Key points are not available for this paper at this time.
Etoricoxib (Et), a new potent COX-2 anti-inflammatory drug that suffers from severe side effects after oral administration. The present study is concerned with preparation and characterization of transdermal gel formulations containing Et cubosomes nanoparticles. Et cubosome dispersions were formulated using different concentrations of lipid phase Glycerol Monooleate (GMO), nonionic surfactant Poloxamer 407 (P407) and water as aqueous phase. The prepared Et cubosomal dispersions were characterized for % drug content, % entrapment efficiency (EE), particle size, and in vitro drug release. Formulation with highest EE (92.0 ± 1.6 %), small particle size (63.5 ± 1.8 nm) and acceptable drug release profile (S9) was further evaluated for zeta potential and investigated for its internal structure using the transmission electron microscope (TEM). Results confirmed formation of cubic to spherical shaped particles with acceptable zeta potential (-20 ± 0.379 mV). Selected formulation was incorporated in different gel formulations using CMC-Na (1, 1.5 % w/w) as gelling agent and glycerol (2.5, 5, 7.5 % w/w) as penetration enhancer. The cubosomal gels were characterized along with drug loaded gel for macroscopic, physical properties and in vitro drug release. Results confirmed acceptable macroscopic, physical properties with variable drug release profiles depending on gelling agent concentration as well as glycerol concentrations. Selected gel formulation with favorable drug release profile (G3) was further evaluated for ex vivo permeation. Results showed enhanced permeation for G3 compared to Et gel. The developed Et-loaded cubosomal gel offers a promising transdermal method for treating arthritis that will be applied directly to the skin.
Darwish et al. (Sat,) studied this question.