Comparative Pharmacokinetic Study of Standard Astaxanthin and its Micellar Formulation in Healthy Male Volunteers

• Published in: European journal of drug metabolism and pharmacokinetics Vol. 49; no. 4; pp. 467 - 475
• Main Authors: Khayyal, Mohamed T., Teaima, Mahmoud H., Marzouk, Hoda M., -Hazek, Rania M. El, Behnam, Frank, Behnam, Dariush
• Format: Journal Article
• Language: English
• Published: Cham Springer International Publishing 01-07-2024
• Subjects: Administration, Oral; Adult; Area Under Curve; Biological Availability; Biomedical and Life Sciences; Biomedicine; Capsules - pharmacokinetics; Chromatography, High Pressure Liquid - methods; Cross-Over Studies; Half-Life; Healthy Volunteers; Human Physiology; Humans; Male; Medical Biochemistry; Micelles; Original; Original Research Article; Pharmaceutical Sciences/Technology; Pharmacology/Toxicology; Pharmacy; Xanthophylls - administration & dosage; Xanthophylls - blood; Xanthophylls - pharmacokinetics; Young Adult
• ISSN: 0378-7966; 2107-0180; 2107-0180
• DOI: 10.1007/s13318-024-00898-0

Background and Objective
Astaxanthin is a naturally occurring carotenoid with high anti-oxidant properties, but it is a very lipophilic compound with low oral bioavailability. This study was conducted to compare the pharmacokinetic parameters of a novel astaxanthin preparation based on micellar solubilization technology, NovaSOL
®
400-mg capsules (Test product), and those of astaxanthin 400-mg capsules (reference product), after single oral dose administration to healthy male adults.
Methods
A single oral dose (400 mg equivalent to 8 mg astaxanthin) of test and reference astaxanthin were administered with 240 mL of water to 12 volunteers according to crossover design, in two phases, with a washout period of 1 week in between. Blood samples were collected at hourly intervals for the first 12 h, then at 24.0, 48.0, and 72.0 h after administration. Aliquots of plasma were centrifuged and the clear supernatant was injected into the high performance liquid chromatography–diode array detection (HPLC-DAD) system. Plasma concentration of astaxanthin versus time profiles were constructed, and the primary pharmacokinetic parameters, maximum concentration (
C
max
), area under concentration time curve from time of administration (0) to time (t) [AUC
0-t
] or to infinity ∞, [AUC
0-∞
],  half-life (
T
½
) and time to reach
C
max
(
T
max
) were calculated.
Results
The test micellar astaxanthin reached a
C
max
of 7.21 µg/ml after 3.67 h compared to only 3.86 µg/ml after 8.5 h for the reference native astaxanthin.
Conclusion
Micellar formulation of astaxanthin is capable of producing a high concentration of astaxanthin in plasma in a shorter time, thereby expected to provide faster potential therapeutic efficacy.