Abstract
We created composite nanoparticles containing hydrophilic additives using a supercritical antisolvent (SAS) process to increase the solubility and dissolution properties of trans-resveratrol for application in oral and skin delivery. Physicochemical properties of trans-resveratrol-loaded composite nanoparticles were characterized. In addition, an in vitro dissolution–permeation study, an in vivo pharmacokinetic study in rats, and an ex vivo skin permeation study in rats were performed. The mean particle size of all the composite nanoparticles produced was less than 300 nm. Compared to micronized trans-resveratrol, the trans-resveratrol/hydroxylpropylmethyl cellulose (HPMC)/poloxamer 407 (1:4:1) nanoparticles with the highest flux (0.792 μg/min/cm2) exhibited rapid absorption and showed significantly higher exposure 4 h after oral administration. Good correlations were observed between in vitro flux and in vivo pharmacokinetic data. The increased solubility and flux of trans-resveratrol generated by the HPMC/surfactant nanoparticles increased the driving force on the gastrointestinal epithelial membrane and rat skin, resulting in enhanced oral and skin delivery of trans-resveratrol. HPMC/surfactant nanoparticles produced by an SAS process are, thus, a promising formulation method for trans-resveratrol for healthcare products (owing to their enhanced absorption via oral administration) and for skin application with cosmetic products.
Highlights
Trans-resveratrol is abundant in various foods, such as grapes, peanuts, and berries, and is usually taken as a dietary supplement
In pH 1.2 buffer solution, 53.7 μg/mL in pH 4.0 buffer solution, and 51.1 μg/mL in pH 6.8 buffer solution. These results indicate that the solubility of trans-resveratrol is very poor in aqueous solution and is similar to previously reported data [31]
The solubility of trans-resveratrol increased with increasing viscosity of hydroxylpropylmethyl cellulose (HPMC), while trans-resveratrol solubility showed the opposite trend in PVP
Summary
Trans-resveratrol is abundant in various foods, such as grapes, peanuts, and berries, and is usually taken as a dietary supplement. Trans-resveratrol is known as 3,5,4‘-trihydroxystilbene, a non-flavonoid polyphenolic compound produced by plants in response to injury or attack by bacteria and fungi [1]. When exposed to UV light, the typically low transformation of trans-resveratrol to cis-resveratrol is accelerated [2]. Trans-resveratrol has been shown to have several beneficial properties, including anti-aging, anticancer, antidiabetic, anti-inflammatory, antioxidant, cardioprotective, and neuroprotective activities [3,4,5,6]. Antioxidants 2019, 8, 554 instability, short plasma half-life, and extensive metabolism in the intestine and liver, clinical uses of trans-resveratrol are limited to oral administration [1,7,8,9].
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