In-vitro and in-vivo evaluation of chitosan-based thermosensitive gel containing lorazepam NLCs for the treatment of status epilepticus.
IET Nanobiotechnol
; 14(2): 148-154, 2020 Apr.
Article
in En
| MEDLINE
| ID: mdl-32433032
ABSTRACT
The objective of this study was to develop an in-situ gel containing lorazepam (LZM) loaded nanostructured lipid carriers (NLCs) for direct nose-to-brain delivery in order to increase drug therapeutic efficacy in the treatment of epilepsy. Accordingly, LZM loaded NLCs were formulated using emulsification solvent diffusion and evaporation method; then the effects of the formulation variables on different physicochemical characteristics of NLCs were investigated. Thermosensitive in-situ gels containing LZM-NLCs were prepared using a combination of chitosan and ß-glycerol phosphate (ß-GP). The anticonvulsant efficacy of LZM-NLCs-Gel was then examined using the pentylenetetrazole (PTZ) model. The optimised NLCs were spherical, showing the particle size of 71.70 ± 5.16â
nm and the zeta potential of -20.06 ± 2.70â
mV. The pH and gelation time for the chitosan solution with 15% (w/v) ß-GP were determined to be 7.12 ± 0.03 and 5.33 ± 0.58â
min, respectively. The in-vivo findings showed that compared with the control group and the group that received LZM-Gel, the occurrence of PTZ-induced seizures in the rats was significantly reduced by LZM-NLCs-Gel after intranasal administration. These results, therefore, suggested that the LZM-NLCs-Gel system could have potential applications for brain targeting through nasal route and might increase LZM therapeutic efficacy in the treatment of epilepsy.
Full text:
1
Collection:
01-internacional
Database:
MEDLINE
Main subject:
Status Epilepticus
/
Chitosan
/
Nanostructures
/
Gels
/
Lorazepam
Limits:
Animals
Language:
En
Journal:
IET Nanobiotechnol
Journal subject:
BIOTECNOLOGIA
Year:
2020
Document type:
Article
Affiliation country: