The aim of this study was to prepare nanostructured lipid carriers (NLC)-based topical gel of aceclofenac for the treatment of inflammation and allied conditions. Stearic acid as the solid lipid, oleic acid as the liquid lipid, pluronic F68 as the surfactant, and phospholipon 90G as the co-surfactant were used. NLCs were prepared by melt-emulsification, low-temperature solidification, and high-speed homogenization methods. Characterization of the NLC dispersion was carried out through particle size analysis, scanning electron microscopy (SEM), differential scanning calorimetry (DSC), and an in vitro release study. The anti-inflammatory effect of the NLC gel was assessed by the rat paw edema technique and compared to marketed aceclofenac gel. The NLC dispersions exhibited d90% between 233 nm and 286 nm. All of the NLC showed high entrapment efficiency ranging from 67% to 82%. The particle size of NLC was further confirmed by the SEM study. The result of DSC showed that aceclofenac was dispersed in NLC in an amorphous state. Both the entrapment and release rate were affected by the percentage of oleic acid, but the method of preparation affected only the entrapment efficiency. The nanoparticulate dispersion was suitably gelled and assessed for in vitro permeation. Finally, NLC-based gels were found to possess superior (almost double) the anti-inflammatory activity compared to the marketed product. The anti-inflammatory activity of NLC gel showed a rapid onset of action, as well as a prolonged duration of action as compared with the marketed gel.
IntrOductIOnSpinal anaesthesia is the gold standard for lower abdominal surgeries. It has got the advantage of being, cost-effective, easy administration technique, rapid onset of action, with relatively less adverse effects and most importantly patient remaining aroused throughout the procedure [1]. But at times short duration and uncomfortable postoperative period offset the above advantages. Therefore, in order to extend the intraoperative analgesia into postoperative period, following spinal anaesthesia, various spinal adjuvants like morphine, buprenorphine and fentanyl, clonidine, ketamine are being used in anaesthetic practice. Such adjuvants have been helpful in induction of early ambulation along with prolongation of analgesia but at the cost of their associated adverse effects. Therefore search for an effective adjuvant is still going on.Alpha-2 (α 2 ) adrenergic receptor agonists have been tried by many clinicians due to their sedative, anxiolytic, hypnotic, analgesic, perioperative sympatholytic and stable haemodynamic properties [2]. The initiation for the use of α 2 agonists in anaesthesia resulted from observations made in patients who were receiving clonidine therapy. Dexmedetomidine, a Dextro (s) isomer of medetomidine was approved for short term sedation in 1999. It possesses all the above properties but lacks respiratory depressant action; making it a relatively safe agent [3]. Currently its adjuvant action in spinal anaesthesia is being explored. Various adjuvants like morphine, buprenorphine and fentanyl, clonidine, ketamine are being used in anaesthetic practice since long for improvement of peri-operative analgesia following spinal anaesthesia. Such adjuvants have been helpful in induction of early ambulation but at the cost of their associated adverse effects. Therefore search for an effective adjuvant is still going on. Currently Dexmedetomidine, a highly selective α 2 -adrenoreceptor agonist is being studied for its adjuvant action in spinal anaesthesia.
Objective:The present study was designed to evaluate the effect of Aegle marmelos unripe fruit extract (AMFE) on inflammatory bowel disease (IBD) in Wistar albino rats.Materials and Methods:Effect of AMFE was studied on acetic acid induced ulcerative colitis (1 ml of 4% acetic acid solution, transrectal) and indomethacin-induced enterocolitis (10 mg/kg, single dose, p.o) in Wistar albino rats. The extract was administered orally at different dose of 150, 200 and 250 mg/kg body weight. Disease pathogenesis was assessed by measuring disease activity index (DAI), macroscopic score, microscopic score, mesenteric mast cell protection, superoxide dismutase (SOD), and malonaldehyde (MDA) levels in the above two models.Results:The results showed a dose dependent decrease in intestinal inflammation following treatment with AMFE. Significant protection in mast cell degranulation was observed in acetic acid and indomethacin-induced IBD models. Treatment with AMFE significantly decreased the MDA levels and increased SOD activity.Conclusion:In our study, AMFE produced anti-inflammatory, antioxidant, and mast cell stabilizing effects demonstrating protective effect in inflammatory bowel disease.
Background:Erythropoietin, originally recognized for its role in erythropoiesis, has been shown to improve neurological outcome after stroke. Low-dose methotrexate is effective against certain inflammatory diseases, such as severe psoriasis and rheumatoid arthritis as well as Crohn's disease. Immunosuppressive effect of methotrexate also reduces the proportion of patients with chronic progressive multiple sclerosis with modest clinical benefits. Combination of erythropoietin and methotrexate can target neuroinflammation along with immunosupression.Objective:To evaluate the role of erythropoietin and methotrexate in experimental autoimmune encephalomyelitis, a commonly used animal model of several degenerative human diseases like multiple sclerosis.Materials and Methods:In the present study, C57BL/J6 mice were immunized with 200 μg of myelin basic protein (MBP) emulsified in complete Freund's adjuvant (CFA) supplemented with 1 mg/ml of killed mycobacterium tuberculosis (MBP: CFA in 1:1 ratio). These animals were given a combination of methotrexate and erythropoietin. Neurological function tests were scored daily by grading of clinical signs. Cerebral histopathology was performed to detect inflammatory infiltrates and demyelination.Results:Treatment with erythropoietin and methotrexate significantly improved the neurological function recovery, reduced inflammatory infiltrates, and demyelination as compared to controls possibly by stimulating oligodendrogenesis and down-regulating proinflammatory infiltrates.Conclusion:The findings suggest an adjunctive use of methotrexate in demyelinating disease.
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