[Pharmacological activity of n-(1-phenethyl-4-piperidyl) propionanilide modified by encapsulation in PLGA nanoparticles].

Technological parameters for the effective encapsulation of n-(1-phenethyl-4-piperidyl)propionanilide in poly(lactid-co-glycolide) (PLG) nanoparticles have been determined. Depending on the ratio of drug fractions adsorbed on the particle surface and associated with the polymer matrix, n-(1-phenethyl-4-piperidyl)propionanilide (200 microg/kg, i/m) loaded PLG nanospheres accelerated time onset and increased duration of sleep in rats: by a factor of 1.6 - 2.0 for polymer associated drug fraction within 40 - 60% and by a factor of 2.2 - 2.6 for polymer associated drug fraction within 60 - 80%. A similar increase of sleep duration was observed when free n-(1-phenethyl-4-piperidyl)-propionanilide was administered at doses within 400 - 500 microg/kg.