The aim of the present investigation was to biotransform the anti-inflammatory compound meloxicam by enzymes present in whole cells of five actinomycete cultures to produce novel bioactive derivatives. Among the actinomycetes screened, Streptomyces griseus NCIM 2622 was found to possess the enzyme system (s) that oxidize meloxicam into two metabolites whereas that present in S. griseus NCIM 2623 could oxidize meloxicam to only one metabolite in significant quantities. The formation of enzymatic metabolites was monitored and confirmed by high-performance liquid chromatography (HPLC) analysis. The structures were elucidated based on liquid chromatography-tandem mass spectrometry (LC-MS/MS) data and previous reports as 5-hydroxymethyl meloxicam and 5-carboxy meloxicam. From the results obtained in this study, it can be concluded that S. griseus NCIM 2622 possesses oxidizing enzymes, which can be employed to oxidize meloxicam.

Meloxicam is a poorly water soluble non steroidal anti-inflammatory drug and antipyretic agent. The aim of the present work was to investigate the effect of different types of carriers on in vitro dissolution of meloxicam. Meloxicam solid dispersions were prepared by physical mixing, co-grinding and solvent evaporation methods with polyethylene glycol (PEG) 6000.The effect of solubilization by sodium lauryl sulphate (SLS) was also studied. The dissolution was determined by USP XXVII Apparatus I, using phosphate buffer with a pH of 7.4 as the dissolution medium. The maximum in vitro dissolution of meloxicam, i.e. 97.45% in 60 min, was observed for solid dispersions containing meloxicam (150 mg), PEG 6000 (350 mg) and SLS (75 mg) prepared by solvent evaporation method containing a sum of 3 g of Lactose and MCC (4:1) as additives. The general trend indicated that there was an increase in dissolution rate for solid dispersions containing the solubilizer SLS. The best-fit model indicating the mechanism of dissolution from the formulation showing the highest release for was found to be Higuchi matrix release (r=0.9774, b=13.042, a=2.4798). Infra red spectroscopy (IR) indicated that meloxicam in solid dispersions showed physical entrapment. The increased in dissolution rate of meloxicam by solid dispersion technique may be due to increase wettability and hydrophilic nature of carrier.

In this study, buccal mucoadhesive tablets of meloxicam were formulated for drug delivery as an alternative route. Direct compression method was applied for the preparation of tablets. Also, different polymers, including hydroxypropyl methyl cellulose (HPMC) 1000, 4000, and 10000, as well as carbopol 934p and carbopol 971p were used as the mucoadhesive polymer and retardant polymer. Thirteen formulations were investigated with various concentrations of polymers. The physicochemical characteristics, in-vitro drug release, swelling index, and taste modification of tablets were evaluated. Also, Carr’ s index and Hausner ratio were studied. In addition, zero-order, first-order, and Higuchi kinetics were investigated and the results showed that the highest correlation coefficient (R 2 ) is related to zero-order kinetic for formulations B2 and B3. Furthermore, the highest R 2 is related to Higuchi kinetic for formulation C3. Formulation B2 showed the maximum release of 99% in 12 h. The results demonstrated that Formulation B2 can be considered as a proper buccal mucoadhesive tablet of meloxicam with desired property.

Background: Non-steroidal anti-inflammatory drugs (NSAID) have been associated with antioxidant property and have been shown to improve the circulating antioxidant status on daily dosing in different inflammatory conditions. The present study was conducted to investigate the antioxidant role of meloxicam in aluminum induced oxidative stress in rat brain.Methods: In the in vivo experiments, Sprague-Dawley rats where randomized into 4 groups receiving daily treatment for 4 weeks: 1) double distilled water i.p., 2) 4.2 mg/k aluminum i.p. 3) meloxicam (5.0 mg/kg, i.m.) 4) 5.0 mg/kg, meloxicam i.m. + 4.2 mg/kg aluminum i.p. brain homogenates from the above animals were assayed for lipid peroxidation levels as well as superoxide dismutase activity. In the in vitro experiments, brain homogenates from Sprague-Dawley rats were treated with either, aluminum, meloxicam or their combinations and were then assayed as per the in vivo samples. Results: In vivo data showed elevated lipid peroxidation levels in brain homogenate in aluminium-treated group as compared to aluminium + meloxicam treatment which showed a significant decrease in the malonaldehyde levels. Similar results were observed in the in vitro experiments when brain homogenates were treated with either, aluminum, meloxicam or their combinations. Furthermore, no change was observed in superoxide dismutase activity in any treatment group as compared to the control in either experiment. Conclusion: These results indicate that NSAID can be used in Alzheimer management.  

