Journal: Journal of Pharmacy Research

Article Id: JPRS-PCS-00001962
Title: Preparation of intranasal pregabalin microspheres: In vitro, ex vivo and in vivo pharmacodynamic evaluation
Category: Pharmaceutics
Section: Research Article
  • Abstract
  • Audio Abstract
  • Authors
  • Pdf File
  • Citation
  • My Reference
  • Methodology
  • Abstract

    Background and Objective: Although, pregabalin shows high oral absorption, greater intrinsic efficacy to prevent seizure activity, its delayed transport across the blood-brain barrier limits the use in emergency epileptic seizures. Due to the particular anatomical features of the nasal cavity, intranasal (IN) administration has been explored as a means of preferential drug delivery to the brain. The objective of the present study was to improve therapeutic efficacy through IN administration of pregabalin- loaded mucoadhesive microspheres. Materials and Methods: Chitosan-based mucoadhesive microspheres were prepared by ionotropic gelation method using glutaraldehyde as a crosslinking agent. Effect of chitosan concentration, glutaraldehyde concentration, and the stirring speed was investigated for the formation of microspheres. The physicochemical properties of microspheres, including particle size, zeta potential, drug content, entrapment efficiency, swelling index, and morphology were examined using suitable tools. Ex vivo bioadhesion, biocompatibility, and drug permeation were determined using sheep nasal mucosa. Anticonvulsant effect of pregabalin-loaded microspheres was investigated in pentylenetetrazole (PTZ) induced seizures in mice through IN administration. Results: Pregabalin-loaded chitosan microspheres were spherical shape 18.2–24.35 µm mean diameter, positive zeta potential, 80% entrapment efficiency, and 87.29% ex vivo drug permeation. The results of in vivo studies clearly indicated the greater anticonvulsant effect pregabalin in PTZ-induced seizures by IN route as compared to its peripheral administration. Conclusion: Thus, IN administration of pregabalin via mucoadhesive microspheres may be appropriate and valuable drug delivery system for the chronic and acute attacks of epileptic seizures.

  • Abstract Audio

    No Audio file found

  • About the authors and Affiliations

    Author(s) Name:

    Jayshree B. Taksande*, Milid J. Umekar

    Affiliation(s) Name:

    Department of Pharmaceutics, Shrimati Kishoritai Bhoyar College of Pharmacy, Kamptee, Nagpur – 441 002, Maharashtra, India

    *Corresponding author: Dr. Jayshree B. Taksande,Shrimati Kishoritai Bhoyar College of Pharmacy, Kamptee, Nagpur – 441 002, Maharashtra, India.

  • View Article File in pdf format.

    Article File
  • View Article Citation Here.

    0 View More
  • How to Cite my Article.

    Author:

    Jayshree B. Taksande*, Milid J. Umekar

    Title:Preparation of intranasal pregabalin microspheres: In vitro, ex vivo and in vivo pharmacodynamic evaluation
    Journal:Journal of Pharmacy Research
    Vol(issue):12 (January)
    Year:2018
    Page No: (112-121)
  • Experimental Methods Keywords

    Methodology:In vitro, ex vivo and in vivo pharmacodynamic evaluation
    Research Materials:Intranasal pregabalin microspheres,Pregabalin

Keywords

Chitosan Epilepsy Intranasal Microspheres Pregabalin

Our Services

Most Downloaded List