Liposomal form with lipoic acid and carnosine: production, antiplatelet and antioxidant effect

Optimal conditions were selected for obtaining the liposomal form with lipoic acid (LA) and carnosine. Using methods of active and passive loading, it was possible to achieve high efficiency inclusion of carnosine (60±5%) and lipoic acid (75±5%) in nanoparticles (NPs). It has been shown that the addition of sucrose or cholesterol (Chol) to nanodispersions (NDs) led to a slight decrease in the efficiency incorporation of carnosine in nanoparticles (45±5%). The production of PC-liposomes (PC-Ls) with LA and carnosine by passive loading led to a significant decrease in the efficiency inclusion of carnosine in liposomes (16%). At the same time, the efficiency of inclusion of LA in PC liposomes using methods of both passive and active loading practically did not change (58-69%). It has been found that the obtained nanodispersions are homogeneous system of nanoparticles with size of 175-250 nm. By transmission electron microscopy, it has been shown that LA+Carn. Liposomes represent a homogeneous system consisting mainly of spherical nanoparticles with a size of 120-200 nm. It is important to note that the obtained liposomes with LA and carnosine are stable during long-term storage (15 months) at + 4 ° and at room temperature. It was established that liposomes LA with Carn exhibit an antioxidant effect, leading to a 15-fold decrease in the concentration of lipid peroxidation products. The effect of the obtained liposomal forms on platelet aggregation caused by arachidonic acid has been revealed. It has been found, that liposomes with LA and carnosine reduce the degree of aggregation of platelets by 60-70%, relative to controls.