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舒芬太尼聚合物溶解微针对雄性小鼠热板法的镇痛作用。

Anti-Nociceptive Effect of Sufentanil Polymeric Dissolving Microneedle on Male Mice by Hot Plate Technique.

机构信息

Department of Pharmacology, School of Medicine, Zanjan University of Medical Sciences, Zanjan, Iran.

Department of Pharmaceutical Biomaterials, Tehran University of Medical Sciences, Tehran, Iran.

出版信息

Iran Biomed J. 2024 Jul 1;28(4):192-205. doi: 10.61186/ibj.4062.

Abstract

BACKGROUND

Despite the widespread use of opioids to manage severe pain, its systemic administration results in side effects. Among the subcutaneous and transdermal drug delivery systems developed to deal with adverse effects, microneedles have drawn attention due to their rapid action, high drug bioavailability, and improved permeability. Sufentanil (SUF) is an effective injectable opioid for treating severe pain. In this study, we investigated the analgesic effects of SUF using dissolvable microneedles.

METHODS

SUF polymeric dissolvable microneedles were constructed through the mold casting method and characterized by SEM and FTIR analysis. Its mechanical strength was also investigated using a texture analyzer. Fluorescence microscopy was applied in vitro to measure the penetration depth of microneedle arrays. Irritation and microchannel closure time, drug release profile, and hemocompatibility test were conducted for the validation of microneedle efficiency. Hot plate test was also used to investigate the analgesic effect of microneedle in an animal model.

RESULTS

Local administration of SUF via dissolving microneedles had an effective analgesic impact. One hour after administration, there was no significant difference between the subcutaneous and the microneedle groups, and the mechanical properties were within acceptable limits.

CONCLUSION

Microneedling is an effective strategy in immediate pain relief compared to the traditional methods.

摘要

背景

尽管阿片类药物被广泛用于治疗重度疼痛,但全身给药会产生副作用。在开发用于应对不良反应的皮下和透皮药物输送系统中,由于其快速作用、高药物生物利用度和改善的通透性,微针引起了关注。舒芬太尼(SUF)是一种用于治疗重度疼痛的有效注射用阿片类药物。在这项研究中,我们使用可溶解微针研究了 SUF 的镇痛作用。

方法

通过模铸法构建 SUF 聚合物可溶解微针,并通过 SEM 和 FTIR 分析进行表征。还使用质地分析仪研究了其机械强度。荧光显微镜用于体外测量微针阵列的穿透深度。进行了刺激性和微通道闭合时间、药物释放曲线和血液相容性测试,以验证微针的效率。还使用热板试验研究了动物模型中微针的镇痛效果。

结果

通过溶解微针局部给予 SUF 具有有效的镇痛作用。给药后 1 小时,皮下组和微针组之间没有显著差异,机械性能在可接受的范围内。

结论

与传统方法相比,微针在即时缓解疼痛方面是一种有效的策略。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/3f50/11444482/4bb3514a8072/ibj-28-192-g001.jpg

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