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

  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.