Abstract

A liposomal form of anticancer drugs is often used to improve pharmacokinetics and reduce systemic toxicity of the drugs. The goal of the study is to develop a method for quantitative analysis of a liposomal form of sodium iodoacetate (IA), glycolysis inhibitor, which exhibits a pronounced antitumor activity. Liposomes were prepared by extrusion at a temperature of 25 – 55°C under argon pressure ranged from 2 to 10 MPa. The obtained liposomes were purified from the non-incorporated component using dialysis. The method of HPLC was used to analyze the inhibitor solution in liposomes. The method of hydrophilic interaction chromatography revealed a high selectivity of iodoacetate with aminopropyl silica gel as a stationary phase. The best option for analysis was to use a spectrophotometric detector. The results of analysis showed that the dose of the inhibitor in 1 ml of liposomes was 0.20 – 0.23 mg regardless of the liposome size. In terms of the weight of an animal, the amount of iodoacetate was 8 – 9 mg/kg. The analysis of liposomes by the developed method showed that the highest yield and a high degree of purification is attained at low temperature (no more than 40°C) and duration of dialysis for about 3 h. For these purposes, the use of liposomes with a diameter of 400 nm turned out to be the best option.

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