Development and Characterization of Vitamin A-Loaded Solid Lipid Nanoparticles for Topical Application

Abstract

Vitamin A and its esters are commonly found in topical applications because of their advantageous properties, however, have the drawback that are highly sensitive to ultraviolet radiation. The aim of this work was to develop and characterize a novel formulation of solid lipid nanoparticles suitable for topical applications in order to protect vitamin A from degradation. Vitamin A-loaded nanoparticles were successfully prepared by hot homogenization employing Gelucire 44/14 ® and cetyl alcohol as carrier materials, showing an entrapment efficiency of more than 90%. Particle size, measured by dynamic light scattering, was ca. 40 nm, while transmission electron microscopy images showed that dried nanoparticles were spherical with an average size of about 30-50 nm. Small angle X-ray scattering was used to study their aspect ratio and their physicochemical properties were evaluated by differential scanning calorimetry, infrared spectroscopy and X-ray powder diffraction, additionally, stability of vitamin A was studied by UV-Vis spectroscopy.

Fatty acids based α‐Tocopherol loaded nanostructured lipid carrier gel: In vitro and in vivo evaluation for moisturizing and anti‐aging effects

“…Furthermore, addition of liquid lipid in lipid mixture leads to reduction of crystallinity of solid lipid and develops imperfections in structure to entrap more α‐tocopherol 20. High entrapment efficiency is likely to be beneficial due to avoidance of irritation related to direct contact of drug to the skin 22…”

“…20 High entrapment efficiency is likely to be beneficial due to avoidance of irritation related to direct contact of drug to the skin. 22 Optimized formulation was selected for further study on the basis of least particle size and PDI while higher zeta potential and entrapment efficiency.…”

Topical Gel of Vitamin A Solid Lipid Nanoparticles: A Hopeful Promise as a Dermal Delivery System

“…The palmitate derivate of Vit A is more lipophile than Vit A-acetate for this reason, EE% of the mentioned study is higher than the current study. 1 …”

“…4 Several research published using lipid NPs for dermal utilization of cosmetic and pharmaceutical active materials, including ascorbyl palmitate, tocopherol (Vitamin E), co-enzyme Q10, and retinol (Vitamin A). 1 Chemical stability of these sensitive actives can be augmented if they are combined into the drug carrier systems. Authors particularly examined the stabilization effects of SLN on retinol, and proposed dependence of stabilization on the kind of lipids and surfactants employed.…”

“…Moreover, its roles as an anti-oxidant and prevents tissue atrophy and collagen loss during aging. 1 Due to its anti-oxidant and moisturizing features, Vit A is usually observed in creams or gels for topical use. Nevertheless, it has high sensitivity to ultra-violet radiation and oxygen that may quickly enhance its degradation, which result in declining the contents of Vit A in epidermis.…”