PMID- 30059851
OWN - NLM
STAT- MEDLINE
DCOM- 20181221
LR  - 20181221
IS  - 1873-4367 (Electronic)
IS  - 0927-7765 (Linking)
VI  - 171
DP  - 2018 Nov 1
TI  - Mixed cationic liposomes for brain delivery of drugs by the intranasal route: The 
      acetylcholinesterase reactivator 2-PAM as encapsulated drug model.
PG  - 358-367
LID - S0927-7765(18)30497-1 [pii]
LID - 10.1016/j.colsurfb.2018.07.049 [doi]
AB  - New mixed cationic liposomes based on L-alpha-phosphatidylcholine and 
      dihexadecylmethylhydroxyethylammonium bromide (DHDHAB) were designed to overcome 
      the BBB crossing by using the intranasal route. Synthesis and self-assembly of 
      DHDHAB were performed. A low critical association concentration (0.01 mM), good 
      solubilization properties toward hydrophobic dye Orange OT and antimicrobial 
      activity against gram-positive bacteria Staphylococcus aureus (MIC=7.8 mug mL(-1)) 
      and Bacillus cereus (MIC=7.8 mug mL(-1)), low hemolytic activities against human 
      red blood cells (less than 10%) were achieved. Conditions for preparation of 
      cationic vesicles and mixed liposomes with excellent colloidal stability at room 
      temperature were determined. The intranasal administration of rhodamine B-loaded 
      cationic liposomes was shown to increase bioavailability into the brain in 
      comparison to the intravenous injection. The cholinesterase reactivator, 2-PAM, 
      was used as model drug for the loading in cationic liposomes. 2-PAM-loaded 
      cationic liposomes displayed high encapsulation efficiency ( approximately  90%) and 
      hydrodynamic diameter close to 100 nm. Intranasally administered 2-PAM-loaded 
      cationic liposomes were effective against paraoxon-induced acetylcholinesterase 
      inhibition in the brain. 2-PAM-loaded liposomes reactivated 12 +/- 1% of brain 
      acetylcholinesterase. This promising result opens the possibility to use marketed 
      positively charged oximes in medical countermeasures against organophosphorus 
      poisoning for reactivation of central acetylcholinesterase by implementing a 
      non-invasive approach, via the "nose-brain" pathway.
CI  - Copyright (c) 2018 Elsevier B.V. All rights reserved.
FAU - Pashirova, Tatiana N
AU  - Pashirova TN
AD  - Arbuzov Institute of Organic and Physical Chemistry, FRC Kazan Scientific Center 
      of RAS, Arbuzov St., 8, Kazan, 420088, Russia. Electronic address: 
      tatyana_pashirova@mail.ru.
FAU - Zueva, Irina V
AU  - Zueva IV
AD  - Arbuzov Institute of Organic and Physical Chemistry, FRC Kazan Scientific Center 
      of RAS, Arbuzov St., 8, Kazan, 420088, Russia.
FAU - Petrov, Konstantin A
AU  - Petrov KA
AD  - Arbuzov Institute of Organic and Physical Chemistry, FRC Kazan Scientific Center 
      of RAS, Arbuzov St., 8, Kazan, 420088, Russia; Kazan Federal University, 
      Kremlyovskaya St., 18, Kazan, 420008, Russia.
FAU - Lukashenko, Svetlana S
AU  - Lukashenko SS
AD  - Arbuzov Institute of Organic and Physical Chemistry, FRC Kazan Scientific Center 
      of RAS, Arbuzov St., 8, Kazan, 420088, Russia.
FAU - Nizameev, Irek R
AU  - Nizameev IR
AD  - Arbuzov Institute of Organic and Physical Chemistry, FRC Kazan Scientific Center 
      of RAS, Arbuzov St., 8, Kazan, 420088, Russia; Kazan National Research 
      Technological University, Karl Marx St., 68, 420015, Kazan, Russia.
FAU - Kulik, Natalya V
AU  - Kulik NV
AD  - Arbuzov Institute of Organic and Physical Chemistry, FRC Kazan Scientific Center 
      of RAS, Arbuzov St., 8, Kazan, 420088, Russia.
FAU - Voloshina, Aleksandra D
AU  - Voloshina AD
AD  - Arbuzov Institute of Organic and Physical Chemistry, FRC Kazan Scientific Center 
      of RAS, Arbuzov St., 8, Kazan, 420088, Russia.
