Formulation and Optimization of Zaltoprofen Loaded Ethosomal Gel by using 23 Full Factorial Designs

Aim:The objective of the present study is to design and characterize the ethosomal gel containing Zaltoprofen for sustained drug delivery and also to reduce the side effects. Zaltoprofen was chosen here as the drug candidate because of its short half-life and increased dosing frequency.

Methods: The ethosomes containing Zaltoprofen was prepared by using cold method. A 23 full factorial design containing 10 experimental trails was used in order to obtain an optimized formulation. The prepared ethosomes were characterized by Scanning Electron Microscopy, PDI, zeta potential, vesicle size, and percentage entrapment efficiency. Optimized ethosomal formulation was incorporated in 1% carbopol gel to deliver the drug through topical route. Invitro drug permeation studies of ethosomal gel (EGL) and conventional gel (CGL) was conducted and flux and permeability coefficient were calculated.

Results:The vesicle size, zeta potential, and % entrapment efficiency of optimized formulation were found to be 124.33 nm, -45.2 mV and 70.03%, respectively. The surface of the vesicles was found to be spherical and smooth. The in vitro drug release studies of the ethosomal gel formulation showed sustained drug delivery when compared with the conventional gel containing the pure drug. In vitro permeability studies show that the flux of ethosomal gel was 2.5 fold higher than conventional gel, which may be the attribution of ethanol and flexible nature of ethosomes.

Conclusion: It was concluded that the ethosomal gel could be a better choice for the topical delivery of Zaltoprofenwith improved bioavailability for its anti-inflammatory activity.