Solid lipid nanoparticles of lutein with improved dissolution behavior and oral absorption

Abstract

The present study aimed to develop solid lipid nanoparticles of lutein (SLN/LT) with improved dissolution behavior and oral absorption. SLN/LT were prepared by a flash nanoprecipitation method using a multi-inlet vortex mixer, and their physicochemical, photochemical, and pharmacokinetic properties were evaluated. The mean particle size of SLN/LT re-dispersed in water was 237 nm, and small spherical particles with no significant aggregation were observed. LT significantly generated singlet oxygen upon exposure to pseudo-sunlight (250 W/m², 1 h), suggesting its high photoreactivity. The remaining LT in LT solution, crystalline LT, and SLN/LT after irradiation with pseudo-sunlight (250 W/m², 2 h) were 56.3, 86.7, and 101%, respectively. SLN/LT showed improved dissolution behavior of LT in simulated intestinal fluid, and the dissolved amounts of LT at 2 h were at least 50 times higher than that of crystalline LT. Orally administered SLN/LT (100 mg-LT/kg) exhibited enhanced oral absorption of LT, as evidenced by a relative bioavailability of 3.7 to crystalline LT in rats. SLN/LT may be a promising dosage form for orally available LT supplements, possibly leading to enhanced nutritional functions of LT.

Keywords:

• Dissolution
• lutein
• oral absorption
• photostability
• solid lipid nanoparticles

Disclosure statement

No potential conflict of interest was reported by the author(s).

Additional information

Funding

This work was supported in part by JSPS KAKENHI [Grant-in-Aid for Scientific Research (C) (no. 20K07158: S.O. and no. 20K07180: H.S.)].