-
The Science of the Total Environment Dec 2023Santa Catarina is the main producer state of oysters and mussels in Brazil, reaching 98 % of national production. To assure the safety of bivalve mollusks production,...
Santa Catarina is the main producer state of oysters and mussels in Brazil, reaching 98 % of national production. To assure the safety of bivalve mollusks production, control programs of marine biotoxins (MBs) have been continuously performed. Herein, the co-occurrence of MBs and contaminants of emerging concern (CECs) in oyster and mussels from the main production sites of Santa Catarina was reported, covering 178 compounds. Samples of wild and non-cultivated oysters and mussels were also assessed. Chemometric tools were used to evaluate and optimize several sample preparation techniques such as solid-liquid, ultrasound assisted, and pressurized liquid extraction. The optimized protocol was based on ultrasound assisted extraction followed by liquid chromatography coupled to tandem mass spectrometry. The results showed the incidence of several CECs and MBs. In the case of MBs, all results were below the regulatory limits for both cultivated and non-cultivated samples. Wild mollusks have shown a higher number of compounds. Regarding CECs, the more frequent compounds were caffeine, diclofenac, meloxicam, and sertraline. Domoic acid and okadaic acid were the main toxins detected. The results highlighted the need of monitoring for MBs and the potential of oyster and mussels as sentinel organisms to risk analysis of CECs in coastal regions. To the best of our knowledge, this is the first method to describe a simultaneous sample preparation and analysis of CECs and MBs in bivalve mollusks, as well as the first report of meloxicam and florfenicol in mussels and oysters.
Topics: Animals; Marine Toxins; Brazil; Meloxicam; Bivalvia; Okadaic Acid; Ostreidae
PubMed: 37741417
DOI: 10.1016/j.scitotenv.2023.167254 -
Frontiers in Pain Research (Lausanne,... 2023Castration is a stressful and painful procedure that can impact swine welfare negatively. The objectives of this study were to (1) evaluate the effect of one incision...
Castration is a stressful and painful procedure that can impact swine welfare negatively. The objectives of this study were to (1) evaluate the effect of one incision compared to two incisions and the use of a topical vapocoolant (VAPO; ethyl chloride; a topical anesthetic) applied before castration and (2) evaluate the most effective combination in reducing pain in objective 1 and the use of Metacam®; meloxicam before castration on measures of performance, behavior, and physiology. Study 1 consisted of six treatment groups ( = 27 pigs per treatment) and included: nothing (NO); sham castrated (SH); one incision castration (C1); one incision castration plus VAPO (C1V); two incision castration (C2); two incision castration plus VAPO (C2V). Body weights and blood samples were taken at baseline and other time points after castration. Behavior measures were collected for 24 h after castration. Wound scores were collected daily for 10 days. The C1 pigs and C1V pigs were significantly heavier than the other castrated treatment groups but not different from NO and SH pigs. Vocalizations were louder for C1 and C1V pigs ( = 0.0015). Study 2 ( = 40 pigs per treatment) included: nothing (NO); one incision castration (C1); and one incision castration plus meloxicam administered 15 min before castration (C1M). The same measures (performance, behavior, and physiology) were collected as in Study 1. Performance measures and behavior did not differ among treatment groups. Physiological measures were only different for red blood cells (RBC; = 0.0304). Pigs in C1 and C1M treatment groups had cortisol concentrations that were greater than the NO treatment group at 15 min post-castration ( < 0.05). The data collected give insight into the benefits of one-incision castration compared to 2-incision castration. However, the data only support a lower-level relief from acute pain associated with castration, as it is evident that pigs still experience stress at 15 min post-castration with or without the use of meloxicam. Further research could potentially identify the correct timing, route and dose for the administration of meloxicam.
PubMed: 37575637
DOI: 10.3389/fpain.2023.1113039 -
Animal Bioscience Apr 2024This research was performed to investigate effect of administering chromium (Cr) and meloxicam (MEL) on growth performance, cortisol and blood metabolite, and behaviors...
OBJECTIVE
This research was performed to investigate effect of administering chromium (Cr) and meloxicam (MEL) on growth performance, cortisol and blood metabolite, and behaviors in young regrouped heifers.
METHODS
Fifty Holstein dairy heifers (body weight (BW) 198 ± 32.7 kg and 6.5 ± 0.82 months of age) were randomly assigned to non-regrouped group or four regrouped groups. Non-regrouped animals were held in the same pen throughout entire experimental period (NL: non-regrouping and administration of lactose monohydrate (LM; placebo). For regrouping groups, two or three heifers maintained in four different pens for 2 weeks were regrouped into a new pen and assigned to one of four groups: regrouping and LM administration (RL); regrouping and Cr administration (RC); regrouping and MEL administration (RM), and regrouping and Cr and MEL administration (RCM). LM (1 mg/kg BW), Cr (0.5 mg Cr picolinate/kg dry matter intake), and MEL (1 mg/kg BW) were orally administered immediately before regrouping. Blood was collected before regrouping (0 h) and at 3, 9, and 24 h and 7 and 14 d thereafter. Behaviors were recorded for 7 consecutive days after regrouping.
