Adv Ther. 2026 Jul 14. doi: 10.1007/s12325-026-03713-1. Online ahead of print.
ABSTRACT
INTRODUCTION: Lutein is a dietary xanthophyll carotenoid with established roles in ocular health, yet its systemic bioavailability is highly variable and dependent on the nature of the formulation. This study was designed to compare the bioavailability and pharmacokinetic profile of a newly formulated oil suspension of lutein (LUT) with a commercially available reference lutein formulation (REF), following a single oral dose under fed conditions in healthy adults.
METHODS: This was a randomized, double-blind, single-dose, parallel-group comparative bioavailability study conducted in healthy adult male subjects (n = 80). Subjects received a single oral dose of 25 mg lutein as either LUT or REF under standardized high-fat fed conditions. Serial blood samples were collected – 2.00 and 0.00 h (pre-dose) and 2.00, 4.00, 6.00, 8.00, 10.00, 12.00, 24.00, 48.00 and 72.00 h (post-dose). Serum lutein concentrations were quantified using a validated HPLC method. Pharmacokinetic parameters, including Cmax, Tmax, AUC0-24, AUC0-48, AUC0-72, AUC0-t, and AUC0-∞, were calculated using Phoenix WinNonlin 6.4 software by non-compartmental analysis. Statistical comparisons were performed on log-transformed parameters using ANOVA by SAS® version 9.4.
RESULTS: Peak serum lutein concentrations were observed between 12 and 24 h post-dose for both formulations. LUT demonstrated significantly higher baseline-corrected serum lutein concentrations than REF from 8 h through 72 h (p < 0.05). Maximum serum concentration (Cmax) for LUT was approximately 32% higher than REF (p < 0.05). Total systemic bioavailability was significantly greater for LUT, with AUC0-48, AUC0-72, and AUC0-t increased by approximately 35%, 39%, and 38%, respectively, compared with REF (p < 0.05). AUC0-∞ for LUT was 78% higher compared to REF. Further, LUT showed consistently > 2 folds higher serum lutein levels from baseline across all post-dose time points compared to REF. Both formulations were well tolerated, with no product-related adverse events reported.
CONCLUSION: The LUT formulation provides significantly greater systemic lutein bioavailability than the reference formulation following single-dose administration under fed conditions, highlighting the critical influence of formulation design on lutein bioavailability. Future clinical efficacy studies are warranted to evaluate the impact of this enhanced bioavailability.
TRIAL REGISTRATION: Clinical Trials Registry of India: CTRI/2018/01/011167.
PMID:42449082 | DOI:10.1007/s12325-026-03713-1
