Biocompatible and biodegradable nanoparticles for enhancing solubility and bioavailability of trans‐resveratrol

Abstract

ObjectivesTrans‐resveratrol (R) is a natural polyphenolic compound found in red grapes, mulberries, and other berries. Cell and animal studies indicate that it can improve metabolic health through its anti‐inflammation, anti‐obesity, anti‐oxidant properties. However, the evidence is inconclusive in human studies regarding its effectiveness in improving metabolic health, most likely due to its low aqueous solubility, and trivial bioavailability. The objectives of this study are to encapsulate R into biocompatible and biodegradable nanoparticles (R‐NPs), and measure their characteristics and oral bioavailability in C57BL/6J mice.MethodsThe R‐NPs were made of soy phosphatidylcholine, vitamin E, Tween 80, and R. Their size, polydispersity index and zeta potential were measured using Zetasizer Pro. R‐NPs were stored in dark at 4°C, 22°C and 37°C, and their physical and chemical stability was measured every day. The physical stability was determined using Zetasizer Pro. The encapsulation efficiency and chemical stability were determined using an Agilent 1290 Infinity II UHPLC system. After oral administration of R‐NPs and free R at R concentration 50 mg/kg body weight in C57BL/6J mice, their oral bioavailability was determined by measuring blood R concentrations using the UHPLC system.ResultsNanoencapsulation significantly increased aqueous solubility of R by more than 140 times. The mean particle size of freshly made R‐NPs was around 70 nm. The polydispersity index was less than 0.3. The zeta potential of R‐NPs was around −13 mV. R’s encapsulation efficiency was more than 95%. The size, polydispersity index, zeta potential, and R concentrations of R‐NPs did not change significantly at 4°C, 22°C and 37°C for 3 days. The encapsulation efficiency of R‐NPs remained above 94% after storage for 3 days at three tested temperatures. These data indicated good chemical and physical stability of R‐NPs. As compared to free R, R‐NPs had higher oral bioavailability in C57BL/6J mice.ConclusionsNanoencapsulation increased the aqueous solubility and stability of R, and improved R’s oral bioavailability in mice.