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Lipase-Catalyzed Epigallocatechin Gallate-Based Polymer for Long-Term Transdermal Administration

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Abstract

Epigallocatechin gallate (EGCG) is an antioxidant agent with many advantageous pharmaceutical properties such as anti-cancer, anti-virus, and anti-oxidative activities with high efficacies and few side effects. However, its’ in vivo instability hinders its practical use. Therefore, this study aimed to synthesize a polymer film that can stably administer EGCG over long periods. The flexible polymer film was synthesized from EGCG and tetraethylene glycol adipate divinyl ester by lipase-catalyzed polymerization. It was confirmed that EGCG conversions and the molecular weights of the polymer were influenced by the reaction conditions such as reaction temperature, lipase concentration, and the substrate concentration. Under acidic conditions, the ester linkages of the polymer gradually degrade to release EGCG for more than 4 days without decreasing its anti-oxidative activity. A permeability experiment using a skin model membrane to assess the utilization of EGCG in transdermal applications showed that the EGCG released from the degradation of the polymer gradually permeates the membrane. These results suggest that the prepared EGCG-based polymer film has the potential for the long-term transdermal administration of EGCG.

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Acknowledgements

We would like to thank Dr. Sachi Shibata (Fukuyama University) for assistance with the cytotoxicity study, Dr. Choshi and Dr. Nishiyama (Fukuyama University) for assistance with the NMR analyses, and Dr. Yamaguchi (Fukuyama University) for the assistance with microplate reader. This work was supported by a JSPS Grant-in-Aid for JSPS Research Fellow (Grant Number 17J40043).

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Authors and Affiliations

  1. Research Center for Green Science, Fukuyama University, 1 Sanzo, Gakuen-cho, Fukuyama, 729-0292, Hiroshima, Japan

    Sachiko Nitta & Hiroyuki Iwamoto

  2. Department of Biotechnology, Fukuyama University, Fukuyama, 729-0292, Hiroshima, Japan

    Hiroyuki Iwamoto

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  1. Sachiko Nitta
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SN wrote the main manuscript. Both authors reviewed the manuscript.

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Correspondence to Sachiko Nitta.

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Nitta, S., Iwamoto, H. Lipase-Catalyzed Epigallocatechin Gallate-Based Polymer for Long-Term Transdermal Administration. J Polym Environ 31, 4421–4429 (2023). https://doi.org/10.1007/s10924-023-02872-4

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