Fryazino, Moscow, Russian Federation
Moscow, Moscow, Russian Federation
Moscow, Moscow, Russian Federation
Moscow, Moscow, Russian Federation
Moscow, Moscow, Russian Federation
Moscow, Moscow, Russian Federation
Moscow, Moscow, Russian Federation
The optimal conditions were selected for obtaining the liposomal form, containing carnosine with lipoic acid. Using methods of active and passive loading, it was possible to achieve a sufficiently high efficiency inclusion of lipoic acid (EI = 69%) and carnosine (EI = 56%) into liposomes. It has been found that the addition of cholesterol or sucrose to PC liposomes led to a slight decrease of efficiency incorporation of carnosine into nanoparticles (EI = 31-38%). The preparation of PC liposomes with LA and carnosine by the method of passive loading led to a significant (3-fold) decrease in the efficiency inclusion of carnosine (EI = 16%) into liposomes. At the same time, the efficiency incorporating of LA into PC liposomes when using methods passive and active loading practically did not change (EI = 58-69%). It has been established that the obtained liposomes represent a homogeneous system of nanoparticles with the size of 185-260 nm. The method of electron microscopy was used to study the morphology of nanoforms. It has been found that liposomes with LA/Carn. represent a homogeneous system consisting mainly of spherical nanoparticles with a size of 150-250 nm, and empty PC liposomes form small aggregates. It should be noted that the obtained liposomal drugs are stable during long-term storage at room temperature and do not form any aggregates. The effect of the obtained liposomes on platelet (Pt) aggregation induced by arachidonic acid (AA) was evaluated. It has been revealed that the liposomes, containing LA and carnosine, suppresses platelet aggregation by 50-60%, relative to the control (Pt + AA), while empty PC liposomes and water-soluble forms of Carn and LA practically do not affect the Pt aggregation, caused by this inductor.
liposomes, carnosine, lipoic acid, arachidonic acid
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