Background: Transdermal drug delivery is an attractive approach for both local and systemic
therapeutics of various diseases. Transdermal drug delivery systems show various advantages
like reduction of local irritation, prevention of first-pass hepatic metabolism, and bioavailability enhancement
of bioactive molecules over conventional drug delivery systems.
Objective: The main objective of the present research work was to develop and characterize (in-vitro
and ex-vivo) econazole nitrate loaded transethosomes and their comparison with marketed cream of
econazole nitrate [Ecoderm, Brown and Burk Pharmaceutical (Pvt.) Ltd., Bengaluru, India] for effective
Method: Transethosomes loaded with econazole nitrate were developed by homogenization method
and evaluated for entrapment (%), vesicular size, zeta potential, polydispersity index (PDI), and invitro
drug release. Furthermore, optimized econazole nitrate loaded transethosomes were added to
Carbopol 934 gel and this gel was evaluated for viscosity, pH, drug content, ex-vivo skin permeation
and retention studies followed by in-vitro antifungal activity against C. albicans fungus.
Results: The optimized transethosomes loaded with econazole nitrate showed vesicle size of 159.3 ±
4.3 nm, entrapment efficiency about 78.3 ± 2.8%, acceptable colloidal properties like (zeta potential =
-27.13 ± 0.33 mV, PDI = 0.244 ± 0.045), approximately 57.56 ± 2.33% drug release up to 24 h. Results
of DSC analysis confirmed the encapsulation of econazole nitrate inside transethosomes. Optimized
transethosomes showed drug release following zero order through diffusion mechanism.
Transethosomal gel showed high drug content (92.35 ± 0.63%) and acceptable values of pH (5.68 ±
0.86) or viscosity (10390 ± 111 cPs). Transethosomal gel showed less ex-vivo skin penetration (17.53
± 1.20%), high ex-vivo skin retention (38.75 ± 2.88%), and high in-vitro antifungal activity compared
to the marketed cream of econazole nitrate.
Conclusion: Therefore, it can be concluded that econazole nitrate loaded transethosomes are effective
to deliver econazole nitrate transdermally in a controlled fashion for effective elimination of cutaneous