98%
921
2 minutes
20
Periarticular injections with a combination of local anesthetics, non-steroidal anti-inflammatory analgesics (NSAIDs), and epinephrine are becoming increasingly popular in the perioperative analgesia of artificial joint replacement. However, data on the efficacy and safety of local injection NSAIDs are still scarce. The purpose of this study was to investigate the efficacy and safety of a local injection of Flurbiprofen Ester Lipid microspheres into the inflammatory model of femoral shaft closed fractures in rats. A systemic inflammatory model was induced in SD rats (60) by closed femoral shaft fracture; 12 non-fractured rats were used as the blank control group (group A). The systemic inflammation model of 60 rats was divided into 5 groups (12 in each group); Group B: intramuscular injectionof the same amount of normal saline at different time points as a negative control; Group C: intravenous injection of Flurbiprofen Ester microspheres (4.5 mg/kg) at different time points; Group D: intramuscular injection of Flurbiprofen Ester microspheres (2.25 mg/kg) at different time points; Group E: intramuscular injection of Flurbiprofen Ester microspheres (4.5 mg/kg) at different time points; Group F: intramuscular injection of Flurbiprofen Ester microspheres (9 mg/kg) at different time points. The behavioral test observed the behavior of the rats. Then, the inflammation factors of CRP, IL-6, COX-1, COX-2 and TNF-αby ELISA were recorded. Through the behavioral test it could be found that the effect of the intramuscular and intravenous injections of Flurbiprofen Ester microspheres was similar. Fracture rats with a local injection of Flurbiprofen Ester microspheres showed lower inflammation levels measured by COX-1, CRP, and TNF-α compared with the control group. Pathological sections at 24, 48, and 96 h after surgery did not display any local muscle necrosis at the local injection site. These findings suggested that a Flurbiprofen Ester microsphere muscular injection exhibited a similar effect to an intravenous injection. The local injection of Flurbiprofen Ester microspheres significantly reduced the inflammatory response in fracture rats and did not increase the risk of muscle necrosis, suggesting its feasibility in local injection analgesia.
Download full-text PDF |
Source |
---|---|
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC8987705 | PMC |
http://dx.doi.org/10.3389/fphar.2022.769577 | DOI Listing |
Int J Pharm
June 2025
West Pomeranian University of Technology in Szczecin, Faculty of Chemical Technology and Engineering, Department of Organic Chemical Technology and Polymer Materials, Piastów Ave. 42, 71-065 Szczecin, Poland; Center for Advanced Materials and Manufacturing Process Engineering (CAMMPE), Piastów Ave
The present study aimed to evaluate the influence of chemical modifications on the properties of flurbiprofen derivatives, focusing particularly on their skin permeation and accumulation. Comprehensive characterization of all synthesized compounds was conducted using NMR, FTIR, and HRMS for structural analysis. Crystallinity was assessed via XRD, while thermal stability and properties were evaluated using TG and DSC, respectively.
View Article and Find Full Text PDFInt J Biol Macromol
June 2025
College of Pharmacy, Dalian Medical University, Dalian 116044, China. Electronic address:
Targeted drug delivery strategy can accurately deliver multiple drugs to tumor cells by biocompatible materials, enhance the therapeutic effect and weaken adverse side effects. Chondroitin sulfate (CS) is a biodegradable material which has dual-targeting ability to CD44 receptors and Golgi apparatus. Flurbiprofen is a COX-2 inhibitor that can be used as an anticancer adjuvant in combination with docetaxel to enhance the antitumor effect.
View Article and Find Full Text PDFJ Toxicol Sci
May 2025
Faculty of Pharmaceutical Sciences, Josai International University.
Three-dimensional cultured skin (3D skin) models have been utilized for in vitro skin permeation tests to evaluate the skin permeation rate and local effects (efficacy and toxicity) of applied chemicals, particularly from the perspective of the 3Rs (reduction, replacement, refinement) approach. The steady-state concentration of applied chemicals at different depths in the viable epidermis and dermis (VED) is affected by their skin permeation parameters, such as permeability coefficient (K) and partition coefficient (K) from the donor solution to the skin of the chemicals. In the present study, the steady-state concentration of chemicals in the VED of EpiDerm 606X (EpiDerm) as representative of a 3D skin model were compared with hairless rat skin.
View Article and Find Full Text PDFClin J Pain
December 2024
Department of Anesthesiology, First Hospital of China Medical University, Shenyang, China.
Chem Commun (Camb)
September 2024
Department of Chemistry, Indian Institute of Technology Delhi, Hauz Khas, New Delhi, 110016, India.
A metal-free strategy has been developed for the α-arylation of carboxylic acids, secondary amides, and esters employing arenes as key reagents. This process entails the Lewis-acid catalyzed reductive Friedel-Crafts alkylation of arenes utilizing α-ketoacids, facilitated by silane in HFIP solvent. The transformation exhibits exceptional functional group tolerance, enabling late-stage functionalization of natural products.
View Article and Find Full Text PDF