Citation: Bing Xie, Qi Jiang, Fang Zhu, Yaoyao Lai, Yueming Zhao, Wei He, Pei Yang. Transdermal delivery of amphotericin B using deep eutectic solvents for antifungal therapy[J]. Chinese Chemical Letters, ;2025, 36(5): 110508. doi: 10.1016/j.cclet.2024.110508 shu

Transdermal delivery of amphotericin B using deep eutectic solvents for antifungal therapy

Bing Xie ^{a, 1} ,
Qi Jiang ^{a, 1} ,
Fang Zhu ^{b, 1} ,
Yaoyao Lai ^a ,
Yueming Zhao ^{b, *,} ,
Wei He ^{a, c, *,} ,
Pei Yang ^{d, *,}

a.
School of Pharmacy, China Pharmaceutical University, Nanjing 211198, China
b.
Department of Respiratory and Critical Medicine, Nanjing First Hospital, Nanjing Medical University, Nanjing 210000, China
c.
Key Laboratory of Modern Preparation of TCM, Ministry of Education, Jiangxi University of Chinese Medicine, Nanchang 330004, China
d.
School of Science, China Pharmaceutical University, Nanjing 211198, China

sabrina-zym@163.com

weihe@cpu.edu.cn

yangpei@cpu.edu.cn

Received Date: 2 August 2024
Revised Date: 23 September 2024
Accepted Date: 25 September 2024
Available Online: 26 September 2024

Figures(4)

Candida albicans is one of the most common pathogens causing invasive fungal infections, with a mortality rate of up to 20%–50%. Amphotericin B (AmB), a biopharmaceutics classification system (BCS) IV drug, significantly inhibits Candida albicans. AmB is primarily administered via oral and intravenous infusion, but severe infusion adverse effects, nephrotoxicity, and potential hepatotoxicity limit its clinical application. Deep eutectic solvents (DESs), with excellent solubilization ability and skin permeability, are attractive for transdermal delivery. Herein, we used DESs to deliver AmB for antifungal therapy transdermally. We first prepared and characterized DESs with different stoichiometric ratios of choline (Ch) and geranate (Ge). DESs increased the solubility of AmB by a thousand-fold. In vitro and in vivo, skin permeation studies indicated that DES_1:2 (Ch and Ge in 1:2 ratio) had the most outstanding penetration and delivered fluorescence dye to the dermis layer. Then, DES_1:2-AmB was prepared and in vitro antifungal tests demonstrated that DES_1:2-AmB had superior antifungal effects compared to AmB and DES_1:2. Furthermore, DES_1:2-AmB was skin-irritating and biocompatible. In conclusion, DES-AmB provides a new and effective therapeutic solution for fungal infections.
- Amphotericin B,
- Deep eutectic solvents,
- Transdermal delivery,
- Candida albicans,
- Fungal infections
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