Affiliation:
1. Pharmaceutics Department, University of Mumbai, Navi Mumbai, India
Abstract
Background:
Eperisone hydrochloride possesses short biological half-life due to first
pass metabolism resulting in low bioavailability and short duration of response with toxic effects,
ultimately limits its utilization for treatment of muscle spasm.
Objective:
In view of this background, current study was designed for the development of Eperisone
hydrochloride-loaded microemulsion and Eperisone hydrochloride-loaded microemulsion
based cream for topical delivery and compared it with conventional cream.
Methods:
Firstly, water-in-oil microemulsion was prepared by spontaneous emulsification method.
The concentration of components was found out from existence of microemulsion region by
constructing pseudoternary phase diagram. The oil was selected on the basis of drug solubility effect
on the drug release, whereas surfactant and cosurfactant were screened on the basis of their
efficiency to form microemulsion region. The influence of components on microemulsion formation,
drug release capacity, permeation was studied by differential scanning calorimetry, X-ray
diffraction, in-vitro release and ex-vivo drug permeation studies respectively. By using microemulsion,
the cream was prepared for proving optimum structure for topical application.
Microemulsion was evaluated for droplet size, zeta potential, pH, viscosity and conductivity. Besides
the cream was characterized for pH, rheology and stability. Permeation of EPE from microemulsion
across the rat skin was evaluated and compared with conventional cream.
Results:
The microemulsion consisting Isopropyl Myristrate/Water/Span 80:Tween 80 (50/8/42%
by weight) possessed droplet size of 95.77nm, zeta potential of −5.23 mV with 7.25 pH and conductivity
near to zero (<0.05mScm-1). Physical parameters of the cream were satisfactory, also
2.33-fold higher permeation and 1.57-fold higher release observed as compared to conventional
cream.
Conclusion:
It can be concluded that Eperisone hydrochloride-loaded microemulsion and its
cream is being effectively used for muscle spasticity by topical route.
Publisher
Bentham Science Publishers Ltd.
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