Lysophosphatidylcholine‐based liposome to improve oral absorption and nephroprotective effects of astaxanthin

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 a sevenfold higher release of AX than PC/AX. After the oral administration of LPC/AX (33.2 mg AX kg−1) 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 the LPC‐based liposomal approach might be a promising option to improve the nutraceutical properties of AX. © 2022 Society of Chemical Industry.

Gynura procumbensLeaf Extract-Loaded Self-Microemulsifying Drug Delivery System Offers Enhanced Protective Effects in the Hepatorenal Organs of the Experimental Rats

“…This negative charge could be attributed to free fatty acids on the surface of emulsions derived from MCT, which may prevent particle aggregations due to the electric repulsion between particles 42 . As per a prior study, colloidal dispersions exhibit favorable stability when their zeta potential is high and negative, exceeding −20 mV 43 . This is because of the electric repulsion between the particles.…”

“…Cisplatin can penetrate renal epithelial cells via organic cation transporter 2 (OCT2) and copper transporter 1 (Ctr1), leading to mitochondrial DNA damage and elevated levels of reactive oxygen species (ROS). This ultimately leads to tubular apoptosis and necrosis 43,52 . The kidney tissues were examined under a light microscope after 72 h of cisplatin exposure.…”

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“…It was found that in the presence of LPC, the SUVs were smaller, and the LMVs had less leakage, but LPC did not exert any significant effect ( p > 0.05) on the transfer of carboxyfluorescein to the lymphocytes. A recent investigation [ 109 ] used LPC and phosphatidylcholine (PC) for the manufacture of liposomes in order to improve nephroprotective effects and the oral absorption of astaxanthin. The authors reported that at a pH close to neutral (pH 6.8), such liposomes exhibited an improved dissolution behaviour of astaxanthin when compared to the behaviour of untreated/crystalline astaxanthin.…”

“…Particularly, the release of astaxanthin from the liposome-containing LPC was seven-fold higher than that of those manufactured using PC, besides a significant increase ( p < 0.05) in systemic exposure to astaxanthin (a 15-fold higher after 24 h after oral administration), when compared to liposomes made of PC. Based on the results obtained from histological analysis and plasma biomarkers in the rat model of kidney injury, the researchers concluded that the LPC-based liposomes exhibited the improved nephroprotective effects of astaxanthin [ 109 ]. Therefore, these findings suggest that an LPC-based liposomal approach might provide a sustainable option for improving the bio-efficacy of astaxanthin, which may be applicable to other lipophilic bioactive ingredients as well.…”