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: | |
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| Format: | Thesis |
| Language: | English |
| Published: |
2018
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| Subjects: | |
| Online Access: | http://psasir.upm.edu.my/id/eprint/83624/1/FS%202019%206%20-ir.pdf |
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| Summary: | 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. |
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