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Published on:January 2018
Indian Journal of Pharmaceutical Education and Research, 2018; 52(2):230-240
Original Article | doi:10.5530/ijper.52.2.26

Formulation and in-vitro drug Released Mechanism of CNS Acting Venlafaxine Nanostructured Lipid Carrier for Major Depressive Disorder


Authors and affiliation (s):

Pankaj M Pimpalshende, Roop N Gupta

Department of Pharmaceutical Sciences and Technology, Birla Institute of Technology, Mesra, Ranchi (JH), INDIA.

Abstract:

Venlafaxine (VLX) is a first line, dual acting and unique antidepressant drug which belong to the class of serotonin and norepinephrine reuptake inhibitors. Oral administration of VLX has many adverse effects, poor bioavailability due first-pass hepatic metabolism and low permeability shows poor antidepressant action in the brain. The aim of this present study was to formulate Venlafaxine Nanostructured lipid carrier (VLX-NLC) and deliver directly into the brain through intranasal route. VLZ-NLC were prepared by Melt- Emulsification-Ultrasonication process and characterized by particle size, polydispersity index, zeta potential, Encapsulation efficiency and analyzed by differential scanning calorimetry (DSC), X-ray diffraction (XRD), transmission electron microscope (TEM). The VLX-NLC was also evaluated for in-vitro drug release and ex-vivo sheep nasal mucosa permeation. The mean particle size of VLX-NLC was between 155 and 293 nm in diameter with entrapment efficacy was up to 74.13%. TEM gave confirm of spherical nature of NLC. The DSC result shows a sharp peak at 208ºC corresponds to melting peak hence confirm the peak of Venlafaxine and X-ray diffraction 2θ scattered angle represent crystallinity nature of pure Venlafaxine whereas VLX-NLC reveals decrease intensity of peak which indicates amorphization of VLX due to solubilization in lipid. In vitro studies exhibit initial burst release and afterward prolong release, ex vivo permeation through nasal sheep mucosa showed 66.45 % of drug diffused in 24 h from VLX-NLC.

Key words: Venlafexine, Nanostructured lipid carrier, Antidepressant.

 

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The Official Journal of Association of Pharmaceutical Teachers of India (APTI)
(Registered under Registration of Societies Act XXI of 1860 No. 122 of 1966-1967, Lucknow)

Indian Journal of Pharmaceutical Education and Research (IJPER) [ISSN-0019-5464] is the official journal of Association of Pharmaceutical Teachers of India (APTI) and is being published since 1967.

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IJPER uses reference linking service using Digital Object Identifiers (DOI) by Crossref. Articles from the year 2013 are being assigned DOIs for its permanent URLs