In vitro Biological Activities of Azulene, Guaiazulene, and Sodium Guaiazulene Sulfonate and Its Application to Formulations through PEG-PCL Micelles

    Su In Park ,Kwang Won Lee ,Shinsung Park ,Moon Sam Shin
    Keywords: Azulene, Guaiazulene, Sodium Guaiazulene Sulfonate, Anti-inflammation, Anti-oxidation, PEG-PCL micelles ,

    Abstract

    Abstract
    Atopic dermatitis (AD) is developed by complex interplay of various factors such as skin barrier
    dysfunction, immunological derangement, and oxidative stress, so multipronged approaches are
    needed to treat AD. Azulene (AZ), guaiazulene (GA), and sodium guaiazulene sulfonate (GAS-Na) are
    known to have biological activities. This study aimed to evaluate the bioactivities of AZ, GA, GAS-Na from
    the perspective of AD treatment. Anti-inflammatory properties were estimated by measuring inhibitory
    effect on IL-6 and IL-8 production of TNF-╬▒ treated HaCaT cells via enzyme-linked immunosorbent assay
    (ELISA). Antioxidant properties were estimated by measuring DPPH and ABTS+ radical scavenging activity.
    Based on the experimental results that GA showed a wider range of anti-inflammatory and antioxidant
    effects than AZ and GAS-Na, we concluded that GA is the most suitable for treating both immunological
    derangement and oxidative stress. Furthermore, to overcome poor water solubility of GA hindering its
    application to various cosmetic formulations, we developed 1% of GA loaded PEG-PCL micelles and
    confirmed its stable characteristics via particle size, PDI, and zeta potential values. Through this study, we
    suggest the widespread use of GA for the treatment of AD.

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