Vitamin E-loaded bigels and emulsions: Physicochemical characterization and potential biological application.

Bigels have been studied as topical formulations for its benefits over sensory and drug delivery parameters. However, there is still few evidences about the properties of the combination of organogelators, oily phases and bioactive molecules into rheological and stability behavior. We investigated the use of classical organogelators (candelilla wax and 12-hydroxystearic acid) and oily phases (sunflower and mineral oil) in 5/95 organogel/polymeric hydrogel ratio to compare vitamin E bigels with its corresponding emulsions. The rheological measurements, microstructure, physical and oxidative stability properties and biological behavior were evaluated. The obtained oil-in-water bigels and emulsions showed crystallization pattern at the interface with high thermal and centrifuge-stress stability. Viscoelastic weak gels were obtained with higher thixotropy and consistency of 12-hydroxystearic bigels. The diameter of the inner phase was increased by vitamin E, despite its little influence over physical and oxidative stability of bigels and emulsions. Those findings indicated that sensory attributes may be regulated by the organogel composition.

A new phytocosmetic preparation from Thymus vulgaris stimulates adipogenesis and controls skin aging process: In vitro studies and topical effects in a double-blind placebo-controlled clinical trial.

BACKGROUND: The use of the injectable products for soft tissue augmentation and treatment of skin aging is an uncomfortable, invasive and related to several complications, and chronic reactions, mainly after long-term application. Efforts to develop new topically active anti-aging products with fewer adverse effects are a huge challenge that should be faced. AIMS: We evaluated the anti-aging effects of a phytocosmetic preparation containing Thymus vulgaris associated with lecithin (ThymLec) on the facial wrinkles, expression lines, and face oval remodeling using a double-blind placebo-controlled clinical trial and in vitro cell culture assays. METHODS: A clinical trial was conducted to evaluate the effects of ThymLec 2% on the area, length, and depth of the perioral and crow's feet wrinkles, nasolabial and smile lines, as well as face oval remodeling in female volunteers using a sophisticated Bio3D Structured-light Scanner. In the in vitro studies using 3T3-L1 mouse embryonic fibroblasts, adiponectin was measured by immunoenzymatic assay, adipogenesis by the AdipoRed reagent method, and the PPAR-γ expression by RT-PCR analysis. RESULTS: Topical treatment with ThymLec 2% reduced facial wrinkles and expression lines promoting a face oval remodeling. In the in vitro studies, ThymLec upregulated the PPAR-γ expression increasing adiponectin production and stimulating the adipogenesis process. CONCLUSIONS: The phytocosmetic preparation containing Thymus vulgaris and lecithin is an innovative and safe topical anti-aging product promoting fat tissue augmentation by adipogenesis stimulation via the upregulation of PPAR-γ expression and adiponectin production.

Coumaric acid derivatives as tyrosinase inhibitors: Efficacy studies through in silico, in vitro and ex vivo approaches.

p-Coumaric acid is a known inhibitor of tyrosinase, an enzyme involved in the initial steps of the melanin synthesis in human and other species. However, its low lipophilicity impairs its penetration through skin and efficacy as antimelanogenic agent indeed. Accordingly, this paper reports the assessment of several coumaric acid derivatives as tyrosinase inhibitors and antimelanogenic agents in in vitro, in silico and ex vivo assays. The compounds were designed with modifications in the aromatic and acid moieties of p-coumaric acid, being the coumarate esters the most promising derivatives. The compounds showed higher tyrosinase inhibitory activity (pIC50 3.7-4.2) than the parent acid, being compounds 1d, 1e and 1f the most potent inhibitors. Docking analysis showed that these esters are competitive inhibitors per se, and act independently of a redox mechanism as suggested by DPPH assays. Moreover, the esters showed efficacy in reducing the melanin deposition in human skin fragments at 0.1% concentration, especially compound 1e. In summary, there is an important equilibria between tyrosinase affinity and lipophilicity that must be considered to get effective antimelanogenic agents with adequate permeability in the skin.

Novel topical skin hydration agent containing Anadenanthera colubrina polysaccharide-standardized herbal preparation.

BACKGROUND: Hydration is an important factor to promote skin barrier function, metabolism, and appearance. In this process, the presence of aquaglyceroporins, envelope and lipid synthesis, and metabolism proteins are essential to provide greater corneocyte cohesion and to form a barrier avoiding transepidermal water loss. OBJECTIVE: We evaluated the effects of a new topical pigment-free agent containing an Anadenanthera colubrina polysaccharide-rich dermocosmetic preparation (ACP) on the aquaporin-3 (AQP-3), filaggrin (FLG), involucrin (INV), glucocerebrosidase (GBA), and elongation of very-long-chain fatty acid (ELOVL) proteins production in skin human fragments, as well as on the transepidermal water loss in a double-blind placebo-controlled clinical trial. METHODS: AQP3, FLG, INV, GBA, and ELOVL3 levels were measured by immunofluorescence analysis in human skin explants. Clinical trial was conducted to evaluate the effects of ACP 1% and ACP 3% on the transepidermal water loss (TEWL). RESULTS: Image and statistical analysis showed that ACP 3% significantly increased at 90% the expression of AQP3. Similarly, ACP 3% was able to promote a significant increase of 68% and 51% in FLG and INV, respectively. ACP 3% produced no effects on the GBA and ELOVL3 proteins. Transepidermal water loss was significantly reduced in human volunteers under treatment with ACP 1% and ACP 3%. CONCLUSION: ACP reduced transepidermal water loss in a clinical trial, promoting human skin hydration. These effects were related to modulation of the AQP3, FLG, and INV as evidenced by immunofluorescence assay. This way, A colubrina polysaccharide-rich phytopharmaceutical preparation is an effective additive product to skin hydration.