Hyaluronic Acid-Based Dissolving Microneedle Patch Loaded with Methotrexate for Improved Treatment of Psoriasis,ACS Applied Materials & Interfaces

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Hyaluronic Acid-Based Dissolving Microneedle Patch Loaded with Methotrexate for Improved Treatment of Psoriasis
ACS Applied Materials & Interfaces ( IF 8.3 ) Pub Date : 2019-11-08 , DOI: 10.1021/acsami.9b15668
Hongyao Du ₁ , Pei Liu ₂ , Jinjin Zhu ₁ , Jiajia Lan ₁ , Yan Li ₁ , Lianbin Zhang ₂ , Jintao Zhu ₂ , Juan Tao ₁

Affiliation

Methotrexate (MTX) is one of the first-line treatments for moderate to severe psoriasis, while the side effects caused by injection and oral administration of MTX greatly restrict its clinical application. Transdermal drug delivery offers a desirable alternative to the conventional approaches, but the performances of the currently available skin penetration enhancement techniques are not so satisfactory. To address these limitations, we developed a dissolving microneedle (MN) patch made of hyaluronic acid (HA) with excellent water solubility, biocompatibility, biodegradability, and mechanical properties. The amount of MTX encapsulated in the needles of the patch could be controlled during the fabrication process for precise dosage. Interestingly, the MTX-loaded MNs successfully penetrated imiquimod (IMQ)-induced thickened epidermis in mice and delivered the drug intralesionally. Meanwhile, fast dissolution of HA endowed the MNs with operability for patients. We found that the MTX-loaded MNs not only showed well-maintained inhibitory effect in vitro but also alleviated the psoriasis-like skin inflammation in mice. Moreover, the MTX-loaded MNs were significantly more efficacious than taking the same dose of drug orally. Consequently, a higher oral dose of MTX was required for a comparable amelioration, which in turn increased its systemic toxicity. Taken together, the proposed MTX-loaded dissolving MN patch strategy provides a new opportunity for efficient and safe treatment of psoriasis.

中文翻译：

负载甲氨蝶呤的透明质酸可溶性微针贴剂改善牛皮癣的治疗

甲氨蝶呤（MTX）是中度至重度牛皮癣的一线治疗药物，而注射和口服MTX引起的副作用极大地限制了其临床应用。透皮药物递送提供了常规方法的理想替代方案，但是当前可用的皮肤渗透增强技术的性能并不令人满意。为了解决这些局限性，我们开发了由透明质酸（HA）制成的可溶性微针（MN）贴剂，具有出色的水溶性，生物相容性，生物降解性和机械性能。可以在制造过程中控制贴剂针头中所包封的MTX的量，以实现精确剂量。有趣的是，载有MTX的MNs成功穿透了咪喹莫特（IMQ）诱导的小鼠增厚表皮，并病灶内递送了药物。同时，HA的快速溶解赋予了MN患者可操作性。我们发现，载有MTX的MNs不仅在体外显示出良好的抑制作用，而且还减轻了小鼠的牛皮癣样皮肤炎症。此外，MTX负载的MN比口服相同剂量的药物有效得多。因此，要想获得同等的改善，就需要更高的口服MTX剂量，从而增加了其全身毒性。综上所述，建议的MTX-负载型溶解性MN贴剂策略为牛皮癣的有效，安全治疗提供了新的机会。HA的快速溶解使MN具有患者可操作性。我们发现，载有MTX的MNs不仅在体外显示出良好的抑制作用，而且还减轻了小鼠的牛皮癣样皮肤炎症。此外，MTX负载的MN比口服相同剂量的药物有效得多。因此，要想获得同等的改善，就需要更高的口服MTX剂量，从而增加了其全身毒性。综上所述，建议的MTX-负载型溶解性MN贴剂策略为牛皮癣的有效，安全治疗提供了新的机会。HA的快速溶解使MN具有患者可操作性。我们发现，载有MTX的MNs不仅在体外显示出良好的抑制作用，而且还减轻了小鼠的牛皮癣样皮肤炎症。此外，MTX负载的MN比口服相同剂量的药物有效得多。因此，要想获得同等的改善，就需要更高的口服MTX剂量，从而增加了其全身毒性。综上所述，建议的MTX-负载型溶解性MN贴剂策略为牛皮癣的有效，安全治疗提供了新的机会。与口服相同剂量的药物相比，MTX负载的MNs的功效明显更高。因此，要想获得同等的改善，就需要更高的口服MTX剂量，从而增加了其全身毒性。综上所述，建议的载有MTX的溶解性MN贴剂策略可为有效，安全地治疗牛皮癣提供新的机会。与口服相同剂量的药物相比，MTX负载的MNs的功效明显更高。因此，要想获得同等的改善，就需要更高的口服MTX剂量，从而增加了其全身毒性。综上所述，建议的MTX-负载型溶解性MN贴剂策略为牛皮癣的有效，安全治疗提供了新的机会。

更新日期：2019-11-08

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