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实验性诱导银屑病模型中载有氯倍他索的微针贴剂与丙酸氯倍他索软膏的开发及对比分析

Development and comparative analysis of clobetasol-loaded microneedle patches versus clobetasol propionate ointment in experimental induced-psoriasis model.

作者信息

Bazargani Zohreh, Khorram Mohammad, Zomorodian Kamiar, Ghahartars Mehdi, Omidifar Navid

机构信息

Department of Chemical Engineering, School of Chemical and Petroleum Engineering, Shiraz University, Shiraz 71348-51154, Iran.

Department of Chemical Engineering, School of Chemical and Petroleum Engineering, Shiraz University, Shiraz 71348-51154, Iran.

出版信息

Int J Pharm. 2025 Apr 15;674:125423. doi: 10.1016/j.ijpharm.2025.125423. Epub 2025 Mar 10.

Abstract

The utilization of dissolvable microneedles (MNs) is a promising and cutting-edge approach to drug delivery for the treatment of psoriasis, an autoimmune skin disorder characterized by the appearance of red, scaly patches on the skin. This study presents the development of a dissolving MN patch made of polyvinylpyrrolidone for the purpose of delivering Clobetasol 17-Propionate through the skin. The MN patches were evaluated for their physical characteristics, including morphology, solubility, strength, and ability to penetrate the skin. This evaluation was conducted on both unloaded and drug-loaded MN patches to determine their suitability for future applications. The manufacturing of 484 pyramidal-shaped tips, each measuring roughly 400 µm in height, was demonstrated by microscopy photographs. Compression tests revealed that the MN patch could endure a force greater than 1 N/needle while displacing around 300 µm, confirming the needle's ability to penetrate the stratum corneum. Following H&E staining, the penetration depth in mice skin was determined to be around 200 µm. The MN tips exhibited rapid drug release within a 10-minute timeframe, while the MN patch dissolved in the mice skin in roughly 20 min. An animal model was utilized to examine the effects of the produced patches on the treatment of psoriasis. Psoriasis was artificially induced in three groups of mice using imiquimod cream, applied for eight consecutive days to evaluate the inhibitory effect of clobetasol on exacerbating the disease. This assessment was accomplished using two methods: applying clobetasol ointment and using CP-loaded MNs. This innovative drug delivery system demonstrated encouraging results in terms of quick and effective administration, highlighting the potential of dissolvable MNs for psoriasis treatment.

摘要

可溶微针(MNs)的应用是一种治疗银屑病很有前景的前沿给药方法。银屑病是一种自身免疫性皮肤病,其特征是皮肤上出现红色鳞屑斑块。本研究介绍了一种由聚乙烯吡咯烷酮制成的可溶微针贴片的研发情况,目的是通过皮肤递送丙酸氯倍他索。对微针贴片的物理特性进行了评估,包括形态、溶解性、强度以及穿透皮肤的能力。对未负载药物和负载药物的微针贴片均进行了此项评估,以确定它们在未来应用中的适用性。显微镜照片展示了484个金字塔形尖端的制造情况,每个尖端高度约为400微米。压缩试验表明,微针贴片在位移约300微米时能够承受大于1牛/针的力,证实了微针穿透角质层的能力。苏木精-伊红染色后,确定微针在小鼠皮肤中的穿透深度约为200微米。微针尖端在10分钟内迅速释放药物,而微针贴片在小鼠皮肤中大约20分钟溶解。利用动物模型研究了所制备的贴片对银屑病治疗的效果。用咪喹莫特乳膏在三组小鼠中人工诱导银屑病,连续涂抹八天,以评估氯倍他索对疾病加重的抑制作用。该评估通过两种方法完成:涂抹氯倍他索软膏和使用负载CP的微针。这种创新的给药系统在快速有效给药方面显示出令人鼓舞的结果,突出了可溶微针在银屑病治疗中的潜力。

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