated with the early onset of acute gout. Accordingly, CLC-loaded MAPs could represent a new minimally-invasive alternative strategy for management of acute gout.

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Colchicine (purity, 95%) was procured from Alfa Aesar (Lancashire, UK). Soluplus® was kindly donated by BASF (Ludwigshafen, Germany). PVP 90 kDa (Plasdone™ K-29/32) was obtained by Ashland (Kidderminster, UK). HPLC grade water used in the current work was supplied from a water purification system (Elga PURELAB DV 25, Veolia Water Systems, Dublin, Ireland). All other reagents that were of analytical grade were procured from Sigma-Aldrich (Dorset, UK) or Fisher Scientific (Loughborough, UK). The full-thickness neonatal porcine skins used in the current work were sourced from stillborn piglets within 24 h post-mortem and frozen at −20 °C prior to experimentation.

Qonita Kurnia Anjani , Akmal Hidayat Bin Sabri , Natalia Moreno-Castellanos , Emilia Utomo , Álvaro Cárcamo-Martínez, Juan Domínguez-Robles, Luki Ahmadi Hari Wardoyo and Ryan F. Donnelly
Biomater. Sci., 2022
DOI: 10.1039/d2bm01068b

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