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Cardamonin-loaded liposomal formulation for improving percutaneous penetration and follicular delivery for androgenetic alopecia

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Abstract

Androgenic alopecia (AGA) has a considerable impact on the physical and mental health of patients. Nano preparations have apparent advantages and high feasibility in the treatment of AGA. Cardamonin (CAR) has a wide range of pharmacological activities, but it has the problems of poor solubility in water and low bioavailability. There are few, if any, researches on the use of nano-loaded CAR to improve topical skin delivery of AGA. In this study, a CAR-loaded liposomal formulation (CAR@Lip and CAR@Lip Gel) was developed and characterized. The prepared CAR@Lip exhibited a uniform and rounded vesicle in size. CAR@Lip and CAR@Lip Gel can significantly improve the cumulative release of CAR. Additionally, CAR@Lip can obviously promote the proliferation and migration of human dermal papilla cells (hDPCs). Cell uptake revealed that the uptake of CAR@Lip significantly increased compared with the free drug. Furthermore, both CAR@Lip and CAR@Lip Gel groups could markedly improve the transdermal performance of CAR, and increase the topical content of the drug in the hair follicle compared with CAR. The ratchet effect of hair follicles could improve the skin penetration depth of nanoformulations. Notably, Anti-AGA tests in the mice showed that CAR@Lip and CAR@Lip Gel groups could promote hair growth, and accelerate the transition of hair follicles to the growth stage. The anti-androgen effect was revealed by regulating the expression of IGF-1, VEGF, KGF, and TGF-β, participating in SHH/Gli and Wnt/β-catenin pathways. Importantly, the nanoformulations had no obvious skin irritation. Thus, our study showed that CAR-loaded liposomal formulation has potential application in the treatment of AGA.

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Acknowledgements

We thank prof. Wei Wu from the School of Pharmacy, Fudan University, for providing P4 fluorescence probe.

Funding

This work was sponsored by Program for Shanghai High-Level Local University Innovation Team [SZY20220315].

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Authors and Affiliations

  1. School of Pharmacy, Shanghai University of Traditional Chinese Medicine, No.1200, Cai-lun Road, Pudong District, Shanghai, 201203, P.R. China

    Zhenda Liu, Xinyi Ai, Teng Guo & Nianping Feng

  2. School of Pharmaceutical Sciences, Zhengzhou University, Zhengzhou, Henan Province, China

    Zehui He

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  1. Zhenda Liu
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All authors contributed to the conception and design of this manuscript. The original draft of the manuscript, investigation, and formal analysis were performed by Zhenda Liu. The data was collected, processed, interpreted, and drafted by Zehui He and Xinyi Ai. Teng Guo wrote, reviewed, and edited the study. Nianping Feng supervised the study. All authors read and approved the final manuscript.

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Correspondence to Teng Guo or Nianping Feng.

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The study was reviewed and approved by the Experimental Animal Ethics Committee of Shanghai University of Traditional Chinese Medicine with registration numbers PZSHUTCM210723001 and PZSHUTCM210926005.

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Liu, Z., He, Z., Ai, X. et al. Cardamonin-loaded liposomal formulation for improving percutaneous penetration and follicular delivery for androgenetic alopecia. Drug Deliv. and Transl. Res. (2024). https://doi.org/10.1007/s13346-024-01519-8

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