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油酸和氮酮对左甲状腺素钠贴剂释放和渗透过程的影响及作用模式。

Effects and Action Mode of Oleic Acid and Azone on Release and Penetration Process of Levothyroxine Sodium Patches.

机构信息

Dalian University of Technology, No. 2 Linggong Road, Ganjingzi District, Dalian, 116024, Liaoning, P. R. China.

Central Hospital affiliated to University of Science and Technology, Dalian, 116021, P. R. China.

出版信息

AAPS PharmSciTech. 2024 Aug 6;25(6):180. doi: 10.1208/s12249-024-02875-x.

Abstract

In recent years, there has been a significant increase in the prevalence of thyroid diseases, particularly hypothyroidism. In this study, we investigated the impact and mechanisms of Chemical permeation enhancement(CPE) on transdermal permeation of levothyroxine sodium (L-T4) patches.We found that the combination of oleic acid (OA) and Azone (NZ) yielded the best transdermal permeation effect for L-T4.Subsequently, we also investigated the relevant propermeability mechanism.The results demonstrate that the combined application of OA and NZ significantly enhances the transdermal permeation of L-T4 compared to individual applications,it is attributed to two mechanisms: firstly, OA improves drug release by increasing the flowability of the pressure-sensitive adhesive (PSA) matrix; secondly, both OA and NZ act on the stratum corneum, especially facilitating L-T4 permeation through the hair follicle pathway. No skin irritation or cytotoxicity is observed with these final patches, which exhibit a remarkable therapeutic effect on hypothyroidism. this study contributes to the development of transdermal formulations of L-T4.

摘要

近年来,甲状腺疾病的患病率显著增加,特别是甲状腺功能减退症。在这项研究中,我们研究了化学渗透增强(CPE)对左甲状腺素钠(L-T4)贴片经皮渗透的影响和机制。我们发现,油酸(OA)和氮酮(NZ)的组合对 L-T4 具有最佳的经皮渗透效果。随后,我们还研究了相关的渗透性机制。结果表明,OA 和 NZ 的联合应用显著增强了 L-T4 的经皮渗透,与单独应用相比,这归因于两个机制:首先,OA 通过增加压敏胶(PSA)基质的流动性来改善药物释放;其次,OA 和 NZ 都作用于角质层,特别是促进 L-T4 通过毛囊途径渗透。这些最终的贴片没有皮肤刺激或细胞毒性,对甲状腺功能减退症有显著的治疗效果。这项研究为 L-T4 的经皮制剂的开发做出了贡献。

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