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Pegylated nanoparticles for the oral delivery of nimodipine: Pharmacokinetics and effect on the anxiety and cognition in mice.
- Source :
-
International journal of pharmaceutics [Int J Pharm] 2018 May 30; Vol. 543 (1-2), pp. 245-256. Date of Electronic Publication: 2018 Mar 28. - Publication Year :
- 2018
-
Abstract
- Nimodipine may be of interest to treat behavioral alterations and memory deficits. However, its oral administration is hampered by a low bioavailability. The aim of this work was to develop pegylated nanoparticles as oral carriers of nimodipine and test their capability to both reverse the anxiety and protect against cognitive impairment of in stressed mice. Pegylated nanoparticles (NMD-NP/PEG), with a size of 190 nm and a payload of 68 µg/mg, significantly improve the oral bioavailability of nimodipine; about 7-times higher than for the control drug solution (62% vs 9%). The effect of oral nimodipine on the anxiety and cognitive capabilities in a model of stressed mice was also evaluated. NMD-NP/PEG displayed a poor effect on the anxiety-like behavior of animals. Nevertheless, only the treatment with NMD-NP/PEG exerted a protective effect against the memory impairments induced by chronic corticosterone administration, improving the cognitive capabilities of animals when compared with controls. These pegylated nanocarriers may represent a useful strategy to develop new oral treatments for preventing from cognitive impairments.<br /> (Copyright © 2018 Elsevier B.V. All rights reserved.)
- Subjects :
- Administration, Oral
Animals
Anxiety blood
Anxiety drug therapy
Behavior, Animal drug effects
Calcium Channel Blockers blood
Calcium Channel Blockers chemistry
Calcium Channel Blockers pharmacokinetics
Cognition drug effects
Corticosterone blood
Drug Carriers chemistry
Drug Carriers pharmacokinetics
Drug Liberation
Locomotion drug effects
Male
Maze Learning drug effects
Mice, Inbred C57BL
Nanoparticles chemistry
Neuroprotective Agents blood
Neuroprotective Agents chemistry
Neuroprotective Agents pharmacokinetics
Nimodipine blood
Nimodipine chemistry
Nimodipine pharmacokinetics
Polyethylene Glycols chemistry
Polyethylene Glycols pharmacokinetics
Rats, Wistar
Stress, Psychological blood
Stress, Psychological drug therapy
Calcium Channel Blockers administration & dosage
Drug Carriers administration & dosage
Nanoparticles administration & dosage
Neuroprotective Agents administration & dosage
Nimodipine administration & dosage
Polyethylene Glycols administration & dosage
Subjects
Details
- Language :
- English
- ISSN :
- 1873-3476
- Volume :
- 543
- Issue :
- 1-2
- Database :
- MEDLINE
- Journal :
- International journal of pharmaceutics
- Publication Type :
- Academic Journal
- Accession number :
- 29604372
- Full Text :
- https://doi.org/10.1016/j.ijpharm.2018.03.048