Meloxicam is a non steroidal anti-inflammatory drug, used in the treatment of rheumatoid arthritis and oestoarthritis. It is practically insoluble in water leading to poor dissolution, variations in bioavailability and gastric irritation on oral administration. In order to modulate its gastric side effect and to increase aqueous solubility, physical mixture and solid dispersion of the drug were prepared with polyethylene glycol 6000 and polyvinyl pyrrolidine. The analgesic, anti-inflammatory and ulcerogenic effects were assessed for physical mixture and solid dispersion in comparison with meloxicam alone. The results indicate that both physical mixture and solid dispersion possess better analgesic and anti-inflammatory properties with less ulcerogenic potential as compared to pure meloxicam.

Cerebral vasospasm considered to be a serious cause of morbidity and mortality following subarachnoid haemorrhage (SAH). Despite several available therapeutic options, current protocols do not prevent major consequences of vasospasm. Inflammation is believed to play an important role in post-haemorrhagic vasospasm. Meloxicam is a non-steroidal antiinflammatory drug. The aim of this study was to compare the efficacy of meloxicam versus placebo on vasospasm in patients with SAH. In this randomized, double-blind, placebocontrolled trial, SAH patients randomly received 7. 5 mg meloxicam or placebo twice daily for 7 days. End points were, middle cerebral artery velocity obtained with transcranial doppler, in-hospital mortality, hospital stay and discharge Glasgow Outcome Scale. Eighty-one patients enrolled in the study. (40 received meloxicam, 41 received placebo). Baseline characteristics were similar between the groups. There were no differences in length of hospitalization (17. 4 ± 3. 1 vs 18. 6 ± 4. 2 days; p = 0. 145), in-hospital mortality rate (15 vs 22%; p-value=0. 569), or GOS (p = 0. 972) between the two groups. MCA velocity were slightly less in patients who had received meloxicam, but not to a significant degree (p-value=0. 564(. No side effect has been detected for meloxicam. This study did not prove meloxicam efficacy in vasospasm of SAH patients. But it demonstrated that clinical trial of meloxicam in these patients is feasible and probably safe. The effectiveness of meloxicam on cerebral vasospasm has to be studied in larger trials.

Objective(s): Drug delivery through the skin can transfer therapeutic levels of drugs for pharmacological effects. Analgesics such as NSAIDs have gastrointestinal side effects and topical dosage forms of these drugs are mainly preferred, especially for local pains. Meloxicam is one of NSAIDs with no topical form in the market. In this research, we attempted to quantify the skin permeation of a meloxicam topical preparation and to show how permeation would be increased by using thymol as an enhancer. The effect of eutectic point of drug and thymol mixture on rate and extent of skin permeation was also studied.Materials and Methods: Different mixtures of thymol and meloxicam (2:8, 4:6, 5:5, 6:4, 8:2) were prepared and their melting point were obtained by differential scanning calorimetry. Then drug permeation was measured using diffusion cells and the Guinea pig skin.Results: Mixtures in ratios 5:5 and 4:6 of meloxicam / thymol showed a new endotherm at 149 and 140oC in DSC thermograms. The permeability of meloxicam from the creams containing 6:4, 5:5 and 4:6 ratios of meloxicam to thymol were 4.71, 15.2, 22.06 mg/cm2 respectively. This was significantly different from the cream of pure meloxicam (3.76 μg/cm2).Conclusion: This study set out to determine that thymol plays as a skin permeation enhancer and increases the meloxicam skin absorption and this enhancement is significant at the eutectic point of drug-enhancer mixture.