Aim: Negatively charged deformable liposomes (DL) of ketoprofen were formulated to enhance transdermal delivery of ketoprofen (KP) under the influence of iontophoresis for intraarticular delivery. Methods: Conventional and deformable KP liposomes were prepared using thin film hydration, characterized and intraarticular delivery of KP was evaluated using Sprague-Dawley rats. Results: Vesicles displayed entrapment efficiency (>71%); zeta potential <-25 mV; size between 152.4 ± 12.42 nm to 220.4 ± 6.22 nm, KP-DL were stable under iontophoresis. Conventional and deformable liposomes exhibited relatively higher iontophoretic flux values than passive flux; Iontophoretic delivery enhanced KP availability in the synovial fluid (1.34 ± 0.12 μg.h/ml) fourfold over passive delivery (0.329 ± 0.15 μg.h/ml). Conclusion: Iontophoretic mediated transport of deformable liposomes could improve transdermal delivery of ketoprofen into the synovial joints than conventional liposomes.
Keywords: NSAID; deformable liposomes; intraarticular; iontophoresis; microdialysis.
The present work is testing the effect of current on the movement of a drug. The name of the drug is ketoprofen (KP). To prepare small-size particles of KP, a new preparation called as deformable liposomes is used. These liposomes were prepared using solvents to dissolve drugs and fats. Later the solvents were removed to form a thin film. Further to the thin film, a water-based solvent was added to form minute particle dispersed in water. The suspension was tested to find out the size, charge and amount of drug gone into it. More than 70% of KP was included and surface charge was negative and size was very less. Amount of KP entering inside the bone joints on the knee showed that four-times higher amount moved inside with the help of current than without the help of current (passive). So, with the help of current, higher amount of drug could be transported to decrease pain.