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一种具有可持续药物释放特性的新型甲基丙烯酰壳聚糖水凝胶微针贴剂,用于有效治疗银屑病。

A Novel Methacryloyl Chitosan Hydrogel Microneedles Patch with Sustainable Drug Release Property for Effective Treatment of Psoriasis.

作者信息

Dai Panpan, Ge Xing, Sun Caixia, Jiang Hui, Zuo Wanchao, Wu Pengcheng, Liu Cong, Deng Shuyue, Yang Jun, Dai Jianjun, Ju Yanmin

机构信息

College of Pharmacy, China Pharmaceutical University, Nanjing, 211198, China.

Nanjing Institute for Food and Drug Control, Nanjing, 210038, China.

出版信息

Macromol Biosci. 2023 Dec;23(12):e2300194. doi: 10.1002/mabi.202300194. Epub 2023 Aug 9.

Abstract

Psoriasis is a chronic and recurrent skin disease that often requires long-term treatment, and topical transdermal drug delivery can reduce systemic side effects. However, it is still a challenge in efficient transdermal drug delivery for psoriasis treatment due to low penetration efficiency of most drugs and the abnormal skin conditions of psoriasis patients. Here, a safe and effective methacryloyl chitosan hydrogel microneedles (CSMA hMNs) patch is developed and served as a sustained drug release platform for the treatment of psoriasis. By systematically optimizing the CSMA preparation, CSMA hMNs with excellent morphological characteristics and strong mechanical properties (0.7 N needle ) are prepared with a concentration of only 3% (w/v) CSMA. As a proof-of-concept, methotrexate (MTX) and nicotinamide (NIC) are loaded into CSMA hMNs patch, which can produce a sustained drug release of 80% within 24 h in vitro. In vivo experiments demonstrated that the CSMA hMNs patch can effectively inhibit the skin thickening and spleen enlargement of psoriatic mice and has a good biosafety profile at sufficient therapeutic doses. This study provides a new idea for the preparation of hMN systems using modified CS or other biocompatible materials and offers an effective therapeutic option for psoriasis treatment.

摘要

银屑病是一种慢性复发性皮肤病,常需长期治疗,局部透皮给药可减少全身副作用。然而,由于大多数药物的渗透效率低以及银屑病患者的皮肤状况异常,高效的透皮给药治疗银屑病仍是一项挑战。在此,开发了一种安全有效的甲基丙烯酰壳聚糖水凝胶微针(CSMA hMNs)贴片,并将其作为治疗银屑病的持续药物释放平台。通过系统优化CSMA的制备,以仅3%(w/v)的CSMA浓度制备出具有优异形态特征和强机械性能(0.7 N针)的CSMA hMNs。作为概念验证,将甲氨蝶呤(MTX)和烟酰胺(NIC)负载到CSMA hMNs贴片中,其在体外24小时内可实现80%的持续药物释放。体内实验表明,CSMA hMNs贴片可有效抑制银屑病小鼠的皮肤增厚和脾脏肿大,且在足够治疗剂量下具有良好的生物安全性。本研究为使用改性壳聚糖或其他生物相容性材料制备hMN系统提供了新思路,并为银屑病治疗提供了一种有效的治疗选择。

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