Abstract
Astaxanthin (Asta), a xanthophyll carotenoid, has been reported to be a strong antioxidative agent and has anti-inflammatory, antitumor and free radical-scavenging activities. However, inadequate stability and water solubility results in its low bioavailability. This study incorporated Asta into hydrophilic hyaluronan nanoparticles (HAn) to produce Asta-HAn aggregates (AHAna) using an electrostatic field system and investigated the restorative effects of AHAna on retrorsine-CCl4-induced liver fibrosis in rats in vivo. Transmission electron microscopy (TEM) revealed that the prepared HAn were approximately 15 ± 2.1 nm in diameter and after the incorporation of Asta into HAn, the size increased to 210–500 nm. The incorporation efficiency of Asta was approximately 93% and approximately 54% of Asta was released after incubation for 18 h. Significant reductions in alanine aminotransferase and aspartate aminotransferase levels were observed after the rats were intraperitoneally injected with AHAna. Histopathological findings revealed the greatest reduction in hepatic fibrosis and hepatocyte necrosis in the rats after 2 weeks of intraperitoneal injection with AHAna, which is consistent with the data acquired from serum biochemical analysis. The restorative effects on liver damage displayed by AHAna in vivo demonstrated that Asta aggregated through HAn incorporation exerts therapeutic effects on liver fibrosis and necrosis.
Highlights
Astaxanthin (Asta) is a xanthophyll carotenoid found in various marine animals and algae including Haematococcus pluvialis
The incorporation efficiency (IE) of Asta in the Asta-HAn aggregates (AHAna) was determined as follows: 1 mL of solution containing the prepared AHAna was added to a centrifuge tube and was subsequently solution containing the prepared AHAna was added to a centrifuge tube and was subsequently placed placed on a 40-rpm shaker at 37 °C
The sample was centrifuged at 14,000 rpm for 60 min before the amount amount of nonencapsulated Asta in the supernatant was used to determine the amount of Asta of nonencapsulated Asta in the supernatant was used to determine the amount of Asta through through high-performance liquid chromatography (HPLC, Agilent 1100 series; Agilent, Santa Clara, high-performance liquid chromatography (HPLC, Agilent 1100 series; Agilent, Santa Clara, CA, USA)
Summary
Astaxanthin (Asta) is a xanthophyll carotenoid found in various marine animals and algae including Haematococcus pluvialis. When the liver suffers huge and/or long-term injury, such as an excess of uptake and constant exposure to hepatotoxic substances or drugs, the liver may progress into a stage of functional deficiency to overwhelm or even inhibit the intrinsic regeneration or liver tissue repair, resulting in severe consequences such as delayed repair in liver, liver fibrosis, liver failure or death. Lipid-based liposomes, micelles and emulsions, as well as other biopolymeric nanoparticles such as chitosan and gelatin, which possess advantageous biocompatible and biodegradable features, are selected as carriers in the drug delivery system. These biodegradable nanoparticles provide favorable drug and vaccine encapsulation and convenient release profiles for numerous drugs, vaccines and biomolecules to enhance nanoparticle permeability, cellular uptake, bioavailability and retention. The effects of pure Asta, HAn and Asta–HAn aggregates (AHAna) on liver fibrosis and necrosis were investigated in vivo in a rat model
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