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Duloxetine loaded-microemulsion system to improve behavioral activities by upregulating serotonin and norepinephrine in brain for the treatment of depression.
- Source :
-
Journal of psychiatric research [J Psychiatr Res] 2018 Apr; Vol. 99, pp. 83-95. Date of Electronic Publication: 2018 Jan 31. - Publication Year :
- 2018
-
Abstract
- Duloxetine is a well-known antidepressant molecule which is used in the treatment of depression but due to poor solubility it suffers with the drawback of low oral bioavailability. The objective of present work was to formulate and characterize duloxetine loaded microemulsion to enhance the oral bioavailability. Prepared microemulsion was studied for droplet size, zeta potential, refractive index, polydispersity index (PDI), percentage transmittance, viscosity and in vitro release study. Optimized microemulsion (D1) showed spherical droplets with mean diameter of 35.40 ± 3.11 nm, PDI of 0.170 and zeta potential values of -25.8 mV. Formulation showed good transmittance (greater than 99%), viscosity (0.205 Pa s) and refractive index (1.43 ± 0.01). Increased duloxetine release was obtained with microemulsion in comparison to drug suspension. Behavioral tests like mobility test, tail suspension test and forced swimming test performed in depressed and treated rats with duloxetine microemulsion significantly improved the behavioral activities in comparison to duloxetine suspension. Pharmacokinetic studies showed that microemulsion exhibited 1.8 times increment in bioavailability in comparison to duloxetine suspension.<br /> (Copyright © 2018 Elsevier Ltd. All rights reserved.)
- Subjects :
- Animals
Biological Availability
Brain drug effects
Disease Models, Animal
Duloxetine Hydrochloride administration & dosage
Duodenum
Emulsions
Norepinephrine metabolism
Rats
Serotonin metabolism
Serotonin and Noradrenaline Reuptake Inhibitors administration & dosage
Up-Regulation
Behavior, Animal drug effects
Depression drug therapy
Duloxetine Hydrochloride chemistry
Duloxetine Hydrochloride pharmacokinetics
Pharmaceutical Preparations
Serotonin and Noradrenaline Reuptake Inhibitors chemistry
Serotonin and Noradrenaline Reuptake Inhibitors pharmacokinetics
Subjects
Details
- Language :
- English
- ISSN :
- 1879-1379
- Volume :
- 99
- Database :
- MEDLINE
- Journal :
- Journal of psychiatric research
- Publication Type :
- Academic Journal
- Accession number :
- 29427845
- Full Text :
- https://doi.org/10.1016/j.jpsychires.2018.01.015