Abstract

An oil in water (O/W) nanoemulsion formulation containing kojic monooleate (KMO) in thin film system was developed. Response surface methodology (RSM) was used to optimize and analyzed the effect of three variables, namely concentration of polyvinyl alcohol (PVA) (20–30% w/w), concentration of propylene glycol (PG) (1–10% w/w), and shear rate of high shear homogenizer (3000–9000 rpm) on droplet size as a response, while other compositions remained constant such as KMO (10.0% w/w), Tween 80 (3.19% w/w), castor oil (3.74% w/w), xanthan gum (0.70% w/w), and germall plus (0.7% w/w, PG (and) diazolidinyl urea (and) iodopropynyl butylcarbamate). The optimized KMO nanoemulsion formulation with desirable criteria was PVA (27.61% w/w) and PG (1.05% w/w), and shear rate (8656.17 rpm) with a predicted droplet size (110.21 nm) and actual droplet size (105.93 nm) with a residual standard error (RSE) of less than 2.0% was obtained. Analysis of variance (ANOVA) showed that the fitness of the quadratic polynomial fit the experimental data with a F-value of 65.30, p–value of p < 0.0001, and a non-significant lack-of-fit. The optimized KMO formulation shows the desired criteria of the thin film system and the physicochemical properties (Zeta potential −37.37 mV, PDI 0.13, pH 4.74) and stability at four different conditions indicate its suitability for cosmeceutical applications.

Highlights

  • A derivative of kojic acid, kojic monooleate (KMO) is non-toxic, soluble in oil, and enhances stability to pH, temperature, and storability compared to kojic acid [1]

  • KMO possesses higher 2, 2-diphenyl-1-picrylhydrazyl (DPPH) inhibition, better mushroom tyrosinase inhibition, and B16F1 melanoma tyrosinase inhibition as well as less cytotoxicity compared to kojic acid [2], a formulation containing KMO was developed for cosmeceutical application in this study

  • The concentration of propylene glycol (PG) was fixed at 1% and 10% to study the effect of the concentration of polyvinyl alcohol (PVA) on Thin Film System (TFS)

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Summary

Introduction

A derivative of kojic acid, kojic monooleate (KMO) is non-toxic, soluble in oil, and enhances stability to pH, temperature, and storability compared to kojic acid [1]. To achieve a desired effect on skin, penetration of the active compound into the skin after its topical application is required [3]. The size of the droplet plays a major role in determining the effect of a formulation on skin. Nanoemulsion drug delivery systems such as lipid based formulations. Cosmetics 2020, 7, 73 that improve the solubility and bioavailability of hydrophobic drugs are the most appropriate for topical applications, considering the composition of the skin structure and its barrier property [3,4]. Nanoemulsions are oil-in-water (O/W) or water-in-oil (W/O) emulsions with a droplet size range of between 20–200 nm [5,6,7]

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