RESULTS
Average daily gain was lower (P < 0.05) in RL than NL heifers, but was higher (P < 0.05) in RM, RC, and RCM than RL heifers. RL heifers had higher (P < 0.05) cortisol than NL heifers on d 1 after regrouping. The cortisol concentrations in RC, RM, and RCM groups were lower (P < 0.05) than in RL treatment 1 d after regrouping. Displacement behavior was greater (P < 0.05) in RL group than all other groups at 2, 3, and 6 d after regrouping.
CONCLUSION
Regrouping caused temporal stress, reduced growth performance, and increased displacement behavior in heifers. Administering Cr and MEL recovered the retarded growth rate and reduced displacement behavior, thereby alleviating regrouping stress.
PubMed: 38665072
DOI: 10.5713/ab.24.0104 -
Animals : An Open Access Journal From... Mar 2024(1) Background: It has been well established that castration and tail docking are both painful during and following the procedure, yet there are limited convenient and...
(1) Background: It has been well established that castration and tail docking are both painful during and following the procedure, yet there are limited convenient and effective products to address both short-term and long-term pain. Lidocam Topical Gel (LTG) (4% lidocaine and 0.3% meloxicam) was developed to address industry needs for an effective and safe product to address animal welfare concerns regarding castration and tail docking in piglets. (2) Methods: Study 1: Male piglets aged 4-8 days of age were treated with LTG (n = 30) or a control gel (n = 30). Approximately 30 min after application of the gel, the piglets were surgically castrated and tail docked. The efficacy of pain control during the surgical procedures and post-procedure (24 h) pain and inflammation control were evaluated using both behavioral and physiological measurements. Study 2: Meloxicam residue depletion following LTG treatment was followed for 28 days. Study 3: Clinical and pathological safety were evaluated in five groups of eight piglets receiving LTG with: (1) no treatment, (2) nominal topical dose, (3) two times the nominal topical dose, (4) three times the nominal topical dose, and 5) one times the nominal topical dose and 2 mL of LTG by oral gavage daily for 3 days. (3) Results: LTG-treated piglets had a significant reduction in electrocutaneous stimulation response before the procedures and 4 and 24 h post-procedures. Stress vocalization intensity and duration were less in piglets receiving LTG during the surgical procedures. Plasma cortisol and substance P were significantly lower in LTG-treated piglets 3 h after castration and tail docking. The weight and average daily gain were significantly increased in piglets receiving LTG. LTG did not interfere with wound healing or cause irritation at the application sites. There were no abnormal clinical or pathological findings associated with the use of LTG at three times the nominal dose given daily for three days. As meloxicam persisted in the application site tissue, a slaughter withdrawal time of 24 days was determined. (4) Conclusions: When applied to the skin 30 min before castration and tail docking, LTG is effective in surgical pain control and provides post-surgical pain control for up to 24 h. LTG is safe for use in piglets and provides an acceptable withdrawal time for commercial use. LTG is a potentially effective product for commercial use for piglet castration and tail docking.
PubMed: 38540028
DOI: 10.3390/ani14060930 -
Molecules (Basel, Switzerland) Jul 2023Secure and efficient treatment of diverse pain and inflammatory disorders is continually challenging. Although NSAIDs and other painkillers are well-known and commonly...
Secure and efficient treatment of diverse pain and inflammatory disorders is continually challenging. Although NSAIDs and other painkillers are well-known and commonly available, they are sometimes insufficient and can cause dangerous adverse effects. As yet reported, derivatives of pyrrolo[3,4-]pyridazinone are potent COX-2 inhibitors with a COX-2/COX-1 selectivity index better than meloxicam. Considering that -acylhydrazone (NAH) moiety is a privileged structure occurring in many promising drug candidates, we decided to introduce this pharmacophore into new series of pyrrolo[3,4-]pyridazinone derivatives. The current paper presents the synthesis and in vitro, spectroscopic, and in silico studies evaluating the biological and physicochemical properties of NAH derivatives of pyrrolo[3,4-]pyridazinone. Novel compounds --- were received with high purity and good yields and did not show cytotoxicity in the MTT assay. Their COX-1, COX-2, and 15-LOX inhibitory activities were estimated using enzymatic tests and molecular docking studies. The title -acylhydrazones appeared to be promising dual COX/LOX inhibitors. Moreover, spectroscopic and computational methods revealed that new compounds form stable complexes with the most abundant plasma proteins-AAG and HSA, but do not destabilize their secondary structure. Additionally, predicted pharmacokinetic and drug-likeness properties of investigated molecules suggest their potentially good membrane permeability and satisfactory bioavailability.
