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