Details

Autor(en) / Beteiligte

• Khayyal, Mohamed T.
• Teaima, Mahmoud H.
• Marzouk, Hoda M.
• -Hazek, Rania M. El
• Behnam, Frank
• Behnam, Dariush

Titel

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

Ist Teil von

• European journal of drug metabolism and pharmacokinetics, 2024-07, Vol.49 (4), p.467-475

Ort / Verlag

Cham: Springer International Publishing

Erscheinungsjahr

2024

Quelle

MEDLINE

Beschreibungen/Notizen

• 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.