Intranasal tetrandrine temperature-sensitive in situ hydrogels for the treatment of microwave-induced brain injury.
Administration, Intranasal
Administration, Oral
Animals
Behavior, Animal
/ drug effects
Benzylisoquinolines
/ administration & dosage
Blood-Brain Barrier
/ metabolism
Brain
/ drug effects
Brain Injuries
/ drug therapy
Calcium Channel Blockers
/ administration & dosage
Calcium Channels
/ drug effects
Delayed-Action Preparations
Disease Models, Animal
Drug Compounding
Drug Liberation
Hydrogels
Male
Microwaves
Poloxamer
/ chemistry
Rats, Wistar
Stimuli Responsive Polymers
/ chemistry
Temperature
Tissue Distribution
Viscosity
Blood-brain barrier (BBB)
Brain targeting
In situ hydrogels
Intranasal administration
Microwave
Temperature-sensitive
Journal
International journal of pharmaceutics
ISSN: 1873-3476
Titre abrégé: Int J Pharm
Pays: Netherlands
ID NLM: 7804127
Informations de publication
Date de publication:
15 Jun 2020
15 Jun 2020
Historique:
received:
04
03
2020
revised:
13
04
2020
accepted:
27
04
2020
pubmed:
7
5
2020
medline:
27
2
2021
entrez:
7
5
2020
Statut:
ppublish
Résumé
The brain is the most sensitive organ to microwave radiation. However, few effective drugs are available for the treatment of microwave-induced brain injury due to the poor drug permeation into the brain. Here, intranasal tetrandrine (TET) temperature-sensitive in situ hydrogels (ISGs) were prepared with poloxamers 407 and 188. Its characteristics were evaluated, including rheological properties, drug release in vitro, and mucosal irritation. The pharmacodynamics and brain-targeting effects were also studied. The highly viscous ISGs remained in the nasal cavity for a long time with the sustained release of TET and no obvious ciliary toxicity. Intranasal temperature-sensitive TET ISGs markedly improved the spatial memory and spontaneous exploratory behavior induced by microwave with the Morris water maze (MWM) and the open field test (OFT) compared to the model. The ISGs alleviated the microwave-induced brain damage and inhibited the certain mRNA expressions of calcium channels in the brain. Intranasal temperature-sensitive TET ISGs was rapidly absorbed with a shorter T
Identifiants
pubmed: 32371003
pii: S0378-5173(20)30368-9
doi: 10.1016/j.ijpharm.2020.119384
pii:
doi:
Substances chimiques
Benzylisoquinolines
0
Calcium Channel Blockers
0
Calcium Channels
0
Delayed-Action Preparations
0
Hydrogels
0
Stimuli Responsive Polymers
0
Poloxamer
106392-12-5
tetrandrine
29EX23D5AJ
Types de publication
Comparative Study
Journal Article
Langues
eng
Sous-ensembles de citation
IM
Pagination
119384Informations de copyright
Copyright © 2020 Elsevier B.V. All rights reserved.
Déclaration de conflit d'intérêts
Declaration of Competing Interest The authors declare that they have no known competing financial interests or personal relationships that could have appeared to influence the work reported in this paper.