Improved Bioavailability of β-Carotene by Amorphous Solid Dispersion Technology in Rats

Abstract

β-Carotene (BC) is a natural lipophilic carotenoid mainly present in vegetables and fruits. Although it has various beneficial pharmacological activities, its bioavailability is low owing to its low water solubility. Recently, we reported that BC solid dispersion prepared using hot-melt technology with polyvinylpyrrolidone and sucrose fatty acid esters was in an amorphous state and showed the highest solubility. We hypothesized that the absorption of BC solid dispersion would be better because of its increased water solubility. To verify this, we conducted a pharmacokinetic analysis of BC for application in functional foods. Crystalline or amorphous BC was orally administered to rats. Blood was collected at various time points, and the BC concentration in the plasma was measured by HPLC. Oral administration of amorphous BC showed increased absorption in rats compared with that of BC crystals. Using blood samples from rats that were intravenously injected with the plasma of rats that had been orally administered BC, pharmacokinetic parameters could be calculated without using organic solvents or surfactants. It was possible to calculate various pharmacokinetic parameters under physiological conditions according to amorphous BC characteristics. Thus, we were able to determine the bioavailability of BC after oral administration. This simple technology to improve BC solubility without the use of organic solvents can be applied not only in the pharmaceutical industry but also in the food industry, and it therefore has high utility value.