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一种用于透皮给药的离子导入辅助释放特比萘芬盐酸盐水凝胶贴剂的制备与评价

The Preparation and Evaluation of a Hydrochloride Hydrogel Patch with an Iontophoresis-Assisted Release of Terbinafine for Transdermal Delivery.

作者信息

Li Mengfei, Chen Xinghao, Su Xiangxiang, Gao Wenyan

机构信息

School of Pharmacy, Hangzhou Medical College, Hangzhou 310013, China.

出版信息

Gels. 2024 Jul 12;10(7):456. doi: 10.3390/gels10070456.

DOI:10.3390/gels10070456
PMID:39057479
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC11275388/
Abstract

Terbinafine hydrochloride (TEB) is a broad-spectrum antifungal medication commonly used to treat fungal infections of the skin. This study designed a hydrogel patch assisted by an iontophoresis system to enhance the transdermal permeability of TEB, enabling deeper penetration into the skin layers. The influences of current intensity, pH levels, and drug concentration on the TEB hydrogel patch's permeability were explored using an adaptive ion electroosmosis system. The pharmacokinetic profile, facilitated by iontophoresis for transdermal permeation, was analyzed through the application of microdialysis technology. Scanning electron microscopy and transmission electron microscopy were employed to assess the impact of ion electroosmotic systems on skin integrity. The cumulative drug accumulation within 8 h of the TEB hydrogel patches, assisted by iontophoresis, was 2.9 and 7.9 times higher than without iontophoresis assistance and TEB cream in the control group, respectively. TEB hydrogel patches assisted by iontophoresis can significantly increase the permeability of TEB, and the AUC was 3.4 and 5.4 times higher, while the C was 4.2 and 7.3 times higher than the TEB hydrogel patches without iontophoresis, respectively. This system has no significant impact on deep-layer cells. This system may offer a safe and effective clinical strategy for the local treatment of deep antifungal infections.

摘要

盐酸特比萘芬(TEB)是一种常用的广谱抗真菌药物,用于治疗皮肤真菌感染。本研究设计了一种在离子导入系统辅助下的水凝胶贴片,以提高TEB的透皮渗透性,使其能够更深地渗透到皮肤层。使用自适应离子电渗系统探讨了电流强度、pH值和药物浓度对TEB水凝胶贴片渗透性的影响。通过应用微透析技术分析了离子导入促进透皮渗透的药代动力学特征。采用扫描电子显微镜和透射电子显微镜评估离子电渗系统对皮肤完整性的影响。在离子导入辅助下,TEB水凝胶贴片在8小时内的累积药物蓄积量分别比对照组中无离子导入辅助的情况和TEB乳膏高2.9倍和7.9倍。离子导入辅助的TEB水凝胶贴片可显著提高TEB的渗透性,其曲线下面积(AUC)分别比无离子导入的TEB水凝胶贴片高3.4倍和5.4倍,而峰浓度(C)分别高4.2倍和7.3倍。该系统对深层细胞无显著影响。该系统可能为深部真菌感染的局部治疗提供一种安全有效的临床策略。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/39e6/11275388/617b8ada4261/gels-10-00456-g006.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/39e6/11275388/14ab4fb84ee6/gels-10-00456-g001.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/39e6/11275388/937c4fd51baf/gels-10-00456-g002.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/39e6/11275388/f2b3cb967c04/gels-10-00456-g003.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/39e6/11275388/f62a49344a7d/gels-10-00456-g004.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/39e6/11275388/1cb253d06ba4/gels-10-00456-g005.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/39e6/11275388/617b8ada4261/gels-10-00456-g006.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/39e6/11275388/14ab4fb84ee6/gels-10-00456-g001.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/39e6/11275388/937c4fd51baf/gels-10-00456-g002.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/39e6/11275388/f2b3cb967c04/gels-10-00456-g003.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/39e6/11275388/f62a49344a7d/gels-10-00456-g004.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/39e6/11275388/1cb253d06ba4/gels-10-00456-g005.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/39e6/11275388/617b8ada4261/gels-10-00456-g006.jpg

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