Development of nanoemulsion containing kojic acid ester for cosmeceutical application

Kojic acid (KA) and its derivatives such as kojic acid ester (KAE) are well-known tyrosinase inhibitor that widely used in food and cosmetic industries. The antityrosinase properties of these compounds known to be effective in the treatment of overproduction of melanin such as hyperpigmentation f...

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Main Author:	Syed Azhar, Sharifah Nurfadhlin Afifah
Format:	Thesis
Language:	English
Published:	2018
Subjects:	Emulsions Nanostructured materials - Analysis Phenol oxidase
Online Access:	http://psasir.upm.edu.my/id/eprint/83624/1/FS%202019%206%20-ir.pdf
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spelling	my-upm-ir.836242022-01-06T02:03:55Z Development of nanoemulsion containing kojic acid ester for cosmeceutical application 2018-11 Syed Azhar, Sharifah Nurfadhlin Afifah Kojic acid (KA) and its derivatives such as kojic acid ester (KAE) are well-known tyrosinase inhibitor that widely used in food and cosmetic industries. The antityrosinase properties of these compounds known to be effective in the treatment of overproduction of melanin such as hyperpigmentation for cosmeceutical applications. Kojic acid ester was used as the active ingredient and encapsulated in the nanoemulsion system. To design excellent formulation, the nanoemulsion containing kojic acid ester (KAE) was screened with different level of variables by using D-optimal experimental mixture design (MED), solubility determination in various oils and finally the preparation system was further developed. DOptimal Mixture Experimental Design (MED) was used for optimizing the composition of nanoemulsions suitable for topical delivery system. The optimized nanoemulsion containing kojic acid ester with desirable criteria was 10.00 % w/w of KAE, 3.19 % w/w of T80, 3.74 % w/w of castor oil: lemon essential oil (ratio 9: 1), 0.70 % w/w of xanthan gum and 81.68 % w/w of deionized water. This optimum nanoemulsion containing KAE showed suitable agreement between the actual droplet size (110.01 nm) and the predicted droplet size (111.73 nm). The residual standard error (RSE) value of nanoemulsion containing KAE was less than 2.0%. The optimized nanoemulsion containing KAE with pH value of 6.28 showed high conductivity value (1492.00 μScmˉ1) indicated that oil-in-water nanoemulsion was obtained. The nanoemulsion remained stable (no phase separation was observed) under accelerated stability during storage at 4°C, 25°C and 45°C within 90 days, centrifugal force as well as freeze-thaw cycles. Rheology measurement justified that the optimized nanoemulsion containing KAE was more elastic (shear thinning and pseudoplastic properties) rather than viscous characteristics. The permeation study showed that the permeability of KAE was significantly improved and the release increased from 4.94% at 1 h to 59.64% at 8 h of application. The permeation rate of nanoemulsion containing KAE at 8 h was 4659.50 μg.cm-2. h- 1 (initial concentration, Co = 2000 μg/mL) with permeability coefficient (Kp) value of 0.48 cm.h-1. Antimicrobial activity of nanoemulsion containing KAE was studied against the skin pathogen bacteria called Staphylococcus aureus ATCC 43300. The results indicated that the inhibition zone size of the optimized nanoemulsion containing KAE (8.00 mm) was slightly bigger than KAE oil (6.5 mm). In vitro cytotoxicity of the optimized nanoemulsion containing KAE and KAE were tested using fibroblast cell line (3T3). The IC50 (50% inhibition of cell viability) of nanoemulsion containing KAE was more than 100 μg/mL. The survival rate of 3T3 cell on nanoemulsion containing KAE (54.76 %) was found to be higher compared to KAE (53.37 %) without any toxicity sign. The in vivo toxicity effect on zebrafish embryos (Danio rerio) was also investigated. The calculated LC50 (50% lethal concentration) values of nanoemulsion containing KAE showed no toxicity effect with more than 500 μg/mL. Nanoemulsion containing KAE proved to be less toxic and can be applied for cosmeceutical applications. This study has revealed that kojic acid ester could be developed as a new active ingredient with nanoemulsion based system and have a potential to be used for further cosmeceutical applications. Emulsions Nanostructured materials - Analysis Phenol oxidase 2018-11 Thesis http://psasir.upm.edu.my/id/eprint/83624/ http://psasir.upm.edu.my/id/eprint/83624/1/FS%202019%206%20-ir.pdf text en public masters Universiti Putra Malaysia Emulsions Nanostructured materials - Analysis Phenol oxidase Ashari, Siti Efliza
institution	Universiti Putra Malaysia
collection	PSAS Institutional Repository
language	English
advisor	Ashari, Siti Efliza
