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

IF 3.4 4区医学 Q2 PHARMACOLOGY & PHARMACY

AAPS PharmSciTech Pub Date : 2024-08-06 DOI:10.1208/s12249-024-02875-x

Xing Li, Kaili Liang, Yingying Dong, Shen Li, Zhengnan Gao, Qing Wang

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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.

Graphical Abstract

Abstract Image

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油酸和氮酮对左旋甲状腺素钠贴片释放和渗透过程的影响及作用模式

近年来，甲状腺疾病，尤其是甲状腺功能减退症的发病率大幅上升。本研究探讨了化学渗透增强（CPE）对左旋甲状腺素钠（L-T4）贴剂透皮渗透的影响和机制，发现油酸（OA）和阿宗（NZ）的组合对左旋甲状腺素钠（L-T4）的透皮渗透效果最好。结果表明，与单独使用相比，联合使用 OA 和 NZ 能显著提高 L-T4 的透皮渗透效果，这归因于两种机制：首先，OA 通过提高压敏胶（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，特别是促进了 L-T4 通过毛囊途径的渗透。这些最终制成的贴片不会对皮肤产生刺激或细胞毒性，对甲状腺功能减退症具有显著的治疗效果。这项研究有助于开发 L-T4 的透皮制剂。

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来源期刊

AAPS PharmSciTech 医学-药学

CiteScore

6.80

自引率

3.00%

发文量

264

审稿时长

2.4 months

期刊介绍： AAPS PharmSciTech is a peer-reviewed, online-only journal committed to serving those pharmaceutical scientists and engineers interested in the research, development, and evaluation of pharmaceutical dosage forms and delivery systems, including drugs derived from biotechnology and the manufacturing science pertaining to the commercialization of such dosage forms. Because of its electronic nature, AAPS PharmSciTech aspires to utilize evolving electronic technology to enable faster and diverse mechanisms of information delivery to its readership. Submission of uninvited expert reviews and research articles are welcomed.