Effects of apolipoproteins on dalargin transport across the blood-brain barrier.
Antinociceptive activity of dalargin (7.5 mg/kg) adsorbed on poly(butyl)cyanoacrylate nanoparticles with different coating was studied on outbred albino mice by the tail-flick test. poly(butyl)cyanoacrylate nanoparticles without coating did not increase the antinociceptive activity of dalargin and hence, did not increase its transport across the blood-brain barrier. poly(butyl)cyanoacrylate nanoparticles coated with apolipoprotein B, apolipoprotein E, and polysorbate 80 increased the transport of dalargin across the blood-brain barrier. Delivery of dalargin to the brain was most effective in case of using poly(butyl)cyanoacrylate nanoparticles with polysorbate 80 coating and subsequent supercoating with apolipoprotein E.
Shamenkov
D A
DA
Department of Pharmacology, Pharmaceutical Faculty, I. M. Sechenov Moscow Medical Academy, Russia. dshamenkov@yandex.ru
Petrov
V E
VE
Alyautdin
R N
RN
D000327:Adsorption; D000700:Analgesics / Q000494:pharmacology*; D000818:Animals; D021461:Animals, Outbred Strains; D001055:Apolipoproteins B / Q000008:administration & dosage / Q000493:pharmacokinetics*; D001057:Apolipoproteins E / Q000008:administration & dosage / Q000493:pharmacokinetics*; D001522:Behavior, Animal / Q000187:drug effects; D001692:Biological Transport / Q000187:drug effects / Q000502:physiology; D001812:Blood-Brain Barrier / Q000187:drug effects* / Q000502:physiology; D020099:Coated Materials, Biocompatible / Q000737:chemistry; D004337:Drug Carriers; D016503:Drug Delivery Systems / Q000379:methods; D004659:Enbucrilate / Q000737:chemistry; D016308:Enkephalin, Leucine-2-Alanine / Q000031:analogs & derivatives* / Q000494:pharmacology; D051379:Mice; D053758:Nanoparticles / Q000737:chemistry; D010316:Particle Size; D011136:Polysorbates / Q000008:administration & dosage / Q000493:pharmacokinetics; D013997:Time Factors
D000700:Analgesics; D001055:Apolipoproteins B; D001057:Apolipoproteins E; D020099:Coated Materials, Biocompatible; D004337:Drug Carriers; D011136:Polysorbates; D016308:Enkephalin, Leucine-2-Alanine; D004659:Enbucrilate; C040996:enkephalin-Leu, Ala(2)-Arg(6)-