Characterization, stability, and skin application of astaxanthin particulates

Abstract Purpose Astaxanthin (AX), commonly used for dermal applications, exhibits anti-inflammatory and antioxidant activities; however, it has poor water solubility. In this study, we investigated the physicochemical properties of AX-containing particulates formulated using the amphiphilic graft copolymer Soluplus (polyvinyl caprolactam-polyvinyl acetate-polyethylene glycol graft copolymer: Sol) and polyethylene glycol-2000 (PEG 2000); in addition, the stability and skin applications of AX particulates were investigated. Methods AX, Sol, and PEG were mixed by weight to prepare AX particles using the hydration method. The prepared particles were subjected to stability evaluations including particle size distribution, zeta potential estimation, and fluorescence spectroscopy as well as physical evaluations including 1 H- 1 H NOESY NMR spectral measurement, powder X-ray diffraction, and differential scanning calorimetry. Functional evaluations included singlet oxygen scavenging, skin permeation test, and fluorescence microscopy. Results Relatively stable particles of Sol/AX and Sol/PEG 2000/AX, approximately 100 nm and 125 nm in size, respectively, were formed at a mixed weight ratio (9/1) of 0.1 M Ascorbic Acid solution (0.1 M ASC) and a mixed weight ratio (8/1/1) of 0.1 M ASC, respectively, at 25 °C after storage for 14 days under light-shielded condition. Stability evaluations revealed a decrease in fluorescence intensity and color fading for Sol/AX = 9/1 and Sol/PEG 2000/AX = 8/1/1 (dispersion medium: distilled water); however, no change in fluorescence intensity of AX was observed immediately after preparation in Sol/AX = 9/1 and Sol/PEG 2000/AX = 8/1/1 (dispersion medium: 0.1 M ASC). The fluorescence intensity of AX did not fluctuate significantly immediately after adjustment, and the particles remained stable, showing a bright orange color with time. NMR spectra of Sol/AX = 9/1 and Sol/PEG 2000/AX (dispersion medium: 0.1 M ASC) showed the interactions between the CH 3 group e from Sol (1.8 ~ 2.0 ppm) and the CH groups H-15,11 from AX (6.7 ~ 6.8 ppm), 8’,12’ (6.4 ~ 6.5 ppm), H-10,14 (6.4 ~ 6.5 ppm), and 7,7’ (6.2 ~ 6.3 ppm), indicating the disappearance of cross peaks. Furthermore, new cross peaks were identified for the CH 3 group e of Sol (1.8 ~ 2.0 ppm), the 7-membered ring z of Sol (1.5 ~ 1.8 ppm), the 5-membered ring S of ASC (3.5 ~ 3.6 ppm), the CH group T (3.8 ~ 3.9 ppm), and the CH group U (4.7 ppm). Fluorescence microscopy observations of microparticles formulated with Sol/PEG 2000/AX showed a slight improvement in skin penetration. Conclusion New AX particulates were formed using Sol/PEG 2000/AX = 8/1/1, suggesting that Sol/PEG 2000/AX maintained the stability and improved the skin penetration of AX.