Superior Bioavailability of a Novel Lutein and Zeaxanthin Formulation in Healthy Human Subjects

Abstract

Introduction: Lutein (L) and zeaxanthin (Z) are carotenoids that are found in the macula of the human eye and are known to improve visual functions. However, poor bioavailability of supplemental L and Z poses a challenge to achieving significant benefits after consumption. We developed a novel patented formulation of L and Z (Ocusorb^®) and demonstrated the improved bioavailability in a pharmacokinetic clinical study.

Methods: Ninety adult human volunteers were recruited in this randomized, double-blind, parallel, comparative bioavailability study. Volunteers were randomly assigned to receive single dose of 10 mg lutein and 2 mg zeaxanthin from test (LZO) or reference (LZC) formulations after breakfast. Blood samples were collected pre-dose at - 48, - 24, and 0 h and at 2, 4, 6, 8, 10, 12, 16, 20, 24, 48, and 72 h post-dose. Serum concentrations of L and Z were quantified by using a validated HPLC method. The LZO and LZC formulations were compared for L and Z on the basis of C_max, AUC_0-72, and AUC_0-t.

Results: All 90 subjects completed the study. The LZO group demonstrated significantly higher levels of L and Z in serum at several time points as compared to LZC group. The LZO group showed significantly higher bioavailability for lutein (2.5 times higher C_max, 2.9 times higher AUC_0-72, and 3.2 times higher AUC_0-t) and zeaxanthin (1.8 times higher C_max, 2.2 times higher AUC_0-72, and AUC_0-t) as compared to the LZC group. No safety issues were reported.

Conclusion: The study results show superior bioavailability of lutein and zeaxanthin from our novel LZO formulation as compared to LZC. The enhanced bioavailability from the LZO formulation can be advantageous for individuals looking to quickly improve their L and Z status and enhance their vision performance.

Trial registration: http://ctri.nic.in/ . Identifier: CTRI/2019/11/022082.

Keywords: Absorption; Bioavailability; Carotenoids; Lutein; Macular pigment optical density; Zeaxanthin.

Fig. 1

Flowchart of this randomized, double-blind, comparative bioavailability study of lutein and zeaxanthin formulations

Fig. 2

Lutein and zeaxanthin serum levels versus time. The LZO group showed significantly (p < 0.05) higher serum lutein levels (> 2-fold) at all time points i.e., 2–72 h post dose (a) and higher serum zeaxanthin levels (> 1.5-fold) from 4 to 72 h post dose (b) as compared to the LZC group

Fig. 3

Pharmacokinetic parameters of lutein in serum for test product (LZO) and reference product (LZC). a Mean serum lutein maximum concentration (C_max). b Lutein area under the curve (AUC) serum concentration versus time for 0–72 h (AUC_0–72) and 0 to last measurable concentration (AUC_0–t). C_max, AUC_0–72, and AUC_0–t were significantly (p < 0.05) higher for LZO compared to LZC

Fig. 4

Pharmacokinetic parameters of zeaxanthin in serum for test product (LZO) and reference product (LZC). a Mean serum zeaxanthin maximum concentration (C_max). b Zeaxanthin area under the curve (AUC) serum concentration versus time for 0–72 h (AUC_0–72) and 0 to last measurable concentration (AUC_0–t). C_max, AUC_0–72, and AUC_0–t were significantly (p < 0.05) higher for LZO compared to LZC