Resveratrol’s poor water solubility, low stability, and bioavailability of less than 1% have limited its clinical application. In recent years, researchers have significantly improved its bioavailability by developing various delivery systems, which are analyzed below:
Nano delivery systems
Nanoparticles: including protein nanoparticles, polysaccharide nanoparticles, etc. By encapsulating resveratrol in nanoparticles, its targeting and stability can be enhanced and the release rate can be increased. For example, self-assembly of resveratrol into nanoparticles using PCL-PEG copolymer can significantly improve its bioavailability.
Nanoemulsions: formed by mixing water phase, oil phase, and emulsifier in appropriate proportions, with particle sizes between 50-200 nm. Nano-emulsion can improve the water solubility and dissolution rate of resveratrol, prolong the retention time and promote absorption.
Nanocapsules: thin layers of polymer encapsulate the drug within its membrane shell, which can improve the water solubility and cellular uptake rate of resveratrol, and provide a physical barrier against degradation.
Nano-liposomes: with the good biocompatibility of liposomes, they can achieve slow release and promote the absorption of resveratrol in the small intestine.
Nano-suspension: formed by dispersing the drug in water under the action of stabilizers, it has the advantages of small particle size and high drug loading capacity, and can significantly improve the saturation solubility of resveratrol.
Alcohol plasmid: composed of high concentration of low molecular weight alcohol, water and phospholipids, with a multilayer vesicle structure, it can encapsulate multiple types of drugs and significantly enhance the antioxidant capacity of resveratrol.
Polymeric nanomicelles: formed by self-assembly of amphiphilic block polymers in aqueous solution, which can encapsulate resveratrol into a hydrophobic core to form drug-carrying nanomicelles for sustained release.
Other delivery systems
Liposome: with a structure similar to cell membrane, it can effectively protect resveratrol from damage by the external environment, has good biocompatibility and biodegradability, and can improve the targeting and bioavailability of resveratrol.
Microcapsules: By encapsulating resveratrol in microcapsules, it can prolong its circulation time in the body, improve targeting and bioavailability, and reduce toxic side effects.
Viral vectors: By utilizing the natural infectious ability of viruses to deliver resveratrol to target cells with high efficiency and specificity, it can improve the targeting and bioavailability of resveratrol and reduce toxic side effects.
Combined use of bioenhancers
Quercetin: By inhibiting the activity of key enzymes responsible for metabolizing resveratrol in the liver and small intestine, as well as hindering the function of several key drug transporter proteins, it can effectively improve the bioavailability and persistence of resveratrol in the body.
Piperine: It can inhibit the activity of ABC transporter, SULT and even UGT enzymes, reduce the production of sulfate and glucuronide metabolites, and enhance the concentration of resveratrol.