Topics: Hydrazones; Cyclooxygenase Inhibitors; Lipoxygenase Inhibitors; Pyridazines; Pyrroles; Humans; Fibroblasts; Computer Simulation; Cell Membrane Permeability; Cell Line
PubMed: 37513351
DOI: 10.3390/molecules28145479 -
Frontiers in Molecular Neuroscience 2024Pain mostly arises because specialized cells called nociceptors detect harmful or potentially harmful stimuli. In lower animals with less convoluted nervous system,...
INTRODUCTION
Pain mostly arises because specialized cells called nociceptors detect harmful or potentially harmful stimuli. In lower animals with less convoluted nervous system, these responses are believed to be purely nociceptive. Amongst invertebrate animal models, planarians are becoming popular in a wide range of pharmacological and behavioral studies beyond the field of regeneration. Recent publications led the way on pain studies by focusing on nociceptive behaviors such as the 'scrunching' gait displayed under various noxious stimuli, as opposed to the 'gliding' gait planarians usually adopt in normal conditions.
METHODS
In this study, we adapted commonly used nociceptive tests to further explore nociception in planarians of the species . By using behavioral analysis in open fields and place preferences, we managed to set up chemical, thermal and mechanical nociceptive tests. We also adapted RNA interference protocols and explored the effects of knocking down TRPA1 ion channels, one of the main effectors of chemically and thermally-induced nociceptive responses in vertebrates.
RESULTS
Consequently, we demonstrated the reliability of the scrunching gait in this planarian species, which they displayed in a dose-dependent manner when exposed to the irritant AITC. We also showed that suppressing the expression of TRPA1 ion channels completely suppressed the scrunching gait, demonstrating the involvement of TRPA1 nociceptors in this nociceptive reaction. Besides, we also explored the effects of two common analgesics that both displayed strong antinociceptive properties. First, morphine reduced the chemically-induced nociceptive scrunching gaits by more than 20% and shifted the of the dose-response curve by approximately 10 μM. Secondly, the NSAID meloxicam drastically reduced chemically-induced scrunching by up to 60% and reduced heat avoidance in place preference tests.
DISCUSSION
Thus, we managed to characterize both behavioral and pharmacological aspects of 's nociception, further developing the use of planarians as a replacement model in pain studies and more globally the study of invertebrate nociception.
PubMed: 38751713
DOI: 10.3389/fnmol.2024.1368009 -
Critical Reviews in Therapeutic Drug... 2024Meloxicam, a selective COX-2 inhibitor, has demonstrated clinical effectiveness in managing inflammation and acute pain. Although available in oral and parenteral...
Meloxicam, a selective COX-2 inhibitor, has demonstrated clinical effectiveness in managing inflammation and acute pain. Although available in oral and parenteral formulations such as capsule, tablet, suspension, and solution, frequent administration is necessary to maintain therapeutic efficacy, which can increase adverse effects and patient non-compliance. To address these issues, several sustained drug delivery strategies such as oral, transdermal, transmucosal, injectable, and implantable drug delivery systems have been developed for meloxicam. These sustained drug delivery strategies have the potential to improve the therapeutic efficacy and safety profile of meloxicam, thereby reducing the frequency of dosing and associated gastrointestinal side effects. The choice of drug delivery system will depend on the desired release profile, the target site of inflammation, and the mode of administration. Overall, meloxicam sustained delivery systems offer better patient compliance, and reduce the side effects, thereby improving the clinical applications of this drug. Herein, we discuss in detail different strategies for sustained delivery of meloxicam.
Topics: Humans; Meloxicam; Analgesics; Drug Delivery Systems; Acute Pain; Inflammation
PubMed: 38608134
DOI: 10.1615/CritRevTherDrugCarrierSyst.2024048988 -
Journal of Veterinary Pharmacology and... May 2024The aim of this study is to determine the pharmacokinetic change after intravenous administration of meloxicam at doses of 0.5, 1 and 2 mg/kg to sheep. The study was...
