1-1-diphenyl-2-picrylhydrazyl and Sunburn

Flavonoids have many positive effects on various cell layers of the skin (e.g. anti-oxidant, anti-allergic and anti-inflammatory effects). However, the limiting factor of the use of flavonoids is their low water solubility. To overcome the poor solubility, apigenin nanosuspensions were prepared using the combination technology (CT), i.e. bead milling and subsequently high pressure homogenization. Distinct reduction in particle size was observed after each bead milling passage resulting in z-average (PCS) of 413 nm and a polydispersity index of 0.202. The LD data showed a similar pattern of particle size reduction reaching a diameter 99% (d(v)99%) of 0.515 μm. The antioxidant capacity of apigenin nanocrystals were almost doubled compared to the original coarse suspension. The developed smartCrystals can be easily incorporated into gels, which makes apigenin nanocrystals available for dermal application as efficient antioxidant.

Topics: Administration, Cutaneous; Antioxidants; Apigenin; Biphenyl Compounds; Chemistry, Pharmaceutical; Crystallography, X-Ray; Humans; Kinetics; Nanoparticles; Nanotechnology; Particle Size; Permeability; Picrates; Skin; Solubility; Sunburn; Sunscreening Agents; Technology, Pharmaceutical; Ultraviolet Rays

Solar ultraviolet radiation (UV) is a major cause of non-melanoma skin cancer in humans. Photochemoprevention with natural products represents a simple but very effective strategy in the management of cutaneous neoplasia. The study investigated the protective activity of Calluna vulgaris (Cv) and red grape seeds (Vitis vinifera L, Burgund Mare variety) (BM) extracts in vivo on UVB-induced deleterious effects in SKH-1 mice skin. Forty SKH-1 mice were randomly divided into 4 groups (n=10): control, UVB irradiated, Cv + UVB irradiated, BM+UVB irradiated. Both extracts were applied topically on the skin in a dose of 4 mg/40 μl/cm(2) before UVB exposure - single dose. The effects were evaluated in skin 24 hours after irradiation through the presence of cyclobutane pyrimidine dimers (CPDs) and sunburn cells, tumor necrosis factor-alpha (TNF-α), interleukin (IL)-6 levels. The antioxidant activity of BM extract was higher than those of Cv extract as determined using stable free radical DPPH assay and ABTS test. One single dose of UVB generated formation of CPDs (p<0.0001) and sunburn cells (p<0.0002) and increased the cytokine levels in skin (p<0.0001). Twenty hours following irradiation BM extract inhibited UVB-induced sunburn cells (p<0.02) and CPDs formation (p<0.0001). Pretreatment with Cv and BM extracts resulted in significantly reduced levels of IL-6 and TNF-α compared with UVB alone (p<0.0001). Our results suggest that BM extracts might be a potential candidate in preventing the damages induced by UV in skin.

Topics: Animals; Apoptosis; Biphenyl Compounds; Calluna; Cytokines; Disease Models, Animal; Female; Free Radical Scavengers; Humans; Mice; Mice, Hairless; Phytotherapy; Picrates; Plant Extracts; Pyrimidine Dimers; Random Allocation; Seeds; Skin; Skin Neoplasms; Sunburn; Ultraviolet Rays; Vitis