Cyclosporine coated microneedle for transcutaneous delivery: Characterization, in vitro evaluation, and in vivo anti-psoriatic efficacy against IMQ-induced psoriasis

Abstract

Cyclosporine (CsA) delivery causes liver and kidney toxicities in long-term oral use, and its injections are inconvenient for frequent administration in psoriatic patients. Therefore, we aimed to develop polyvinyl alcohol (PVA) microneedle (MNs) arrays for poke and release of cyclosporine transcutaneously for systemic effect against psoriasis-like inflammation. Microneedles were fabricated using the micro-molding-cum-solvent casting method, characterized for patch dimensions and strength. Prepared MNs evaluated for drug loading, in vitro release, skin permeation studies, and in vivo anti-psoriatic activity. MNs showed the desired mechanical strength and dimensions with 6.8 ± 0.29 mg drug coated on needles surface per patch. MNs showed slow moisture gain in humid conditions with good skin penetration strength (up to 630 μm). More than a 60% reduction in the needle length was observed within 30 min of skin insertion. MNs showed fast (87% in 60 min) drug release and efficient permeation through the skin layer 60 min post-insertion into porcine skin. The developed MNs showed a significant reduction in PASI scoring and pro-inflammatory cytokines levels and a remarkable reduction in the spleen size. It was found stable for 6 months in accelerated conditions. In conclusion, the developed MNs array could be an excellent alternative to the existing dosage forms that can deliver cyclosporine transdermally to the systemic circulation to treat psoriasis-like inflammation in long-term use.