Preparation And Evaluation Of Pterostilbene Nano/Micro Carriers

Pterostilbene, a naturally occurring analog of resveratrol, is classified as a natural compound, which is an anti-aging gent as effective as resveratrol, while it have many advantages when compared to resveratrol. Firstly, pterostilbene has shown enhanced lipophilicity and membrane permeability and thus greater bioavailability in drug delivery. Secondly, pterostilbene was more effective in free radical scavenging, inhibition of colonic cancer and melanoma cells than resveratrol. In addition, pterostilbene was a potential drug for the prevention and treatment of many skin diseases due to its activity in antifungal. However these potential applications of pterostilbene in cosmetic and pharmaceutical are limited by its poor water solubility and light instability. Therefore, the aim of the study was to develop suitable nanocarriers for potential use of pterostilbene.The pterostilbene-loaded nanoemulsion was developed by hot high-pressure homogenization method. The particle size, loading amount and entrapment efficiency were characterized. The results showed the retention rate of pterostilbene was only 60.8±0.6% after high-pressure homogenization, and the entrapment efficiency of pterostilbene-loaded nanoemulsion was sustained decreased in long-term storage, while the particle size and the PDI was sustained increased, all of these suggested the pterostilbene-loaded nanoemulsion was unstable.The pterostilbene-loaded lipid nanocapsule was developed with improved formula and production process. The particle size, PDI, loading amount, entrapment efficiency were characterized. As compared, the retention rate of pterostilbene was 94.8±1.0%. In long-term storage, the particle size, PDI and entrapment efficiency of pterostilbene-loaded lipid nanocampsule was stable, and the photostability of pterostilbene was improved. The moisture test showed the water content of human skin was improved by using Pt-LNC. A controlled-release behavior of Pt-LNC was observed in in vitro release studies. In vitro penetration studies demonstrated the Pt-LNC possessed higher penetration ability than Pt suspension and Pt solution. Results also revealed an enhancement of cytotoxicity effect of Pt-LNC on mouse melanoma cell (B16F10) with respect to that of free active agent. In addition, in vitro antioxidant activity of Pt-LNC has been proved according to recover the viability of H2O2-damaged-cells (murine fibroblast cells, L929).