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Nanoformulation of Polymyxin E Through Complex Coacervation: A Pharmacokinetic Analysis.
Pharmaceutics
January 2025
Center for Pharmacy, University of Bergen, 5020 Bergen, Norway.
Polymyxin E (PME), a polymyxin antibiotic, serves as a final resort against antibiotic resistance. Nephrotoxicity is the primary concern when employing PME. To alleviate this issue, researchers have explored strategies including dosing adjustments and innovative formulations.
View Article and Find Full Text PDFShaking it off: loss of NHE3-mediated calcium reabsorption is compensated by the distal nephron.
Kidney Int
February 2025
Department of Pediatrics, The Faculty of Medicine and Dentistry, University of Alberta, Edmonton, Alberta, Canada. Electronic address:
Sodium reabsorption is tightly coupled to calcium reabsorption in the proximal tubule via the action of the Na/H exchanger isoform 3 (NHE3). Poulsen et al. provide evidence of reduced proximal calcium reabsorption in kidney tubule-specific NHE3-deficient mice that is compensated distally, unaltered phosphate homeostasis, and NHE3 involvement in the hypocalciuric effect of thiazides.
View Article and Find Full Text PDFDiscovery of selective ROCK2 inhibitors with free radical scavenging ability for the treatment of gouty arthritis.
Mol Divers
January 2025
Key Laboratory of Structure-Based Drugs Design and Discovery of Ministry of Education, Shenyang Pharmaceutical University, Shenyang, PR China.
ROCK inhibitors can inhibit IL-1β and NLRP3, and their therapeutic potential for osteoarthritis and rheumatoid arthritis has been confirmed, but their impact on gouty arthritis has not been reported yet. By hybridization the structure of Edaravone, a series of ROCK inhibitors with pyrazolone scaffold were designed and synthesized. RM-04 has acceptable selective ROCK2 inhibitory activity with an IC of 4.
View Article and Find Full Text PDFDevelopment and In-Vitro Tuning of Piperine Containing Solid Lipid Microparticles for the Treatment of Rheumatoid Arthritis.
AAPS PharmSciTech
January 2025
Department of Pharmaceutics, College of Pharmacy, King Saud University, PO Box 2457, 11451, Riyadh, Saudi Arabia.
The current project was designed to develop piperine-loaded solid lipid microparticles (SLMs) to assess the anti-arthritic potential of piperine (PIP). Variable proportions of carnauba wax, beeswax, and tween 80 were employed for preparing SLMs by using the solvent evaporation technique. The developed formulations were subjected to particle size measurements, entrapment efficiency (EE), and zeta potential (ZP) determination.
View Article and Find Full Text PDFLactoferrin-functionalized PEGylation liposomes loaded with norcantharidin acid for targeted therapy of hepatocellular carcinoma.
Int J Pharm
January 2025
School of Pharmacy, Shenyang Pharmaceutical University, Shenyang 110116, China.
Norcantharidin (NCTD), an antitumor agent with an increased leukocyte function, has been used for the treatment of hepatocellular carcinoma (HCC) in clinical. However, the clinical application of NCTD is limited due to its inadequate hydrophilicity and lipophilicity, short half-life (t), as well as adverse effects such as vascular irritation, cardiotoxicity, and nephrotoxicity. Herein, a lactoferrin (Lf) and DSPE-mPEG functionalized liposomes loaded with norcantharidic acid (NCA), an active metabolite of NCTD, was constructed for the targeted therapy of HCC.
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