Abstract:
Aceclofenac, a nonsteroidal anti-inflammatory drug has been formulated into transdermal Eudragit patches. The drug was first characterized
for its physicochemical properties by studying its solubility and its partition coefficient at different pH values. Formulation of Aceclofenac
into transdermal patches using three acrylic resin polymers like Eudragit L100, L100-55 and S100 was done. The effect of different plasticizers,
like propylene glycol (PG) and polyethylene glycol (PEG 400) in concentrations of 5% and 10%, on the in-vitro drug release was investigated.
Thermodynamics of the in-vitro release of Aceclofenac from Eudragit patches were also studied. The anti-inflammatory effect of the selected
Aceclofenac Eudragit patches was determined in male albino rats, using paw edema method. The results of the in-vitro release show that,
Eudragit patches of Aceclofenac had an acceptable % drug release after 60 minutes and the increase of hydrophilic plasticizers PG or PEG
concentrations form 5% to 10% is accompanied by an increase in drug release. The release of drug from all investigated Eudragit patches
follows zero order kinetic and it increases linearly as a function of temperature. The free energy (rG) values of drug release are negative for
all Eudragit patches and the best thermodynamically stable patch was L100+10% PG, which was chosen for further pharmacodynamic
evaluation of Aceclofenac anti-inflammatory activity. The results show that in all treated rat groups there are significant inhibition in edema
thickness, produced by carrageenan when compared with the non-treated group. This inhibition in edema is statistically significant at P <
0.05. It was also observed, that the group pretreated with water for 30 hours prior to the experiment showed the highest percent edema
inhibition, followed by group pretreated with isopropyl myristate (IPM). This study demonstrates the feasibility of formulating Aceclofenac
into transdermal patches using Eudragit L100+10% PG to deliver it as part of inflammatory management.
