Development of a kojic monooleate-enriched oil-in-water nanoemulsion as a potential carrier for hyperpigmentation treatment

Sharifah Nurfadhlin Afifah Syed Azhar, Siti Efliza Ashari, Norazlinaliza Salim Integrated Chemical BioPhysics Research, Faculty of Science, Universiti Putra Malaysia, Serdang, Selangor, Malaysia Introduction: Kojic monooleate (KMO) is an ester derived from a fungal metabolite of kojic acid with mo...

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Autores principales:	Syed Azhar SNA, Ashari SE, Salim N
Formato:	article
Lenguaje:	EN
Publicado:	Dove Medical Press 2018
Materias:	kojic monooleate anti-tyrosinase hyperpigmentation nanocosmeceutical D-optimal mixture experimental design Medicine (General) R5-920
Acceso en línea:	https://doaj.org/article/d72903b2bb634e3bb3788fdc25f8f7d1
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spelling	oai:doaj.org-article:d72903b2bb634e3bb3788fdc25f8f7d12021-12-02T07:37:12ZDevelopment of a kojic monooleate-enriched oil-in-water nanoemulsion as a potential carrier for hyperpigmentation treatment1178-2013https://doaj.org/article/d72903b2bb634e3bb3788fdc25f8f7d12018-10-01T00:00:00Zhttps://www.dovepress.com/development-of-a-kojic-monooleate-enriched-oil-in-water-nanoemulsion-a-peer-reviewed-article-IJNhttps://doaj.org/toc/1178-2013Sharifah Nurfadhlin Afifah Syed Azhar, Siti Efliza Ashari, Norazlinaliza Salim Integrated Chemical BioPhysics Research, Faculty of Science, Universiti Putra Malaysia, Serdang, Selangor, Malaysia Introduction: Kojic monooleate (KMO) is an ester derived from a fungal metabolite of kojic acid with monounsaturated fatty acid, oleic acid, which contains tyrosinase inhibitor to treat skin disorders such as hyperpigmentation. In this study, KMO was formulated in an oil-in-water nanoemulsion as a carrier for better penetration into the skin.Methods: The nanoemulsion was prepared by using high and low energy emulsification technique. D-optimal mixture experimental design was generated as a tool for optimizing the composition of nanoemulsions suitable for topical delivery systems. Effects of formulation variables including KMO (2.0%–10.0% w/w), mixture of castor oil (CO):lemon essential oil (LO; 9:1) (1.0%–5.0% w/w), Tween 80 (1.0%–4.0% w/w), xanthan gum (0.5%–1.5% w/w), and deionized water (78.8%–94.8% w/w), on droplet size as a response were determined.Results: Analysis of variance showed that the fitness of the quadratic polynomial fits the experimental data with F-value (2,479.87), a low P-value (P<0.0001), and a nonsignificant lack of fit. The optimized formulation of KMO-enriched nanoemulsion with desirable criteria was KMO (10.0% w/w), Tween 80 (3.19% w/w), CO:LO (3.74% w/w), xanthan gum (0.70% w/w), and deionized water (81.68% w/w). This optimum formulation showed good agreement between the actual droplet size (110.01 nm) and the predicted droplet size (111.73 nm) with a residual standard error <2.0%. The optimized formulation with pH values (6.28) showed high conductivity (1,492.00 µScm-1) and remained stable under accelerated stability study during storage at 4°C, 25°C, and 45°C for 90 days, centrifugal force as well as freeze–thaw cycles. Rheology measurement justified that the optimized formulation was more elastic (shear thinning and pseudo-plastic properties) rather than demonstrating viscous characteristics. In vitro cytotoxicity of the optimized KMO formulation and KMO oil showed that IC50 (50% inhibition of cell viability) value was >100 µg/mL.Conclusion: The survival rate of 3T3 cell on KMO formulation (54.76%) was found to be higher compared to KMO oil (53.37%) without any toxicity sign. This proved that the KMO formulation was less toxic and can be applied for cosmeceutical applications. Keywords: kojic monooleate, anti-tyrosinase, hyperpigmentation, nano-cosmeceutical, D-optimal mixture experimental designSyed Azhar SNAAshari SESalim NDove Medical Pressarticlekojic monooleateanti-tyrosinasehyperpigmentationnanocosmeceuticalD-optimal mixture experimental designMedicine (General)R5-920ENInternational Journal of Nanomedicine, Vol Volume 13, Pp 6465-6479 (2018)
institution	DOAJ
collection	DOAJ
language	EN
