Novel resveratrol nanodelivery systems based on lipid nanoparticles to enhance its oral bioavailability

• Type: Article in International Scientific Journal
• Date: 2013

Authors

Ana Rute Neves (Author) Other; Marlene Lucio (Author) FFUP; Susana Martins (Author) Other; Jose Luis C Costa Lima (Author) FFUP; Salette Reis (Author) FFUP

Journal

Title: International Journal of Nanomedicine

Vol. 8

Pages: 177-187

ISSN: 1176-9114

Publisher: Dove Medical Press

Indexing

ISI Web of Knowledge - 160 Citations

Scopus - 220 Citations

Scientific classification

FOS: Engineering and technology > Nano-technology

Other information

Authenticus ID: P-005-3EE

DOI: 10.2147/ijn.s37840

Abstract (EN): Introduction: Resveratrol is a polyphenol found in grapes and red wines. Interest in this polyphenol has increased due to its pharmacological cardio- and neuroprotective, chemopreventive, and antiaging effects, among others. Nevertheless, its pharmacokinetic properties are less favorable, since the compound has poor bioavailability, low water solubility, and is chemically unstable. To overcome these problems, we developed two novel resveratrol nanodelivery systems based on lipid nanoparticles to enhance resveratrol's oral bioavailability for further use in medicines, supplements, and nutraceuticals. Methods and materials: Solid lipid nanoparticles (SLNs) and nanostructured lipid carriers (NLCs) loaded with resveratrol were successfully produced by a modified hot homogenization technique. These were completely characterized to evaluate the quality of the developed resveratrol-loaded nanoparticles. Results: Cryo-scanning electron microscopy morphology studies showed spherical and uniform nanoparticles with a smooth surface. An average resveratrol entrapment efficiency of similar to 70% was obtained for both SLNs and NLCs. Dynamic light scattering measurements gave a Z-average of 150-250 nm, polydispersity index of similar to 0.2, and a highly negative zeta potential of around -30 mV with no statistically significant differences in the presence of resveratrol. These characteristics remained unchanged for at least 2 months, suggesting good stability. Differential scanning calorimetry studies confirmed the solid state of the SLNs and NLCs at both room and body temperatures. The NLCs had a less ordered crystalline structure conferred by the inclusion of the liquid lipid, since they had lower values for phase transition temperature, melting enthalpy, and the recrystallization index. The presence of resveratrol induced a disorder in the crystal structure of the nanoparticles, suggesting a favoring of its entrapment. The in vitro release studies on conditions of storage showed a negligible resveratrol release over several hours for both nanosystems and the in vitro simulation of gastrointestinal transit showed that the resveratrol remained mostly associated with the lipid nanoparticles after their incubation in digestive fluids. Conclusion: Both nanodelivery systems can be considered suitable carriers for oral administration, conferring protection to the incorporated resveratrol and allowing a controlled release after uptake.

Language: English

Type (Professor's evaluation): Scientific

No. of pages: 11