Dissolving microarray patches loaded with a rotigotine nanosuspension: A potential alternative to Neupro® patch

Parkinson’s disease (PD), affecting about ten million people globally, presents a significant health challenge. Rotigotine (RTG), a dopamine agonist, is currently administered as a transdermal patch (Neupro®) for PD treatment, but the daily application can be burdensome and cause skin irritation. This study introduces a combinatorial approach of dissolving microarray patch (MAP) and nanosuspension (NS) for the transdermal delivery of RTG, offering an alternative to Neupro®. The RTG-NS was formulated using a miniaturized media milling method, resulting in a nano-formulation with a mean particle size of 274.09 ± 7.43 nm, a PDI of 0.17 ± 0.04 and a zeta potential of −15.24 ± 2.86 mV.

Highlights

• An alternative approach to deliver rotigotine via microarray patch was introduced.
• Dose per unit area can be improved by using such approach in comparison to Neupro®.
• A single 24 h application can provide therapeutic rotigotine levels to at least 2 days.
• Unnecessarily high rotigotine plasma level may be avoided by using such approach.

The in vitro dissolution study revealed an enhanced dissolution rate of the RTG-NS in comparison to the coarse RTG powder, under sink condition. The RTG-NS MAPs, containing a drug layer and a ‘drug-free’ supporting baseplate, have a drug content of 3.06 ± 0.15 mg/0.5 cm² and demonstrated greater amount of drug delivered per unit area (∼0.52 mg/0.5 cm²) than Neupro® (∼0.20 mg/1 cm²) in an ex vivo Franz cell study using full-thickness neonatal porcine skin.

The in vivo pharmacokinetic studies demonstrated that RTG-NS MAPs, though smaller (2 cm² for dissolving MAPs and 6 cm² for Neupro®), delivered drug levels comparable to Neupro®, indicating higher efficiency per unit area. This could potentially avoid unnecessarily high plasma levels after the next dose at 24 h, highlighting the benefits of dissolving MAPs over conventional transdermal patches in PD treatment.

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Materials

RTG (MW = 315.5 Da) (purity ≥99%) was purchased from Cangzhou Enke Pharma-tech Co., Ltd. (Cangzhou, China). Poly(vinyl alcohol) (PVA) (MW = 9–10 kDa, 80% hydrolysed), poly(vinyl pyrrolidone) (PVP) (MW = 360 kDa) and PVP (MW = 58 kDa) were purchased from Sigma–Aldrich (Dorset, UK). Glycerol AnalaR NORMAPUR (purity 99.5%) was purchased from VWR International UK (Leicestershire, UK). Ceramic beads were purchased from Chemco Advance Material (Suzhou, China).

Yaocun Li, Jiawen Wang, Lalitkumar K. Vora, Akmal Hidayat Bin Sabri, Mary B. McGuckin, Alejandro J. Paredes, Ryan F. Donnelly, Dissolving microarray patches loaded with a rotigotine nanosuspension: A potential alternative to Neupro® patch, Journal of Controlled Release, Volume 372, 2024, Pages 304-317, ISSN 0168-3659, https://doi.org/10.1016/j.jconrel.2024.06.039.

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