Controlled Release Levetiracetam Loaded Eudragits Microspheres for Oral Drug Delivery: Preparation and Evaluation

Abstract

This work aims to prepare controlled release microspheres loaded with levetiracetam (LEV) for oral use that will have a targeted release site, thus reducing dose frequency and improving patient compliance. Levetiracetam is a 2nd generation antiepileptic medication with a T/half-life of 7 hours that is administered twice daily, which makes it suitable for formulation that will reduce dosing intake. The microspheres were prepared by solvent evaporation method using Eudragit E100, L100, and S100 polymers as matrix core polymers at diff erent ratios 1:1, 1:2 and 1:3 with levetiracetam. These polymers have diff erent pH sensitivity profi les, which will aid the release of levetiracetam in a controlled manner along the gastrointestinal tract. The prepared microspheres were evaluated for yield percentage, entrapment effi ciency (EE%), morphological characteristics and in-vitro release profi le. The yield percentage and EE% for the formulation at diff erent ratios ranged from 69–99%. The in-vitro release analysis showed favorable targeted release of the drug at specifi c pH ranges matching specifi c sites in the gastrointestinal tract.