Development and characterization of ketoprofen solid dispersion incorporated topical gels

摘要

The present work aims to increase the therapeutic effectiveness of ketoprofen by increasing its transdermal permeation, via solid dispersion incorporated in gel. 2-hydroxy propyl beta cyclodextrins (HPβ-CD) and β- cyclodextrin (β-CD) were used as carriers and carbopol 940 was the gelling agent. Eight solid dispersion formulations of ketoprofen were prepared using different drug: polymer ratios viz. 1:0.5, 1:1, 1:2, and 1:3 for 2- HPβ-CD and β cyclodextrin using the solvent evaporation method. The formulation of solid dispersion by solvent evaporation method is introduced to reduce the drug particle size and hence increase the dissolution rate. These dispersions were characterized with the help of FT-IR, DSC and X-ray diffraction studies. The optimized solid dispersion of ketoprofen was incorporated into gel and was compared with penetration enhancers. The formulations were analyzed to determine their pH, spreadability, viscosity, and in vitro drug release. The formulation with 1:0.5 SDK (drug: HPβCD) was incorporated in carbopol gel, and produced 98.32 % drug release compared to solid dispersion of ketoprofen with menthol (SDKM5%), which produced 96.26% drug release. In ex vivo studies, SDK and SDKM5% formulations gave 94.37% and 92.26% drug release respectively within 24 h. The percent inhibitions of the edema formation by the gels were in the range of 19.63% to 69.65%, and the maximum inhibition was shown by the SDK formulation. Therefore, SDK formulation incorporated in gel produced better results than other formulations prepared with permeation enhancers. Stability studies conducted for SDK incorporated gel.