topic	kojic monooleate anti-tyrosinase hyperpigmentation nanocosmeceutical D-optimal mixture experimental design Medicine (General) R5-920
spellingShingle	kojic monooleate anti-tyrosinase hyperpigmentation nanocosmeceutical D-optimal mixture experimental design Medicine (General) R5-920 Syed Azhar SNA Ashari SE Salim N Development of a kojic monooleate-enriched oil-in-water nanoemulsion as a potential carrier for hyperpigmentation treatment
description	Sharifah Nurfadhlin Afifah Syed Azhar, Siti Efliza Ashari, Norazlinaliza Salim Integrated Chemical BioPhysics Research, Faculty of Science, Universiti Putra Malaysia, Serdang, Selangor, Malaysia Introduction: Kojic monooleate (KMO) is an ester derived from a fungal metabolite of kojic acid with monounsaturated fatty acid, oleic acid, which contains tyrosinase inhibitor to treat skin disorders such as hyperpigmentation. In this study, KMO was formulated in an oil-in-water nanoemulsion as a carrier for better penetration into the skin.Methods: The nanoemulsion was prepared by using high and low energy emulsification technique. D-optimal mixture experimental design was generated as a tool for optimizing the composition of nanoemulsions suitable for topical delivery systems. Effects of formulation variables including KMO (2.0%–10.0% w/w), mixture of castor oil (CO):lemon essential oil (LO; 9:1) (1.0%–5.0% w/w), Tween 80 (1.0%–4.0% w/w), xanthan gum (0.5%–1.5% w/w), and deionized water (78.8%–94.8% w/w), on droplet size as a response were determined.Results: Analysis of variance showed that the fitness of the quadratic polynomial fits the experimental data with F-value (2,479.87), a low P-value (P<0.0001), and a nonsignificant lack of fit. The optimized formulation of KMO-enriched nanoemulsion with desirable criteria was KMO (10.0% w/w), Tween 80 (3.19% w/w), CO:LO (3.74% w/w), xanthan gum (0.70% w/w), and deionized water (81.68% w/w). This optimum formulation showed good agreement between the actual droplet size (110.01 nm) and the predicted droplet size (111.73 nm) with a residual standard error <2.0%. The optimized formulation with pH values (6.28) showed high conductivity (1,492.00 µScm-1) and remained stable under accelerated stability study during storage at 4°C, 25°C, and 45°C for 90 days, centrifugal force as well as freeze–thaw cycles. Rheology measurement justified that the optimized formulation was more elastic (shear thinning and pseudo-plastic properties) rather than demonstrating viscous characteristics. In vitro cytotoxicity of the optimized KMO formulation and KMO oil showed that IC50 (50% inhibition of cell viability) value was >100 µg/mL.Conclusion: The survival rate of 3T3 cell on KMO formulation (54.76%) was found to be higher compared to KMO oil (53.37%) without any toxicity sign. This proved that the KMO formulation was less toxic and can be applied for cosmeceutical applications. Keywords: kojic monooleate, anti-tyrosinase, hyperpigmentation, nano-cosmeceutical, D-optimal mixture experimental design
format	article
author	Syed Azhar SNA Ashari SE Salim N
author_facet	Syed Azhar SNA Ashari SE Salim N
author_sort	Syed Azhar SNA
title	Development of a kojic monooleate-enriched oil-in-water nanoemulsion as a potential carrier for hyperpigmentation treatment
title_short	Development of a kojic monooleate-enriched oil-in-water nanoemulsion as a potential carrier for hyperpigmentation treatment
title_full	Development of a kojic monooleate-enriched oil-in-water nanoemulsion as a potential carrier for hyperpigmentation treatment
title_fullStr	Development of a kojic monooleate-enriched oil-in-water nanoemulsion as a potential carrier for hyperpigmentation treatment
title_full_unstemmed	Development of a kojic monooleate-enriched oil-in-water nanoemulsion as a potential carrier for hyperpigmentation treatment
title_sort	development of a kojic monooleate-enriched oil-in-water nanoemulsion as a potential carrier for hyperpigmentation treatment
publisher	Dove Medical Press
publishDate	2018
url	https://doaj.org/article/d72903b2bb634e3bb3788fdc25f8f7d1
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Development of a kojic monooleate-enriched oil-in-water nanoemulsion as a potential carrier for hyperpigmentation treatment

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