Abstract
Background The present study was aimed to develop astaxanthin (AX)-loaded liposomes by the utilization of soybean phosphatidylcholine (PC) and lysophosphatidylcholine (LPC) to improve the nutraceutical properties of AX. AX-loaded liposomes consisting of PC (PC/AX) and LPC (LPC/AX) were evaluated in terms of particle size distribution, morphology, release characteristics, pharmacokinetic behavior, and nephroprotective effects in a rat model of acute kidney injury.
Results PC/AX and LPC/AX had uniform size distributions with a mean particle size of 254 and 148 nm, respectively. Under pH 6.8 conditions, both liposomes exhibited improved dissolution behavior of AX compared with crystalline AX (cAX). In particular, LPC/AX showed 7-fold higher release of AX than PC/AX. After the oral administration of LPC/AX (33.2 mg-AX/kg) to rats, there was a significant increase in systemic exposure to AX, as evidenced by a 15-fold higher AUC0–24 h than PC/AX. However, the oral absorption of AX in the cAX group was negligible. Based on the results of histological analysis and measurement of plasma biomarkers, LPC/AX exhibited improved nephroprotective effects of AX in the rat model of kidney injury.
Conclusion From these observations, a strategic application of LPC-based liposomal approach might be a promising option to improve the nutraceutical properties of AX.
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