title: [Pharmacological activity of n-(1-phenethyl-4-piperidyl) propionanilide modified by encapsulation in PLGA nanoparticles].
abstract: 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.
authors: M A
authors: MA
authors: Tiunin
authors: T M
authors: TM
authors: Korniukhina
authors: A S
authors: AS
authors: Nikiforov
authors: V N
authors: VN
authors: Bykov
authors: S V
authors: SV
authors: Chepur
mesh_terms: D000818:Animals; D004337:Drug Carriers / Q000737:chemistry*; D004339:Drug Compounding / Q000379:methods*; D006993:Hypnotics and Sedatives / Q000737:chemistry / Q000494:pharmacology*; D007273:Injections, Intramuscular; D019344:Lactic Acid / Q000737:chemistry*; D008297:Male; D053758:Nanoparticles / Q000737:chemistry*; D010316:Particle Size; D010880:Piperidines / Q000737:chemistry / Q000494:pharmacology*; D020442:Poloxamer / Q000737:chemistry; D011100:Polyglycolic Acid / Q000737:chemistry*; D000077182:Polylactic Acid-Polyglycolic Acid Copolymer; D051381:Rats; D012890:Sleep / Q000187:drug effects*
chemical_list: D004337:Drug Carriers; D006993:Hypnotics and Sedatives; D010880:Piperidines; D020442:Poloxamer; D000077182:Polylactic Acid-Polyglycolic Acid Copolymer; D011100:Polyglycolic Acid; D019344:Lactic Acid