Eco-friendly preparation, characterization, evaluation of anti-melanogenesis/antioxidant effect and in vitro/in vivo safety profile of kojic acid loaded niosome as skin lightener preparation

Abstract

In the current study, an ultrasonic approach (as green method) was utilized to prepared kojic acid niosome (kojisome) which aimed to increase the dermal delivery and improving anti-melanogenesis properties. The study’s findings demonstrated that increasing cholesterol enhanced the mean particle size from 68.333 ± 5.686 nm to 325.000 ± 15.099 nm and entrapment efficiency 0% to 39.341 ± 4.126% of the kojisome. Cholesterol may enhance the number and rigidity of bilayers that induced a size enhancement and entrapment efficiency. The skin permeability test revealed that kojisome gel had more kojic acid in dermal layers (437.563 ± 29.857 μg/cm² or 16.624 ± 1.379%) than kojic acid plain gel (161.290 ± 14.812 μg/cm² or 6.128 ± 0.672%). The niosome’s lipophilicity allowed for gradual penetration, possibly due to better contact with the skin layers. Also, the extended-release behavior of improved kojisome exhibited high safety profile and low side effect in In vitro cytotoxicity assay, dermal irritation test, and Histo-pathological evaluation. Furthermore, optimum kojisome inhibited melanin formation (53.093 ± 2.985% at 1000 µM) higher than free kojic acid (62.383 ± 1.958%) significantly (p < 0.05). In addition, Kojisome 6 inhibited L-dopa auto-oxidation greater extent (94.806 ± 2.411%) than pure kojic acid solution (72.953 ± 2.728%). Kojisome by delivering and targeting large amount of kojic acid on specific site causes high efficacy in inhibition of melanin synthesis. The observations of this study revealed that the produced kojisome might be used as a potential nano-vehicle for kojic acid dermal administration, thereby opening up innovative options for the treatment of hyperpigmentation problems.

Graphical abstract

Keywords:

• Kojic acid
• niosome
• anti-pigmentation
• antioxidant effect
• anti-melanogenesis

Acknowledgment

The authors would wish to express their sincere and special appreciation to research council of Mazandaran University of Medical Sciences, Sari, Iran, for their valuable and technical cooperation.

Disclosure statement

No potential conflict of interest was reported by the authors.

Additional information

Funding

This study was funded by a grant number 10517 from the Mazandaran University of Medical Sciences Research Council, Sari.