Water‐in‐oil microemulsions composed of monoolein enhanced the transdermal delivery of nicotinamide

Objective Nicotinamide, also known as niacinamide, is a water‐soluble vitamin that is used to prevent and treat acne and pellagra. It is often found in water‐based skin care cosmetics because of its high water solubility. Nicotinamide is a small molecule with a molar mass of 122.1 g/mol. However, it...

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Published in:International journal of cosmetic science 2021-06, Vol.43 (3), p.302-310
Main Authors: Kitaoka, Momoko, Nguyen, Trung Cong, Goto, Masahiro
Format: Article
Language:English
Subjects:
Acne
Administration, Cutaneous
Barriers
Bioactive compounds
Chromatography, High Pressure Liquid - methods
Cosmetics
Deficiency diseases
Drug delivery
Emulsions
Emulsions - chemistry
Epidermis
Formulations
Glycerides - chemistry
Humans
Hydrophilicity
Hydrophobic and Hydrophilic Interactions
Hydrophobicity
Light scattering
Microemulsions
Microscopy, Electron, Transmission
Niacinamide - administration & dosage
Nicotinamide
Oil
Oils - chemistry
Penetration
Photon correlation spectroscopy
Saline solutions
Skin
Skin - metabolism
skin barrier
skin physiology
Stratum corneum
structure
Water - chemistry
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Summary:Objective Nicotinamide, also known as niacinamide, is a water‐soluble vitamin that is used to prevent and treat acne and pellagra. It is often found in water‐based skin care cosmetics because of its high water solubility. Nicotinamide is a small molecule with a molar mass of 122.1 g/mol. However, it has a hydrophilic nature that becomes an obstacle when it penetrates through the skin. The topmost layer of the skin, the stratum corneum, acts as a strong hydrophobic barrier for such hydrophilic molecules. The oil‐based formulations are expected to enhance the transdermal delivery efficiency of nicotinamide. Methods We have developed oil‐based microemulsion formulations composed of a squalane vehicle. Monoolein was used as an emulsifier that has a potential to enhance the nicotinamide delivery through the stratum corneum. Results Because the mean size of the emulsions measured by dynamic light scattering was 20.9 ± 0.4 nm, the microemulsion formulation was stable under the long‐term storage. Monoolein acted as a skin penetration enhancer, and it effectively enabled the penetration of nicotinamide through human abdominal skin, compared with nicotinamide in a phosphate‐buffered saline solution. The flux was increased 25‐fold. Microscopic imaging revealed that the hydrophilic bioactive compounds penetrated through the intercellular spaces in the epidermis. Conclusion The monoolein‐based microemulsion was transparent and stable, suggesting that it is a promising formulation for a transdermal nicotinamide delivery. Résumé Objectif Le nicotinamide, aussi connu sous le nom de niacinamide, est une vitamine hydrosoluble utilisée pour prévenir et traiter l’acné et la pellagre. On le trouve souvent dans les produits cosmétiques de soins de la peau à base d’eau en raison de sa forte solubilité dans l’eau. Le nicotinamide est une petite molécule d’une masse molaire de 122,1 g/mol. Cependant, sa nature hydrophile devient un obstacle lorsqu’il pénètre la peau. La couche supérieure de la peau, la couche cornée, agit comme une barrière hydrophobe robuste contre ces molécules hydrophiles. Les formulations à base d’huile devraient améliorer l’efficacité de l’administration par voie transdermique du nicotinamide. Méthodes Nous avons développé des formulations de microémulsions à base d’huile composées d’un véhicule de squalane. La monooléine a été utilisée en tant qu’émulsifiant doté du potentiel d’améliorer l’administration de nicotinamide par la couche cornée. Résultats Étant
ISSN:0142-5463
1468-2494
DOI:10.1111/ics.12695