Anjani Qonita Kurnia, McKenna Peter E, Larrañeta Eneko, Manesiotis Panagiotis, Luo Yidan, Adhami Masoud, Volpe-Zanutto Fabiana, Orr Gareth, Roussel Sabrina, Donnelly Ryan F
School of Pharmacy, Medical Biology Centre, Queen's University Belfast, 97 Lisburn Road, Belfast, BT9 7BL, UK.
School of Chemistry and Chemical Engineering, David Keir Building, 39-123 Stranmillis Road, Belfast, BT9 5 AG, UK.
Drug Deliv Transl Res. 2025 May 31. doi: 10.1007/s13346-025-01880-2.
Hydrogel-forming microarray patches (MAPs) offer a minimally invasive platform for transdermal drug delivery, enabling systemic absorption of active pharmaceutical ingredients. Unlike dissolving MAPs, which deposit their entire polymer matrix into the skin, hydrogel-forming MAPs remain intact upon removal, reducing polymer exposure while delivering higher drug doses than dissolving or coated MAPs. Moreover, they have demonstrated excellent biocompatibility and do not cause skin or systemic issues, even with repeated application in humans. This study assessed the leachable and extractable compounds from hydrogel-forming MAPs composed of Gantrez S-97, PEG 10,000, and sodium carbonate under various conditions. Under physiological conditions (37°C in water), minimal PEG 10,000 leaching (10.4 ± 2.0%) and negligible Gantrez S-97 extraction (< 2%) confirmed the hydrogel matrix's stability and safety. However, stress testing in DMSO at 70°C led to increased PEG 10,000 extraction (up to 32.9 ± 6.1%) and minor Gantrez S-97 degradation, likely due to ester hydrolysis. These findings highlight the robustness of hydrogel-forming MAPs, ensuring minimal systemic exposure to unbound polymers while maintaining effective drug delivery. The results support their potential for chronic therapeutic applications requiring repeated dosing. Further clinical studies are needed to validate these findings, facilitating regulatory approval and broader adoption across diverse medical applications.
形成水凝胶的微阵列贴片（MAPs）为透皮给药提供了一个微创平台，能够使活性药物成分实现全身吸收。与溶解型MAPs不同，溶解型MAPs会将其整个聚合物基质沉积到皮肤中，而形成水凝胶的MAPs在移除后仍保持完整，减少了聚合物暴露，同时比溶解型或包衣型MAPs能递送更高剂量的药物。此外，它们已证明具有出色的生物相容性，即使在人体中反复应用也不会引起皮肤或全身问题。本研究评估了在各种条件下由甘膦S - ninety-seven、聚乙二醇10000和碳酸钠组成的形成水凝胶的MAPs中可浸出和可萃取的化合物。在生理条件下（37℃水中），聚乙二醇10000的浸出极少（10.4±2.0%），甘膦S - ninety-seven的萃取可忽略不计（<2%），证实了水凝胶基质的稳定性和安全性。然而，在70℃的二甲基亚砜中进行应力测试导致聚乙二醇10000的萃取增加（高达32.9±6.1%）以及甘膦S - ninety-seven轻微降解，这可能是由于酯水解所致。这些发现突出了形成水凝胶的MAPs的稳健性，确保在维持有效药物递送的同时，全身对未结合聚合物的暴露最小。结果支持了它们在需要重复给药的慢性治疗应用中的潜力。需要进一步的临床研究来验证这些发现，以促进监管批准并在各种医疗应用中更广泛地采用。
