Calcipotriol Nanosuspension-Loaded Trilayer Dissolving Microneedle Patches for the Treatment of Psoriasis: In Vitro Delivery and In Vivo Antipsoriatic Activity Studies

Psoriasis, affecting 2–3% of the global population, is a chronic inflammatory skin condition without a definitive cure. Current treatments focus on managing symptoms. Recognizing the need for innovative drug delivery methods to enhance patient adherence, this study explores a new approach using calcipotriol monohydrate (CPM), a primary topical treatment for psoriasis. Despite its effectiveness, CPM’s therapeutic potential is often limited by factors like the greasiness of topical applications, poor skin permeability, low skin retention, and lack of controlled delivery.

To overcome these challenges, the study introduces CPM in the form of nanosuspensions (NSs), characterized by an average particle size of 211 ± 2 nm. These CPM NSs are then incorporated into a trilayer dissolving microneedle patch (MAP) made from poly(vinylpyrrolidone) and w poly(vinyl alcohol) as needle arrays and prefrom 3D printed polylactic acid backing layer. This MAP features rapidly dissolving tips and exhibits good mechanical properties and insertion capability with delivery efficiency compared to the conventional Daivonex ointment.

The effectiveness of this novel MAP was tested on Sprague–Dawley rats with imiquimod-induced psoriasis, demonstrating efficacy comparable to the marketed ointment. This innovative trilayer dissolving MAP represents a promising new local delivery system for calcipotriol, potentially revolutionizing psoriasis treatment by enhancing drug delivery and patient compliance.

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Materials

Calcipotriol monohydrate was kindly gifted by LEO Pharma A/S, Ballerup, Denmark. Poly(vinyl alcohol) (Mw = 9−10 kDa, 80% hydrolyzed) (PVA 10 K) was purchased from Sigma−Aldrich (Dorset, UK). Poly(vinylpyrrolidone) (PVP) (Mw = 58 kDa) was obtained from Ashland (Kidderminster, UK). Imiquimod cream (5%, Aldara) was obtained from MEDA Pharmaceuticals GmbH & Co. KG, Bad Homburg, Germany. Dovonex ointment was obtained from LEO Pharma A/S, Ballerup, Denmark. Purified water was obtained using a water purification system (Elga PURELAB DV 25, Veolian Water Systems, Ireland). All the other reagents used were of analytical grade

Xianbing Dai, Andi Dian Permana, Mingshan Li,, Muhammad Nur Amir, Ke Peng, Chunyang Zhang, Haodong Dai, Alejandro J Paredes, Lalitkumar K. Vora, and Ryan F. Donnelly, Molecular Pharmaceutics Article ASAP, DOI: 10.1021/acs.molpharmaceut.3c01223