Chromatographic analysis of iodoacetate encapsulated in liposomes and biochemical assessment of its toxic effect during course application

Glycolysis inhibitors are currently considered as potential anticancer agents due to the fact that significant changes occur in tumor cells, known as metabolic reprogramming. So, in particular, changes in carbohydrate metabolism are called the Warburg effect. However, the use of carbohydrate metabolism inhibitors is severely limited due to the fact that they have pronounced systemic toxicity. But there is a possibility of using metabolic inhibitors, subject to targeted delivery. One of the key such approaches is the use of liposomal forms of drugs.

We have carried out studies comparing the systemic toxicity of the glycolysis inhibitor iodoacetate and its liposomal form.

Using HPLC, the optimal conditions for obtaining iodoacetate encapsulated in liposomes and its final concentration in them were established. Thanks to biochemical blood analysis, it was found that iodoacetate disrupts carbohydrate metabolism and has a pronounced cardiotoxic effect, but does not have hepatotoxic manifestations. Based on the indicators of biochemical markers of the toxic effect of iodoacetate encapsulated in liposomes, it was found that when administered in a course for two weeks, iodoacetate in this form has neither cardiotoxic nor any other negative effects on target organs, that is, it is safe.

Thus, iodoacetate in the form of liposomes has great potential as an anticancer agent, especially in the case of polypharmacy.