Tocopherol succinate-loaded ethosomal gel synthesized by cold method technique: Deeper biophysical characterizations for translational application on human skin.

BACKGROUND: Tocopherols are well-known antioxidant and moisturizing agent. Tocopherol succinate (TS) are widely used in many skin products especially used in anti-aging and skin whitening product formulation. AIM: We previously reported the successful synthesis and preliminary characterizations of stable TS ethosomal gels (TSEG) (DOI: 10.1111/jocd.14907). Herein, we develop and further characterize TSEG to enhance the stability of the developed formulation with increased permeation through skin. METHODS: Cold method technique was used to prepare TS ethosomes. The developed ethosomal vesicle size was 250 nm, which allowed TS to penetrate through the stratum corneum layer and act on melanocytes. For stability study was assessed by thermogravimetric analysis (TGA) by placing TSEG and unloaded/control ethosomal gel (CEG) at various temperature conditions, that is, 8°C, 25°C, 40°C, and 40°C ± 75% RH for 3 months. Organoleptic evaluation was done in terms of color, odor, and phase separation. Transmission electron microscopy (TEM), Fourier Transform infrared spectroscopy (FTIR), x-ray diffraction spectroscopy (XRD), zeta potential (ZP) and particle size (PS) was used for TSEG physical characterizations. In vitro dissolution and ex-vivo permeation studies (using Franz diffusion cell) were performed for both TSEG and CEG formulations. Human women (N = 34) were used to evaluate in vivo biophysical parameters including erythema, melanin, moisture content, sebum level, and skin elasticity. RESULTS: Developed formulation was highly thermostable during the 3 months. Erythema, melanin, and sebum level decreased while marked improvement (p < 0.05) in moisture content and elasticity have been observed for the developed TSEG. CONCLUSION: The developed TSEG formulation was found to be efficient, safe (no adverse effects observed), stable (at least for 3 months), and easy to use for topical application with improved skin complexation and skin integrity.

Profiling of phytochemicals using LC-ESI-MS2 , in vitro, in vivo characterization and cosmeceutical effects of Alpinia galanga (wild) extract loaded emulgel.

BACKGROUND: The potential as a depigmenting agent, sun protection, and healthy benefits is indicated by the sun protection factor, radical scavenging, and tyrosinase inhibitory activities of Alpinia galanga (wild). AIMS: A stable emulgel containing A .galanga (wild) extract is prepared. This emulgel is then characterized by in vitro evaluation and identification of contents by LC-ESI-MS2 . In vivo performance is counted in terms of moisturizing, melanin level, erythema, sebum, skin fine pores and large pores analysis, and other related physiological skin parameters. METHODS: DPPH radical scavenging activity, total phenolic and flavonoid counts were used to measure the free radical scavenging and tyrosinase inhibitory capability of A .galanga (wild) extract, respectively. LC-ESI-MS2 used for phytochemical analysis. Emulgels synthesize, and their globule size, Ultracentrifugation, pH, and conductivity were all evaluated. Among the developed formulations, the optimal emulgels formulation underwent 90-day stability tests for organoleptic characteristics and rheology at 8°C, 25°C, 40°C, and 40°C + 75% RH (relative humidity). Using sebumeter®, mexameter®, and corneometer®, changes in skin physiological parameters were assessed over the course of 12 weeks in 13 healthy male, Asian volunteers. VisioFace® is used for computational analysis of high-resolution pictures to determine the % area, fine pore counts, and large pore counts of the skin. RESULTS: The antioxidant, tyrosinase inhibitory potential and counts of total phenolic and flavonoids of A .galanga (wild) extract were impressive (85%, 75%, and 48.0 mg GAE/g and 14.37 mg quercetin/g, respectively). In terms of stability evaluation, globule size (0.7528 ± 0.192 µm). Optimized A .galanga (wild) ethanol aqueous (AGEA) extract loaded emulgel was stable in terms of organoleptic and in vitro evaluation. The AGEA formulation significantly reduced the amount of sebum, erythema, fine pore counts, large pore counts, fine pore % area and large pores area percentage while significantly improved the moisture and elasticity of the skin. CONCLUSION: A stable A .galanga (wild) extract loaded emulgel was successfully produced that improved the skin physiological parameters in terms of skin's sebum, erythema, moisturizing, melanin, and pores.