Preclinical studies of a high drug-loaded meloxicam nanocrystals injection for analgesia

Colloids Surf B Biointerfaces. 2022 Oct:218:112777. doi: 10.1016/j.colsurfb.2022.112777. Epub 2022 Aug 17.

Abstract

Meloxicam (MLX) is considered to have significant analgesic properties. However, the analgesic effects of MLX are compromised by its poor water solubility and thus the low drug loading. The purpose of this study was to develop a high drug-loaded MLX injection by formulating it into nanocrystals (NCs) for the treatment of analgesia. The developed MLXNCs exhibited satisfactory particle sizes and remarkably in vitro dissolution behaviors. In addition, the plasma concentrations of MLXNCs were comparable with the MLX solution (formulated with 1.0% polyoxyethylene castor oil 35) in rats. The acetic acid-induced writhing tests, hot plate tests and hind paw incision experiments demonstrated that the MLXNCs had significant analgesic effects. The findings provide insights into the developed high drug-loaded MLXNCs and provide new therapeutic options for acute and chronic pain management.

Keywords: Analgesia; Meloxicam; Nanocrystals; Polyethylene glycol; Sodium deoxycholate.

MeSH terms

  • Acetates
  • Analgesia*
  • Animals
  • Anti-Inflammatory Agents, Non-Steroidal
  • Meloxicam / chemistry
  • Nanoparticles*
  • Pain / drug therapy
  • Pain Management
  • Rats
  • Thiazines* / pharmacology
  • Thiazines* / therapeutic use
  • Thiazoles / chemistry
  • Thiazoles / pharmacology
  • Water

Substances

  • Acetates
  • Anti-Inflammatory Agents, Non-Steroidal
  • Thiazines
  • Thiazoles
  • Water
  • Meloxicam