Activity Of Piroxicam Research Articles

Preparation of Piroxicam nanosuspensions by high pressure homogenization and evaluation of improved bioavailability

Objective Inflammation is a natural response of the organism, involving events responsible for releasing chemical mediators and requiring treatments of symptoms such as pain, redness, heat, swelling, and loss of tissue function. Piroxicam (PRX) is a non-steroidal anti-inflammatory drug with the effect of nonselective COX inhibitor activity; however, it shows poor bioavailability caused by the poor and slow water solubility. In this study, we developed PRX nanosuspensions with 200–500 nm in diameter to increase the bioavailability of PRX by improving its solubility. Methods PRX nanosuspensions were fabricated by High pressure homogenization method with PVA, SDS and Tween 80. The nanosuspensions were characterized by XRD, FTIR, DSC, and in vitro release. In vivo pharmacokinetic properties and anti-inflammatory effects were also investigated in rabbits. Results PRX nanosuspensions significantly increased the solubility (14.89 ± 0.03 mg/L for pure PRX and 16.75 ± 0.05 mg/L for PRX nanosuspensions) and dissolution rate as compared to the pure PRX (p < 0.05). Orally administered PRX nanosuspension (AUC 0-t is 49.26 ± 4.29 μg/mL × h) significantly improved the bioavailability of PRX (AUC 0-t is 28.40 ± 12.11 μg/mL × h). The anti-inflammatory effect of PRX nanosuspension was also investigated in rabbits and it was observed that PRX nanosuspension treatment significantly improved the inhibition of COX-2 and NFκB expression as compared to the PRX treatment (p < 0.05). Conclusions The results in this study indicate that PRX nanosuspension is a promising nanomedicine for enhancing the anti-inflammatory activity of PRX and has a high potential for the treatment of inflammation.

Transbuccal permeation, anti-inflammatory activity and clinical efficacy of piroxicam formulated in different gels

In attempts to avoid the systemic side effects of piroxicam (PC) (e.g. gastrotoxicity), several buccal gel formulations containing PC were prepared and their effects on the characteristics of the drug permeation through rabbit buccal mucosa in-vitro were evaluated using a Franz-type diffusion cell. The general rank order of the total flux of 0.5% PC from gels was found to be: hydroxypropylmethylcellulose (HPMC, 2.5%) > hydroxypropylcellulose (HPC, 2.5%) ≥ sodium alginate (Na alg., 7%) > methylcellulose (MC, 3%) > hydroxyethylcellulose (HEC, 1.5%) > carbopol 934 (Carb. 934, 1%) ≥ sodium carboxymethylcellulose (NaCMC, 2%) > pluronic F-127 (PF-127, 20%) > polyvinyl alcohol (PVA, 10%). The effect of various penetration enhancers 1% sodium lauryl sulphate (NaLS), 3% sodium deoxycholate (NaDC), 3% sodium tauroglycocholate (NaTGC) on the rate of permeation across the excised buccal mucosa (of 0.5% PC in gels prepared using 3% MC, 2.5% HPMC or 7% Na alg. base) and histology of the buccal epithelium was also investigated. Pharmacodynamic evaluation of the anti-inflammatory activity of PC in these gel formulations (containing 3% NaDC as an enhancer) was carried out using the kaolin-induced rat paw oedema method. The results obtained indicated that PC administered in 7% Na alg. or 2.5% HPMC gel bases was significantly more effective than the 3% MC gel and oral drug solution in suppressing oedema formation in rats. Comparative clinical studies were conducted in patients with post-operative dental pain and oedema following maxillofacial operations. The results revealed that 7% Na alg. and 2.5% HPMC gel formulations applied to the buccal mucosa were slightly better than or equally effective to the orally administered commercial product (Feldene Flash ® tablet) in reducing pain level, swelling and tenderness within a period of 4 days. These findings suggest that PC (0.5%) administered in the buccal gel may present a potential therapeutical use as a strong anti-inflammatory and analgesic agent.

Influence of vehicles on the in vitro percutaneous absorption of piroxicam to optimise the formulation of patch tests in dermatology

AbstractThe present study evaluated the influence of various vehicles on the in vitro percutaneous absorption of piroxicam across human skin under standard diffusion conditions to optimise the formulation of patch tests in dermatology. The transdermal permeation properties of piroxicam were evaluated from five vehicles (PEG 400, propylene glycol, transcutol P, petrolatum, and petrolatum + transcutol P 10%) using Franz diffusion cells. Piroxicam was applied as a saturated solution in vehicles to ensure equal thermodynamic activity of piroxicam in the vehicles. Concentrations of piroxicam were determined by high performance liquid chromatography in epidermis, dermis, and receptor liquid. The release of piroxicam from its vehicles and consequently its cutaneous absorption are influenced by the vehicle assayed and the solubility of piroxicam in each vehicle. The penetration of piroxicam through human skin was clearly enhanced by propylene glycol and petrolatum + transcutol P 10%, with cumulated amounts of piroxicam in the receptor fluid at 48 h of 116±32 and 159±28 μg/mg/cm2 respectively, whereas petrolatum alone did not allow the diffusion of piroxicam. Additional experiments should be conducted in vivo to correlate the results obtained in vitro and to provide clinicians with a more reliable diagnostic test. Drug Dev. Res. 58:283–290, 2003. © 2003 Wiley‐Liss, Inc.

Effect of Maytenus aquifolium extract on the pharmacokinetic and antiinflammatory effectiveness of piroxicam in rats.

This study explored the interference by Maytenus aquifolium leaves hydroalcoholic (MALHE) extract, administered orally, on the pharmacokinetic and antiinflammatory activity of piroxicam in rats. The results showed no significant difference in piroxicam bioavailability with simultaneous application of MALHE. MALHE also had no effect on the inhibitory effect of piroxicam on inflammatory processes induced by carrageenan and complete Freund adjuvant.

Piroxicam-copper complexes: inhibition of polymorphonuclear leukocyte migration to Pseudomonas aeruginosa chemotactins in vivo and superoxide dismutase-like activity in vitro.

Piroxicam-copper (Cu2+) complexes, formed spontaneously by mixing solutions of piroxicam and CuSO4 (1:1 Cu2+:piroxicam), inhibited the superoxide anion-catalyzed reduction of ferricytochrome C in a dose-related fashion. Addition of ethylenediaminetetraacetate to the mixture decreased in a dose-related manner the superoxide dismutase (SOD)-like activity of piroxicam-Cu2+. Piroxicam alone (10(-5) M, final concentration) did not display SOD-like activity but 10(-5) M Cu2+ exhibited significant activity, similar to that of piroxicam-Cu2+. Intraperitoneal treatment of mice with either 0.64 mg/kg piroxicam or its Cu2+ complexes (0.64 mg/kg piroxicam + 0.12 mg/kg Cu2+) was equally effective in diminishing both the migration of polymorphonuclear leukocytes (PMNL) to the airways and the content of myeloperoxidase activity in the lungs, induced by aerosol challenge with Pseudomonas aeruginosa peptide chemotactins. Therefore, piroxicam-Cu2+ complexes may provide both the anti-inflammatory activity of piroxicam plus the SOD-like activity of Cu2+.