FAU - Almasy, Laszlo
AU  - Almasy L
AD  - Institute for Solid State Physics and Optics, Wigner Research Centre for Physics, 
      Hungarian Academy of Sciences, Budapest, Hungary.
FAU - Kadirov, Marsil K
AU  - Kadirov MK
AD  - Arbuzov Institute of Organic and Physical Chemistry, FRC Kazan Scientific Center 
      of RAS, Arbuzov St., 8, Kazan, 420088, Russia; Kazan National Research 
      Technological University, Karl Marx St., 68, 420015, Kazan, Russia.
FAU - Masson, Patrick
AU  - Masson P
AD  - Kazan Federal University, Kremlyovskaya St., 18, Kazan, 420008, Russia.
FAU - Souto, Eliana B
AU  - Souto EB
AD  - Department of Pharmaceutical Technology, Faculty of Pharmacy, University of 
      Coimbra, Coimbra, Portugal; REQUIMTE/LAQV, Group of Pharmaceutical Technology, 
      Faculty of Pharmacy, University of Coimbra, Coimbra, Portugal.
FAU - Zakharova, Lucia Ya
AU  - Zakharova LY
AD  - Arbuzov Institute of Organic and Physical Chemistry, FRC Kazan Scientific Center 
      of RAS, Arbuzov St., 8, Kazan, 420088, Russia.
FAU - Sinyashin, Oleg G
AU  - Sinyashin OG
AD  - Arbuzov Institute of Organic and Physical Chemistry, FRC Kazan Scientific Center 
      of RAS, Arbuzov St., 8, Kazan, 420088, Russia.
LA  - eng
PT  - Journal Article
DEP - 20180724
PL  - Netherlands
TA  - Colloids Surf B Biointerfaces
JT  - Colloids and surfaces. B, Biointerfaces
JID - 9315133
RN  - 0 (Anti-Bacterial Agents)
RN  - 0 (Cations)
RN  - 0 (Cholinesterase Reactivators)
RN  - 0 (Liposomes)
RN  - 0 (Pralidoxime Compounds)
RN  - 0 (Quaternary Ammonium Compounds)
RN  - 0 (Rhodamines)
RN  - EC 3.1.1.7 (Acetylcholinesterase)
RN  - K7G5SCF8IL (rhodamine B)
RN  - P7MU9UTP52 (pralidoxime)
RN  - Q9CX8P80JW (Paraoxon)
SB  - IM
MH  - Acetylcholinesterase/metabolism
MH  - Administration, Intranasal
MH  - Anti-Bacterial Agents/administration & dosage/chemical 
      synthesis/chemistry/*pharmacology
MH  - Bacillus cereus/drug effects
MH  - Brain/*drug effects/metabolism
MH  - Cations/chemistry
MH  - Cholinesterase Reactivators/administration & dosage/chemistry/*pharmacology
MH  - *Drug Delivery Systems
MH  - Liposomes/chemistry
MH  - Paraoxon/antagonists & inhibitors/pharmacology
MH  - Particle Size
MH  - Pralidoxime Compounds/administration & dosage/chemistry/*pharmacology
MH  - Quaternary Ammonium Compounds/chemical synthesis/chemistry/*pharmacology
MH  - Rhodamines/administration & dosage/chemistry
MH  - Staphylococcus aureus/drug effects
MH  - Surface Properties
OTO - NOTNLM
OT  - Acetylcholinesterase
OT  - Cationic liposomes
OT  - Drug delivery systems
OT  - Organophosphorus agent
OT  - Paraoxon
OT  - Pralidoxime chloride
OT  - Self-assembly
OT  - Surfactant
EDAT- 2018/07/31 06:00
MHDA- 2018/12/24 06:00
CRDT- 2018/07/31 06:00
PHST- 2018/03/24 00:00 [received]
PHST- 2018/07/21 00:00 [revised]
PHST- 2018/07/23 00:00 [accepted]
PHST- 2018/07/31 06:00 [pubmed]
PHST- 2018/12/24 06:00 [medline]
PHST- 2018/07/31 06:00 [entrez]
AID - S0927-7765(18)30497-1 [pii]
AID - 10.1016/j.colsurfb.2018.07.049 [doi]
PST - ppublish
SO  - Colloids Surf B Biointerfaces. 2018 Nov 1;171:358-367. doi: 
      10.1016/j.colsurfb.2018.07.049. Epub 2018 Jul 24.