The purpose of this study was to develop a potato protein (PP)-based delivery system for increasing oral bioavailability of lipophilic bioactives (nutraceuticals and drugs), using astxanthin (AX) as a model, and to evaluate the system in vivo in a crossover clinical study in human volunteers. Three different formulations were prepared, encapsulating AX oleoresin (AXO) with (1) PP only, (2) PP+lecithin (LEC), and (3) PP+olive oil (OO). In a randomized, double-blind, crossover study in human subjects, the PP-OO-AX formulation had a 4.8-fold higher median plasma AX area under the concentration-over time curve (AUC; P\<0.001) compared to the raw AXO formulation. In conclusion, a non-allergenic, vegan, PP based delivery system made of "all-natural ingredients" offers a great promise for increasing oral bioavailability of lipophilic bioactives such as AX, for the enrichment of food and for dietary supplements, or oral delivery of lipophilic drugs.
Astaxanthin (AX) is a red xanthophyll carotenoid found mainly in algae (notably Haematococcus Pluvialis microalga) and marine animals. AX is a stronger antioxidant than vitamin E and β-carotene but has very low oral bioavailability. The purpose of this study was to develop a potato protein (PP)-based delivery system for increasing oral bioavailability of lipophilic bioactives (nutraceuticals and drugs), using AX as a model, and to evaluate the system in vitro and in vivo in a crossover clinical study in human volunteers. Three different formulations were prepared, encapsulating AX oleoresin (AXO) with (1) PP only, (2) PP+lecithin (LEC), and (3) PP+olive oil (OO). The average particle diameters after preparation were 0.29, 0.29, and 1.76 μm, and after freeze-drying and reconstitution 0.17, 0.07, and 6.93 μm, respectively. In vitro bioaccessibility was 33, 47, and 69%, respectively, versus 16% only for the raw AXO. In a randomized, double-blind, crossover study in human subjects, the PP-OO-AX formulation had a 4.8-fold higher median plasma AX area under the concentration-over time curve (AUC; P\<0.001) compared to the raw AXO formulation. In conclusion, a non-allergenic, vegan, PP based delivery system made of "all-natural ingredients" offers a great promise for increasing oral bioavailability of lipophilic bioactives such as AX, for the enrichment of food and for dietary supplements, or oral delivery of lipophilic drugs.
Study Type
INTERVENTIONAL
Allocation
RANDOMIZED
Purpose
BASIC_SCIENCE
Masking
TRIPLE
Enrollment
13
single dose and plasma samples
Rambam Health Campus
Haifa, Israel
Plasma AX AUC
Plasma AX AUC of 13 participants after consuming either the microencapsulated AX or the reference AX oleoresin, measured during 72 hrs post-ingestion, in a cross over study.
Time frame: 1 year
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