Li Xing,Liang Kaili,Dong Yingying,Li Shen,Gao Zhengnan,Wang Qing
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
Nan Longyi,Song Haoyuan,Wang Haijun,Mi Ru,Wang Xiaoxu,Fang Liang
The aim of this study was to design a tulobuterol (TUL) patch with good penetration behavior and mechanical properties. Particular attention was paid to the effect of transdermal permeation enhancers on the release process of metal ligand-based acrylic pressure-sensitive adhesive (AA-NAT/Fe 3+ ). The type and dosage of the enhancers were screened by in vitro transdermal penetration in rat skin. The optimized formulation was evaluated in a pharmacokinetic study in rats. Furthermore, the molecular mechanism by which Azone (AZ) improves the release rate of TUL from AA-NAT/Fe 3+ was investigated by FT-IR, shear strength test, rheological study, and molecular simulation. As a result, the optimized formula using AA-NAT/Fe 3+ showed better mechanical properties compared to commercial products. Meanwhile, the AUC 0-t and C max of the optimized patch were 1045 ± 89 ng/mL·h and 106.8 ± 28.5 ng/mL, respectively, which were not significantly different from those of the commercial product. In addition, AZ increased the mobility of the pressure-sensitive adhesive (PSA) rather than decreasing the drug-PSA interaction, which was the main factor in enhancing TUL release from the patch. In conclusion, a TUL transdermal drug delivery patch was successfully developed using metal-coordinated PSA, and a reference was provided for the design of metal-coordinated acrylic PSA for transdermal patch delivery applications. Graphical Abstract
Yuyu Liang,Bijun Liu,Xiang Li,Shufeng Zhao,Qingye Zhou,Chenchen Yuan,Zeng Huang,Jun Tu,Xingliang Li
Azone, a commercially available amide compound widely used in pharmaceuticals and cosmetics, was investigated for its potential application in nuclear fuel separation. As a green extractant composed solely of carbon, hydrogen, oxygen, and nitrogen, it leaves no residue upon incineration. A comprehensive investigation was conducted to extract uranium selectively over thorium in nitric acid medium, using Azone as an extractant. The extraction behavior, kinetics, and thermodynamics of Azone were systematically examined and compared with those of tri-n-butyl phosphate (TBP). The results show that Azone in trimethylbenzene achieves uranium U(VI) extraction efficiency comparable to that of TBP, offering a significantly higher separation factor due to its near-zero extraction of Th(IV). Moreover, Azone exhibits favorable physicochemical properties, including higher thermal stability and a lower tendency for third-phase formation compared to TBP. The extraction mechanism was elucidated through UV-vis titration and single-crystal X-ray diffraction, confirming coordination between the amide carbonyl oxygen and the uranyl ion. In conclusion, Azone represents a highly promising and efficient extractant for U(VI) recovery in thorium-based fuel cycles.
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