PMID- 7773690 OWN - NLM STAT- MEDLINE DCOM- 19950711 LR - 20190614 IS - 0006-8993 (Print) IS - 0006-8993 (Linking) VI - 674 IP - 1 DP - 1995 Mar 13 TI - Passage of peptides through the blood-brain barrier with colloidal polymer particles (nanoparticles). PG - 171-4 AB - Transport of the hexapeptide dalargin across the blood-brain barrier was accomplished using a nanoparticle formulation. The formulation consisted of dalargin bound to poly(butyl cyanoacrylate) nanoparticles by sorption, coated with polysorbate 80. Intravenous injection of this formulation to mice resulted in an analgesic effect. All controls, including a simple mixture of the three components (drugs, nanoparticles, and surfactant) mixed directly before i.v. injection, exhibited no effect. Analgesia was also prevented by pretreatment with naloxone. Fluorescent and electron microscopic studies indicated that the passage of the particle-bound drug occurred by phagocytic uptake of the polysorbate 80-coated nanoparticles by the brain blood vessel endothelial cells. FAU - Kreuter, J AU - Kreuter J AD - Institut fur Pharmazeutische Technologie, Johann Wolfgang Goethe-Universitat, Frankfurt am Main, Germany. FAU - Alyautdin, R N AU - Alyautdin RN FAU - Kharkevich, D A AU - Kharkevich DA FAU - Ivanov, A A AU - Ivanov AA LA - eng PT - Journal Article PT - Research Support, Non-U.S. Gov't PL - Netherlands TA - Brain Res JT - Brain research JID - 0045503 RN - 0 (Colloids) RN - 0 (Peptides) RN - 0 (Polymers) RN - 0 (Polysorbates) RN - 63631-40-3 (Enkephalin, Leucine-2-Alanine) RN - V13505565P (enkephalin-Leu, Ala(2)-Arg(6)-) SB - IM MH - Animals MH - *Blood-Brain Barrier MH - Colloids/*pharmacokinetics MH - Enkephalin, Leucine-2-Alanine/analogs & derivatives/pharmacokinetics MH - Injections, Intravenous MH - Male MH - Mice MH - Mice, Inbred ICR MH - Microscopy, Electron MH - Microscopy, Fluorescence MH - Particle Size MH - Peptides/*pharmacokinetics MH - Polymers/*pharmacokinetics MH - Polysorbates EDAT- 1995/03/13 00:00 MHDA- 1995/03/13 00:01 CRDT- 1995/03/13 00:00 PHST- 1995/03/13 00:00 [pubmed] PHST- 1995/03/13 00:01 [medline] PHST- 1995/03/13 00:00 [entrez] AID - 0006-8993(95)00023-J [pii] AID - 10.1016/0006-8993(95)00023-j [doi] PST - ppublish SO - Brain Res. 1995 Mar 13;674(1):171-4. doi: 10.1016/0006-8993(95)00023-j.