Stabilized Nanoemulsions of Astaxanthin Esters of Known Fatty-Acid Composition
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Pharmaceutical Chemistry Journal, Vol. 54, No. 8, November, 2020 (Russian Original Vol. 54, No. 8, August, 2020)
DRUG SYNTHESIS METHODS AND MANUFACTURING TECHNOLOGY STABILIZED NANOEMULSIONS OF ASTAXANTHIN ESTERS OF KNOWN FATTY-ACID COMPOSITION I. S. Kulikova,1,* N. Yu. Lotosh,1 V. A. Turanova,2 and A. A. Selishcheva1,3 Translated from Khimiko-Farmatsevticheskii Zhurnal, Vol. 54, No. 8, pp. 18 – 22, August, 2020.
Original article submitted May 29, 2020. The aim of the present study was to develop astaxanthin ester nanoemulsions with phosphatidylcholine and evaluate their stability during storage under various conditions. Monoesters were obtained by column chromatography of an oil extract of Haematococcus pluvialis and mixed astaxanthin esters. Monoester fatty-acid compositions were determined by HPLC. A solution of astaxanthin monoesters or a mixture of astaxanthin mono- and diesters in 5% aqueous EtOH was rapidly degraded in light at room temperature. The addition of antioxidants such as ascorbic acid and butylated hydroxytoluene did not give significant positive results. In contrast, simultaneous addition of albumin, which was used for these purposes for the first time, increased significantly the shelf life. The optimized conditions for producing nanoemulsions from astaxanthin esters and phosphatidylcholine by injection gave nanoemulsions with an average particle size of 50 nm that remained physically and chemically stable during storage for a month. Keywords: astaxanthin, astaxanthin esters, fatty-acid composition, nanoemulsions, phosphatidylcholine.
These compounds are difficult to use because of their poor water solubility and instability in light. AST and extract from H. pluvialis are usually used as oil extracts, which can adversely affect the drug bioavailability. Antioxidants and encapsulation are used for stabilization in light [7]. Solubility problems are solved in two ways. One way is chemical synthesis to add additional groups to the AST molecule that increase the water solubility, e.g., lysine [8]. The other approach involves the creation of a dispersion in which AST and its esters are incorporated into various particles [9, 10].
The carotenoid astaxanthin (AST) (3,3¢-dihydroxy-4,4¢dioxo-b-carotene) (Fig. 1) is synthesized in the free form (unesterified) and as mono- and diesters in cells of the microalga Haematococcus pluvialis stressed by excessive illumination and elevated salt content [1]. Recently, this compound has attracted increased interest because AST showed various potential biological activities in vitro and in vivo [2], primarily antioxidant activity that exceeded those of vitamins C and E and b-carotene [3]. AST is used as a preventive agent that effectively stimulates immunity and exhibits hepatoprotective activity [4]. It was shown to have a positive effect on diabetes, cardiovascular diseases, and neurodegenerative disorders [2, 5, 6]. 1 2 3 *
National Research Center Kurchatov Institute, 1 Acad. Kurchatov Sq., Moscow, 123182 Russia. D. I. Mendeleev University of Chemical Technol
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