Casein nanoparticles as carriers for the oral delivery of folic acid

Abstract

Alimentary proteins can be viewed as an adequate material for the preparation of nanoparticles and microparticles. They offer several advantages such as their digestibility, price and a good capability to interact with a wide variety of compounds and nutrients. The aim of this work was to prepare and characterize casein nanoparticles for the oral delivery of folic acid. These nanoparticles were prepared by a coacervation process, stabilized with either lysine or arginine and, finally, dried by spray‐drying. For some batches, the effect of a supplementary treatment of nanoparticles (before drying) with hydrodynamic high pressure on the properties of the resulting carriers was also evaluated. The resulting nanoparticles displayed a mean size close to 150 nm and a folic acid content of around 25 mg per mg nanoparticle. From the in vitro release studies, it was observed that casein nanoparticles acted as gastro‐resistant devices and, thus, folic acid was only released under simulated intestinal conditions. For the pharmacokinetic study, folic acid was orally administered to laboratory animals as a single dose of 1 mg/kg. Animals treated with folic acidloaded casein nanoparticles displayed significantly higher serum levels than those observed in animals receiving an aqueous solution of the vitamin. As a consequence the oral bioavailability of folic acid when administered in casein nanoparticles was calculated to be around 52%, a 50% higher than with the traditional aqueous solution. Unfortunately, the treatment of casein nanoparticles by hydrodynamic high pressure modified neither the release profile of the vitamin nor its oral bioavailability.