fumaric-acid and Inflammation

Topical administration is a promising clinical strategy to avoid serious gastrointestinal adverse reactions of loxoprofen sodium (LOX), a new non-steroidal anti-inflammatory drug. Small molecule organic acids had been reported with the ability of promoting transdermal rate of several drugs. In this article, the effect of small molecule organic acids on the transdermal delivery of LOX was studied, and the possible mechanism was also explored by Fourier infrared spectroscopy, differential scanning calorimetry, tape stripping, etc. The results showed that lactic acid and fumaric acid could significantly increase the penetration rate of LOX and reduce time lag even without the help of acidic environment. The preliminary mechanism investigation inferred that fumaric acid could increase LOX's distribution in stratum corneum and might change its complexation state, but had little effect on the drug structure and skin's lipids and proteins configuration. The topical LOX gel using fumaric acid as penetration enhancer had higher transdermal rate, significant anti-inflammatory effect and no obvious skin irritation. This study proved the promising application of small molecule organic acids in transdermal enhancing and provided a potential strategy for transdermal delivery of LOX combined with fumaric acid.

Topics: Administration, Cutaneous; Animals; Anti-Inflammatory Agents, Non-Steroidal; Carrageenan; Disease Models, Animal; Female; Fumarates; Gels; Inflammation; Lactic Acid; Male; Phenylpropionates; Rabbits; Rats, Sprague-Dawley; Skin; Skin Absorption; Swine; Swine, Miniature; Time Factors

Topics: Adaptive Immunity; Adult; Antigen Presentation; Arsenic; Cells, Cultured; Cytokines; Dendritic Cells; Fumarates; Humans; Immunity, Innate; Inflammation; Male; Monocytes; Phagocytosis; Toll-Like Receptor 4; Up-Regulation; Young Adult

To improve surgical results in patients with benign prostatic hyperplasia (BPH) and urolithiasis (UL) and to evaluate the efficacy of Furamag used as an agent to prevent infectious and inflammatory complications.. Seventy-two patients with BPH (n = 36; Group 1) and UL (n = 36; Group 2) were examined. Within each group, the patients were divided into two subgroups: A) those in whom no preventive measures were taken during endoscopic operations; B) those who received Furamag as a preventive agent. The preventive efficacy was evaluated from the urine microbial spectrum and renal microcirculatory values.. The preventive use of Furamag could achieve better urine sanitation, normalize renal microcirculatory values, and reduce the incidence of postoperative complications.. The use of Furamag to prevent intravesical obstruction (IVO) during transurethral prostatic resection and UL reduces the incidence of IVO, results in less noticeable renal microcirculatory disorders, and accordingly assists in lowering the incidence of postoperative complications.

Topics: Endoscopy; Fumarates; Humans; Inflammation; Male; Middle Aged; Postoperative Complications; Prostatic Hyperplasia; Treatment Outcome; Urolithiasis

This protocol describes microsphere-based protease assays for use in flow cytometry and high-throughput screening. This platform measures a loss of fluorescence from the surface of a microsphere due to the cleavage of an attached fluorescent protease substrate by a suitable protease enzyme. The assay format can be adapted to any site or protein-specific protease of interest and results can be measured in both real time and as endpoint fluorescence assays on a flow cytometer. Endpoint assays are easily adapted to microplate format for flow cytometry high-throughput analysis and inhibitor screening.

Topics: Animals; Biotinylation; Flow Cytometry; Fluorescence Resonance Energy Transfer; Green Fluorescent Proteins; High-Throughput Screening Assays; Humans; Inflammation; Kinetics; Microspheres; Peptide Hydrolases; Peptides; Reproducibility of Results; Temperature