Abstract
Rutin is a well-known antioxidant from the group of flavonoids. Its use in cosmetic dermal products is, however, limited due to its poor water solubility. In order to increase rutin saturation solubility and improve the diffusion to the skin, rutin nanocrystals were produced by the smartCrystal process, e.g., bead milling followed by high pressure homogenization. Rutin nanocrystals were further incorporated into hydroxypropyl cellulose (HPC) gel and its long-term stability was assessed. Determination of the antioxidant activity was made by the DPPH (2,2-diphenyl-1-picrylhydrazyl) assay for these formulations: rutin nanocrystals (mean size 300 nm), rutin raw drug powder (mean size 33 μm) and commercial product. Furthermore, the skin penetration profile of rutin was investigated by the tape-stripping method on porcine skin. This study demonstrated that rutin nanocrystal gel had the highest neutralizing activity (90%), followed by a commercial product and rutin raw drug powder. According to the skin study, rutin nanocrystals penetrated to the deeper layers of the stratum corneum, the horny layer of the skin.
Highlights
The human skin is constantly and directly exposed to stressful environmental factors such as solar radiation or pollution, both of which induce the generation of aggressive free radicals as well as reactive oxygen species (ROS)
Rutin raw drug powder suspension had a Laser Diffractometry (LD) diameter 50% of 32.2 μm, which was unchanged after six months of storage at 25 ̋ C 2 ̋ C
This in vitro antioxidant activity study revealed the superiority of rutin nanocrystal gel compared to rutin raw drug powder and its water-soluble derivatives with respect to the antioxidant activity
Summary
The human skin is constantly and directly exposed to stressful environmental factors such as solar radiation or pollution, both of which induce the generation of aggressive free radicals as well as reactive oxygen species (ROS). Due to their size in the nano-dimension, nanocrystals possess higher kinetic saturation solubility, and, in combination with the large surface, it leads to fast dissolution. These effects have already been described for rutin nanocrystals developed for oral administration [9,10]. This yields a more uniform product in size with increased physical stability compared to applying a mono process, e.g., bead milling or high pressure homogenization only [7] This is of special interest for dermal formulations, because they often contain suspension-destabilizing agents such as electrolytes or preservatives. SPF [7], which in simpler terms means a 1000-fold higher bioactivity in skin
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