Formulation and Evaluation of Meloxicam Hybrid nano Particles

AAPS PharmSciTech. 2024 Jul 24;25(6):172. doi: 10.1208/s12249-024-02878-8.

Abstract

The goal of the present study was to prepare meloxicam (MX) entrapped hybrid particles (HPs) to enhance intestinal permeation and anti-inflammatory activity. MX-HPs were prepared by nanoprecipitation method using lipid, chitosan, poloxamer, and TPGS. The formulations (MX-HPs1, MX-HPs2, MX-HPs3) were evaluated for particle size, entrapment efficiency, and drug release to select the optimized composition and further evaluated for permeation study, stability study, morphology, interaction study, and anti-inflammatory activity by carrageenan-induced rat paw edema test. The prepared MX-HPs showed nano sized particles (198.5 ± 3.7 to 223.8 ± 2.1 nm) and PDI (<0.3), zeta potential (16.5 ± 2.7 to 29.1 ± 3.6 mV), and high entrapment efficiency (75.1 ± 4.7 to 88.5 ± 3.9%). The surface morphology was assessed by transmission electron microscopy and showed non-aggregated particles. Infra-red (IR) spectroscopy of pure MX as well as formulation revealed no drug-polymer interaction and X-ray diffraction confirmed the conversion of crystalline MX into amorphous form. The release study data revealed prolonged MX release for 24 h. The selected optimized hybrid particles (MX-HPs2) revealed a 2.3-fold improved enhancement ratio than free MX. The storage stability and gastrointestinal stability data demonstrated a stable formulation in SIF as well as SGF. The anti-inflammatory activity showed better therapeutic action than pure MX dispersion. From the study, it can be concluded that the prepared MX-HPs may be a promising delivery system for MX in treating inflammatory disorders.

Keywords: anti-inflammatory activity; chitosan; hybrid particles; intestinal permeation; meloxicam.

MeSH terms

  • Animals
  • Anti-Inflammatory Agents, Non-Steroidal* / administration & dosage
  • Anti-Inflammatory Agents, Non-Steroidal* / chemistry
  • Anti-Inflammatory Agents, Non-Steroidal* / pharmacology
  • Carrageenan / chemistry
  • Chemistry, Pharmaceutical / methods
  • Chitosan / chemistry
  • Drug Carriers / chemistry
  • Drug Liberation*
  • Drug Stability
  • Edema / drug therapy
  • Lipids / chemistry
  • Male
  • Meloxicam* / administration & dosage
  • Meloxicam* / chemistry
  • Meloxicam* / pharmacology
  • Nanoparticles* / chemistry
  • Particle Size*
  • Poloxamer / chemistry
  • Rats
  • Rats, Wistar
  • Thiazines / administration & dosage
  • Thiazines / chemistry
  • Thiazines / pharmacokinetics
  • Thiazines / pharmacology
  • Thiazoles / chemistry
  • Thiazoles / pharmacology
  • Vitamin E / chemistry
  • Vitamin E / pharmacology

Substances

  • Meloxicam
  • Anti-Inflammatory Agents, Non-Steroidal
  • Drug Carriers
  • Thiazines
  • Poloxamer
  • Thiazoles
  • Chitosan
  • Lipids
  • tocophersolan
  • Carrageenan
  • Vitamin E