Title:Optimization of Microemulgel for Tizanidine Hydrochloride
Volume: 19
Issue: 2
Author(s): Swati Jagdale*, Sujata Brahmane and Anuruddha Chabukswar
Affiliation:
- Department of Pharmaceutics, School of Pharmacy, Dr. Vishwanath Karad MIT World Peace University, Survey No. 124, MIT College Campus, Paud Rd, Kothrud, Pune, Maharashtra 411038,India
Keywords:
Delivery, emulsion, factorial, gel, microemulgel, microemulsion, tizanidine.
Abstract:
Background: Tizanidine hydrochloride acts centrally as a muscle relaxant. It is
used for the treatment of painful muscle spasm, spasticity associated with multiple sclerosis
or spinal cord injury and treatment of muscle spasticity in spinal cord disease. Tizanidine
hydrochloride belongs to BCS class II. It has low oral bioavailability and short halflife.
Incorporating this drug in microemulgel is an excellent way to overcome problems associated
with the drug.
Objectives: Present research work was aimed to develop and optimize a microemulsion
based gel system for tizanidine hydrochloride.
Methods: Screening of oil, surfactant and co-surfactant was carried out. Ternary phase diagram
was constructed to obtain concentration range of components. The prepared microemulsion
was evaluated for pH, globule size, zeta potential, conductivity, density and viscosity.
32 level factorial design was applied to study the effect of concentration of carbopol
934 and HPMC K15M on % cumulative drug release and viscosity of microemulgel using
software Design Expert. Microemulgel was evaluated for pH, spreadability, viscosity, syneresis,
drug content, bioadhesive strength, in-vitro as well as ex-vivo diffusion study.
Results: Microemulsion was prepared by using isopropyl myristate as oil, tween 80 as a
surfactant and transcutol P as cosurfactant. Largest transparent microemulsion region was
found with Smix ratio of 1:1. FE-SEM showed globule size 28μm for batch B1 and zeta
potential was -1.27mV indicating good stability of the microemulsion. Optimised batch
was F6 which showed 92% drug release within 8 hours. It followed the Korsmeyer-Peppas
model.
Conclusion: A stable, effective and elegant microemulgel formulation, exhibiting good
in-vitro and ex-vivo drug release was formulated.