The aim of this study is to determine the pharmacokinetic change after intravenous administration of meloxicam at doses of 0.5, 1 and 2 mg/kg to sheep. The study was carried out on six Akkaraman sheep. Meloxicam was administered intravenously to each sheep at 0.5, 1, and 2 mg/kg doses in a longitudinal pharmacokinetic design with a 15-day washout period. Plasma concentrations of meloxicam were determined using the high performance liquid chromatography-ultraviolet, and pharmacokinetic parameters were evaluated by non-compartmental analysis. Meloxicam was detected up to 48 h in the 0.5 mg/kg dose and up to 96 h in the 1 and 2 mg/kg doses. As the dose increased from 0.5 to 2 mg/kg, terminal elimination half-life, and dose normalized area under the concentration versus time curve increased and total clearance decreased. Compared to the 1 mg/kg dose, it was determined that V decreased and C increased in the 2 mg/kg dose. Meloxicam provided the therapeutic concentration of >0.39 μg/mL reported in other species for 12, 48 and 96 h at 0.5, 1 and 2 mg/kg doses, respectively. These results show that meloxicam exhibits non-linear pharmacokinetics and will achieve unpredictable plasma concentrations when administered IV for a rapid effect at dose of ≥1 mg/kg in sheep.
Topics: Animals; Meloxicam; Sheep; Anti-Inflammatory Agents, Non-Steroidal; Area Under Curve; Half-Life; Injections, Intravenous; Dose-Response Relationship, Drug; Female; Male; Administration, Intravenous
PubMed: 38033195
DOI: 10.1111/jvp.13422 -
Annales Pharmaceutiques Francaises Apr 2024.In this study, we investigated the potential of meloxicam (MLX) developed as transferosomal gel as a novel lipidic drug delivery system to address osteoarthritis (OTA),...
OBJECTIVE
.In this study, we investigated the potential of meloxicam (MLX) developed as transferosomal gel as a novel lipidic drug delivery system to address osteoarthritis (OTA), a degenerative joint disease that causes pain and stiffness. By incorporating meloxicam into a transferosomal gel, our aim was to provide a targeted and efficient delivery system capable of alleviating symptoms and slowing down the progression of OTA.
MATERIAL AND METHODS
Classical lipid film hydration technique was utilized to formulate different transferosomal formulations. Different transferosomal formulations were prepared by varying the molar ratio of phospholipon-90H (phosphodylcholine) to DSPE (50:50, 60:40, 70:30, 80:20, and 90:10) and per batch, 80mg of total lipid was used. The quality control parameters such as entrapment efficiency, particle size and morphology, polydispersity and surface electric charge, in vitro drug release, ex vivo permeation and stability were measured.
RESULTS
The optimized transferosomal formulations revealed a small vesicle size (121±12nm) and greater MLX entrapment (68.98±2.3%). Transferosomes mediated gel formulation MLX34 displayed pH (6.3±0.2), viscosity (6236±12.3 cps), spreadability (13.77±1.77 gm.cm/sec) and also displayed sustained release pattern of drug release (81.76±7.87% MLX released from Carbopol-934 gel matrix in 24h). MLX34 revealed close to substantial anti-inflammatory response, with ∼81% inhibition of TNF-α in 48h. Physical stability analysis concluded that refrigerator temperature was the preferred temperature to store transferosomal gel.
CONCLUSION
MLX loaded transferosomes containing gel improved the skin penetration and therefore resulted into increased inhibition of TNF-α level.
PubMed: 38657858
DOI: 10.1016/j.pharma.2024.04.006 -
Environmental Science and Pollution... Oct 2023Graphite-like carbon nitride (g-CN) is favored for its excellent physicochemical properties. However, the high complexation rate of photogenerated carriers greatly...
Graphite-like carbon nitride (g-CN) is favored for its excellent physicochemical properties. However, the high complexation rate of photogenerated carriers greatly limits its practical applications. Based on this, a novel CQDs-doped carbon nitride nanosheets composite (CNS/CQDs) was prepared and applied to the visible light-induced activation of peroxymonosulfate (PMS) for meloxicam (Mel) and tetracycline (TC) degradation. The photocatalytic degradation of Mel and TC were remarkably promoted in the CNS/CQDs+PMS+vis system. Mel photodegradation of 99.90% was achieved over 30 min with 20 mg CNS/CQDs and 20 mg PMS at pH11. And TC photodegradation of 95.97% was achieved over 45 min with 20 mg CNS/CQDs and 20 mg PMS at nature pH6.5. The TOC mineralization rates of Mel and TC were 75.49% and 52.00%, respectively. The transient photocurrent response and electrochemical impedance measurements (EIS) results indicated that the doping of CQDs could improve the charge transfer efficiency of pure g-CN, and CNS/CQDs had a low charge transfer resistance. Capture experiments and EPR tests explored the effective actives in the CNS/CQDs+PMS+vis system. Possible degradation pathways of Mel were also analyzed. This study provides valid residual drugs degradation under the dual conditions of visible light catalytic oxidation and persulfate oxidation, which will be a novel perspective for advanced oxidation technology to effectively remove organic pollutants from water.
Topics: Water; Graphite; Anti-Bacterial Agents; Tetracycline; Catalysis; Light; Carbon
PubMed: 37752394
DOI: 10.1007/s11356-023-30005-w