Cargando…

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

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 c...

Descripción completa

Detalles Bibliográficos
Autores principales: Syed Azhar, Sharifah Nurfadhlin Afifah, Ashari, Siti Efliza, Salim, Norazlinaliza
Formato: Online Artículo Texto
Lenguaje:English
Publicado: Dove Medical Press 2018
Materias:
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC6198893/
https://www.ncbi.nlm.nih.gov/pubmed/30410332
http://dx.doi.org/10.2147/IJN.S171532
_version_ 1783365038019444736
author Syed Azhar, Sharifah Nurfadhlin Afifah
Ashari, Siti Efliza
Salim, Norazlinaliza
author_facet Syed Azhar, Sharifah Nurfadhlin Afifah
Ashari, Siti Efliza
Salim, Norazlinaliza
author_sort Syed Azhar, Sharifah Nurfadhlin Afifah
collection PubMed
description 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 IC(50) (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.
format Online
Article
Text
id pubmed-6198893
institution National Center for Biotechnology Information
language English
publishDate 2018
publisher Dove Medical Press
record_format MEDLINE/PubMed
spelling pubmed-61988932018-11-08 Development of a kojic monooleate-enriched oil-in-water nanoemulsion as a potential carrier for hyperpigmentation treatment Syed Azhar, Sharifah Nurfadhlin Afifah Ashari, Siti Efliza Salim, Norazlinaliza Int J Nanomedicine Original Research 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 IC(50) (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. Dove Medical Press 2018-10-15 /pmc/articles/PMC6198893/ /pubmed/30410332 http://dx.doi.org/10.2147/IJN.S171532 Text en © 2018 Syed Azhar et al. This work is published and licensed by Dove Medical Press Limited The full terms of this license are available at https://www.dovepress.com/terms.php and incorporate the Creative Commons Attribution – Non Commercial (unported, v3.0) License (http://creativecommons.org/licenses/by-nc/3.0/). By accessing the work you hereby accept the Terms. Non-commercial uses of the work are permitted without any further permission from Dove Medical Press Limited, provided the work is properly attributed.
spellingShingle Original Research
Syed Azhar, Sharifah Nurfadhlin Afifah
Ashari, Siti Efliza
Salim, Norazlinaliza
Development of a kojic monooleate-enriched oil-in-water nanoemulsion as a potential carrier for hyperpigmentation treatment
title 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_short 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
topic Original Research
url https://www.ncbi.nlm.nih.gov/pmc/articles/PMC6198893/
https://www.ncbi.nlm.nih.gov/pubmed/30410332
http://dx.doi.org/10.2147/IJN.S171532
work_keys_str_mv AT syedazharsharifahnurfadhlinafifah developmentofakojicmonooleateenrichedoilinwaternanoemulsionasapotentialcarrierforhyperpigmentationtreatment
AT asharisitiefliza developmentofakojicmonooleateenrichedoilinwaternanoemulsionasapotentialcarrierforhyperpigmentationtreatment
AT salimnorazlinaliza developmentofakojicmonooleateenrichedoilinwaternanoemulsionasapotentialcarrierforhyperpigmentationtreatment