Development and Characterization of Water-in-Oil Microemulsion for Transdermal Delivery of Eperisone Hydrochloride

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Author(s): Monika Kumbhar D., Manisha Karpe S.*, Vilasrao Kadam J..

Journal Name: Applied Clinical Research, Clinical Trials and Regulatory Affairs

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Background: Eperisone hydrochloride possesses short biological half-life due to first pass metabolism resulting 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 development of Eperisone hydrochloride-loaded microemulsion and Eperisone hydrochloride-loaded microemulsion based cream for topical delivery and compared it with conventional cream.

Method: Firstly, water-in-oil microemulsion was prepared by spontaneous emulsification method. The concentration of components were 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 were studied by differential scanning calorimetry, X-ray diffraction, in- vitro release and ex-vivo drug permeation studies respectively. By using microemulsion, cream was prepared for proving optimum structure for topical application. Microemulsion was evaluated for droplet size, zeta potential, pH, viscosity, conductivity. Besides cream was characterized for pH, rheology, stability. Permeation of EPE from microemulsion across the rat skin was evaluated and compared with conventional cream.

Result: 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 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, effectively used for muscle spasticity by topical route.

Keywords: Eperisone hydrochloride, Transdermal delivery, Water-in-oil microemulsion, Sustained release, Permeation

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(E-pub Ahead of Print)
DOI: 10.2174/2213476X06666190318120522

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