dc.contributor.author |
Pashirova T. |
|
dc.contributor.author |
Zueva I. |
|
dc.contributor.author |
Petrov K. |
|
dc.contributor.author |
Lukashenko S. |
|
dc.contributor.author |
Nizameev I. |
|
dc.contributor.author |
Kulik N. |
|
dc.contributor.author |
Voloshina A. |
|
dc.contributor.author |
Almasy L. |
|
dc.contributor.author |
Kadirov M. |
|
dc.contributor.author |
Masson P. |
|
dc.contributor.author |
Souto E. |
|
dc.contributor.author |
Zakharova L. |
|
dc.contributor.author |
Sinyashin O. |
|
dc.date.accessioned |
2019-01-22T20:38:37Z |
|
dc.date.available |
2019-01-22T20:38:37Z |
|
dc.date.issued |
2018 |
|
dc.identifier.issn |
0927-7765 |
|
dc.identifier.uri |
https://dspace.kpfu.ru/xmlui/handle/net/148091 |
|
dc.description.abstract |
© 2018 Elsevier B.V. New mixed cationic liposomes based on L-α-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 μg mL–1) and Bacillus cereus (MIC=7.8 μg 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 (∼ 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. |
|
dc.relation.ispartofseries |
Colloids and Surfaces B: Biointerfaces |
|
dc.subject |
Acetylcholinesterase |
|
dc.subject |
Cationic liposomes |
|
dc.subject |
Drug delivery systems |
|
dc.subject |
Organophosphorus agent |
|
dc.subject |
Paraoxon |
|
dc.subject |
Pralidoxime chloride |
|
dc.subject |
Self-assembly |
|
dc.subject |
Surfactant |
|
dc.title |
Mixed cationic liposomes for brain delivery of drugs by the intranasal route: The acetylcholinesterase reactivator 2-PAM as encapsulated drug model |
|
dc.type |
Article |
|
dc.relation.ispartofseries-volume |
171 |
|
dc.collection |
Публикации сотрудников КФУ |
|
dc.relation.startpage |
358 |
|
dc.source.id |
SCOPUS09277765-2018-171-SID85050484821 |
|