topic	Emulsions Nanostructured materials - Analysis Phenol oxidase
spellingShingle	Emulsions Nanostructured materials - Analysis Phenol oxidase Syed Azhar, Sharifah Nurfadhlin Afifah Development of nanoemulsion containing kojic acid ester for cosmeceutical application
description	Kojic acid (KA) and its derivatives such as kojic acid ester (KAE) are well-known tyrosinase inhibitor that widely used in food and cosmetic industries. The antityrosinase properties of these compounds known to be effective in the treatment of overproduction of melanin such as hyperpigmentation for cosmeceutical applications. Kojic acid ester was used as the active ingredient and encapsulated in the nanoemulsion system. To design excellent formulation, the nanoemulsion containing kojic acid ester (KAE) was screened with different level of variables by using D-optimal experimental mixture design (MED), solubility determination in various oils and finally the preparation system was further developed. DOptimal Mixture Experimental Design (MED) was used for optimizing the composition of nanoemulsions suitable for topical delivery system. The optimized nanoemulsion containing kojic acid ester with desirable criteria was 10.00 % w/w of KAE, 3.19 % w/w of T80, 3.74 % w/w of castor oil: lemon essential oil (ratio 9: 1), 0.70 % w/w of xanthan gum and 81.68 % w/w of deionized water. This optimum nanoemulsion containing KAE showed suitable agreement between the actual droplet size (110.01 nm) and the predicted droplet size (111.73 nm). The residual standard error (RSE) value of nanoemulsion containing KAE was less than 2.0%. The optimized nanoemulsion containing KAE with pH value of 6.28 showed high conductivity value (1492.00 μScmˉ1) indicated that oil-in-water nanoemulsion was obtained. The nanoemulsion remained stable (no phase separation was observed) under accelerated stability during storage at 4°C, 25°C and 45°C within 90 days, centrifugal force as well as freeze-thaw cycles. Rheology measurement justified that the optimized nanoemulsion containing KAE was more elastic (shear thinning and pseudoplastic properties) rather than viscous characteristics. The permeation study showed that the permeability of KAE was significantly improved and the release increased from 4.94% at 1 h to 59.64% at 8 h of application. The permeation rate of nanoemulsion containing KAE at 8 h was 4659.50 μg.cm-2. h- 1 (initial concentration, Co = 2000 μg/mL) with permeability coefficient (Kp) value of 0.48 cm.h-1. Antimicrobial activity of nanoemulsion containing KAE was studied against the skin pathogen bacteria called Staphylococcus aureus ATCC 43300. The results indicated that the inhibition zone size of the optimized nanoemulsion containing KAE (8.00 mm) was slightly bigger than KAE oil (6.5 mm). In vitro cytotoxicity of the optimized nanoemulsion containing KAE and KAE were tested using fibroblast cell line (3T3). The IC50 (50% inhibition of cell viability) of nanoemulsion containing KAE was more than 100 μg/mL. The survival rate of 3T3 cell on nanoemulsion containing KAE (54.76 %) was found to be higher compared to KAE (53.37 %) without any toxicity sign. The in vivo toxicity effect on zebrafish embryos (Danio rerio) was also investigated. The calculated LC50 (50% lethal concentration) values of nanoemulsion containing KAE showed no toxicity effect with more than 500 μg/mL. Nanoemulsion containing KAE proved to be less toxic and can be applied for cosmeceutical applications. This study has revealed that kojic acid ester could be developed as a new active ingredient with nanoemulsion based system and have a potential to be used for further cosmeceutical applications.
format	Thesis
qualification_level	Master's degree
author	Syed Azhar, Sharifah Nurfadhlin Afifah
author_facet	Syed Azhar, Sharifah Nurfadhlin Afifah
author_sort	Syed Azhar, Sharifah Nurfadhlin Afifah
title	Development of nanoemulsion containing kojic acid ester for cosmeceutical application
title_short	Development of nanoemulsion containing kojic acid ester for cosmeceutical application
title_full	Development of nanoemulsion containing kojic acid ester for cosmeceutical application
title_fullStr	Development of nanoemulsion containing kojic acid ester for cosmeceutical application
title_full_unstemmed	Development of nanoemulsion containing kojic acid ester for cosmeceutical application
title_sort	development of nanoemulsion containing kojic acid ester for cosmeceutical application
granting_institution	Universiti Putra Malaysia
publishDate	2018
url	http://psasir.upm.edu.my/id/eprint/83624/1/FS%202019%206%20-ir.pdf
_version_	1747813402909081600

Development of nanoemulsion containing kojic acid ester for cosmeceutical application

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