The Anti-Arthritic Activity of Diclofenac Lipid-Core Nanocapsules: Stereological Analysis Showing More Protection of Deep Joint Components

• Published in: Molecules (Basel, Switzerland) Switzerland), 2023-07, Vol.28 (13), p.5219
• Main Authors: Ureña, Nathalie Marte, de Oliveira, Catiúscia Padilha, Guterres, Silvia Stanisçuaski, Pohlmann, Adriana Raffin, da Costa, Oscar Tadeu Ferreira, Boechat, Antonio Luiz
• Format: Article
• Language: English
• Subjects: adjuvant arthritis; Analysis; Animals; Anti-inflammatory agents; Antiarthritic agents; Arthritis; Arthritis, Experimental - drug therapy; Brownian motion; C-reactive protein; Cartilage; Chondrocytes; Creatinine; Cytokines; Diclofenac; Diclofenac - pharmacology; Diclofenac - therapeutic use; Drug delivery; Drug delivery systems; Drugs; Edema; Efficiency; Enzymes; Inflammation; Joint diseases; lipid-core nanocapsules; Lipids; Lipids - therapeutic use; Liver; Nanocapsules; nanoformulation; Nonsteroidal anti-inflammatory drugs; Rats; Self-assembly; Side effects; stereology; Synoviocytes; Vehicles; Xanthine oxidase
• ISSN: 1420-3049; 1420-3049
• DOI: 10.3390/molecules28135219

Diclofenac is the most prescribed nonsteroidal anti-inflammatory drug worldwide and is used to relieve pain and inflammation in inflammatory arthritis. Diclofenac is associated with serious adverse effects, even in regular-dose regimens. Drug delivery systems can overcome this issue by reducing adverse effects and optimizing their efficacy. This study evaluated the activity of lipid-core nanocapsules loaded with diclofenac (DIC-LNCs) in an experimental model of adjuvant-induced arthritis. The diclofenac nanoformulation was obtained via self-assembly. A stereological analysis approach was applied for the morphological quantification of the volume, density, and cellular profile count of the metatarsophalangeal joints of rats. Proinflammatory cytokines and biochemical profiles were also obtained. Our results showed that the diclofenac nanocapsule DIC-LNCs were able to reduce arthritis compared with the control group and the DIC group. DIC-LNCs efficiently reduced proinflammatory cytokines, C-reactive protein, and xanthine oxidase levels. Additionally, DIC-LNCs reduced the loss of synoviocytes and chondrocytes compared with the DIC ( < 0.05) and control groups ( < 0.05). These data suggest that DIC-LNCs have anti-arthritic activity and preserve joint components, making them promising for clinical use.