Development of novel lutein nanocrystal formulation with improved oral bioavailability and ocular distribution. (October 2019)

• Record Type: Journal Article
• Authors: Seto, Yoshiki; Ueno, Kodai; Suzuki, Hiroki; Sato, Hideyuki; Onoue, Satomi
• Is Part Of: Journal of functional foods. Volume 61(2019)
• Publication Date: 2019-10
• Subjects: Lutein -- Nanocrystal formulation -- Oral bioavailability -- Ocular distribution; ANOVA analysis of variance -- AUC0–24h area under the concentration versus time curve from 0 to 24h -- BA bioavailability -- BHT dibutylhydroxytoluene -- Cmax maximum concentration -- DLS dynamic light scattering -- HPC hydroxypropyl cellulose -- HPLC high-performance liquid chromatography -- LED light-emitting diode -- LT lutein -- NC/LT nanocrystal formulation of lutein -- PLM polarized light microscopy -- RH relative humidity -- SEM scanning electron microscopy -- UV ultraviolet -- XRPD X-ray powder diffraction; Functional foods -- Analysis -- Periodicals; Food -- Biotechnology -- Periodicals; Nutrition -- Periodicals; 613.2
• DOI: 10.1016/j.jff.2019.103499
• Languages: English
• ISSNs: 1756-4646

Abstract

Graphical abstract: Highlights: A nanocrystal formulation of lutein (NC/LT) was prepared using a bottom-up system. The dissolution behavior of NC/LT was higher than that of crystalline LT in water. Orally-taken NC/LT showed higher oral absorption of LT compared with crystalline LT. NC/LT may be an efficacious dosage form to enhance nutraceutical properties of LT. Abstract: A nanocrystal formulation of lutein (NC/LT) was prepared by particle size reduction approach with a bottom-up system to improve nutraceutical properties of LT, and physicochemical and pharmacokinetic characterizations of NC/LT were undertaken. In NC/LT, LT nanoparticles with a mean diameter of 230 nm existed in a crystalline state, and, in comparison with crystalline LT, NC/LT exhibited a marked improvement in dissolution/dispersion behavior of LT in water. Orally-administered NC/LT exhibited enhanced oral absorption of LT in male Sprague-Dawley rats, as evidenced by relative bioavailability of 15.2 to crystalline LT. After oral administration of LT samples (100 mg-LT/kg, 7 days) to male Sprague-Dawley rats, the ocular accumulation of LT in NC/LT was 3.4-fold higher than that in crystalline LT. Upon these findings, particle size reduction of LT would be efficacious to improve its dissolution and pharmacokinetic characteristics, and NC/LT may be an attractive dosage form to enhance the nutraceutical properties of LT.