DEVELOPMENT OF ECONOMIC TRANSDERMAL PATCHES CONTAINING LORNOXICAM FOR TREATMENT OF ACUTE AND CHRONIC INFLAMMATORY MODELS IN ALBINO RATS (A PRECLINICAL STUDY)Abstract
Objective: To formulate economic transdermal patch of lornoxicam (LX) and to study its anti-inflammatory activity on acute and chronic inflammatory in rat models. Method: Three LX transdermal patches (F1, F2, and F3) consist of Eudragit RL-100, and RS-100 in three different ratios (1:2, 1:1 and 2:1) were prepared respectively by the solvent evaporation technique. All formulations contain diethyl phthalate as a plasticizer. The physicochemical compatibility of the drug and the polymers was studied by differential scanning calorimetry. The prepared LX transdermal patches were evaluated for their drug content, patch thickness, folding endurance, surface pH, and in vitro drug permeation. The anti-inflammatory activity of LX transdermal patch was determined using two experimental animal designs, one for acute inflammation (rat paw edema) and the other for chronic inflammation (granuloma pouch) on eighty adult albino rats. The results obtained were statistically analyzed. Results: The data showed physicochemical compatibility between the drug and the polymers used. The LX patches (F1, F2, and F3) prepared were uniform thickness, drug content, and the pH of the LX patch was found to be 6.5. Increasing the ratio of the Eudragit® RL-100 polymer to eudragit RS 100 (F3) showed a corresponding increase in the folding endurance of patches. Diethyl phthalate led to increasing elasticity for the patches. F3 showed higher drug permeation than F2 and F1. Edema (anti-inflammatory effect) was significantly decreased in group V followed by group IV then by group III in case of the two animal experimental designs. Group V received LX transdermal patch (F3). Conclusion: The present study showed that the prepared economic lornoxicam transdermal patch has good properties with high efficiency as an anti-inflammatory drug on acute and chronic inflammatory models.
N. A. El-Nabarawy *, R. A. A. Elmonem and H. A. A. Enin
National Egyptian Center of Environmental and Toxicological Research (NECTER), Cairo University, Cairo, Egypt.
23 March 2014
13 June 2014
02 August 2014
01 October 2014