Cheng Lan, Zhang Yanhua, Xu Qian, Li Zheng, Liu Zulan, Dai Fangyin
State Key Laboratory of Resource Insects, Key Laboratory for Sericulture Biology and Genetic Breeding, Ministry of Agriculture and Rural Affairs, College of Sericulture, Textile and Biomass Sciences, Yibin Academy, Southwest University, Chongqing 400715, China.
Luoyang Central Hospital, No. 288 Zhongzhou middle road, Xigong district, Luoyang, Henan province, 471000, China.
Int J Pharm X. 2024 Dec 15;9:100312. doi: 10.1016/j.ijpx.2024.100312. eCollection 2025 Jun.
Systemic administration of methotrexate (MTX), widely regarded as one of the most effective treatments for psoriasis, poses significant challenges due to its high toxicity, limited solubility, and potential for adverse effects. Consequently, developing a topical form of MTX may offer a safer and more effective strategy for psoriasis management. Silk fibroin (SF), a protein-based biomacromolecule, has shown considerable promise as a nanocarrier for sustained and targeted drug delivery, owing to its exceptional physicochemical and biological properties. This study aimed to develop and characterize a novel drug delivery nanocarrier for MTX using SF nanoparticles modified with hyaluronic acid (HA) and to assess their potential for skin-targeted drug delivery with reduced transdermal permeation. The nanoparticles were thoroughly characterized, demonstrating a uniform particle size, high drug-loading capacity, pH sensitivity, and excellent slow-release properties. In vitro and in vivo experiments further indicated that these nanoparticles effectively reduced psoriasis-induced inflammatory responses, including erythema and scaling, by inhibiting keratinocyte proliferation and decreasing levels of pro-inflammatory cytokines. The inclusion of HA improved nanoparticle targeting, particularly through interactions with overexpressed CD44 proteins in psoriatic skin, resulting in enhanced methotrexate accumulation at the sites of inflammation and improved therapeutic efficacy. Our findings suggest that HA/SF nanoparticles loaded with MTX represent a promising, safe transdermal delivery system for the localized treatment of psoriasis.
甲氨蝶呤(MTX)的全身给药被广泛认为是治疗银屑病最有效的方法之一,但由于其高毒性、低溶解度和潜在的副作用,带来了重大挑战。因此,开发MTX的局部给药形式可能为银屑病的治疗提供一种更安全、有效的策略。丝素蛋白(SF)是一种基于蛋白质的生物大分子,由于其卓越的物理化学和生物学特性,作为一种用于持续和靶向给药的纳米载体显示出巨大的潜力。本研究旨在开发并表征一种使用透明质酸(HA)修饰的SF纳米颗粒作为MTX的新型药物递送纳米载体,并评估其用于皮肤靶向给药且减少经皮渗透的潜力。对纳米颗粒进行了全面表征,结果表明其粒径均匀、载药量高、具有pH敏感性且缓释性能优异。体外和体内实验进一步表明,这些纳米颗粒通过抑制角质形成细胞增殖和降低促炎细胞因子水平,有效减轻了银屑病引起的炎症反应,包括红斑和鳞屑。HA的加入改善了纳米颗粒的靶向性,特别是通过与银屑病皮肤中过表达的CD44蛋白相互作用,导致甲氨蝶呤在炎症部位的积累增加,治疗效果得到改善。我们的研究结果表明,负载MTX的HA/SF纳米颗粒是一种用于银屑病局部治疗的有前景的、安全的经皮给药系统。