Development and In-Vitro Tuning of Piperine Containing Solid Lipid Microparticles for the Treatment of Rheumatoid Arthritis

AAPS PharmSciTech. 2025 Jan 22;26(1):44. doi: 10.1208/s12249-024-03034-y.

Abstract

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. Microparticles were also investigated for piperine-lipid compatibility, thermal analysis, surface morphology, piperine (PIP) release trend, and anti-rheumatic activity in rats. The network's grafting was confirmed by FTIR and XRD results. The thermal stability of the constructed network was confirmed by the DSC and TGA results. SEM findings confirm porous surface morphology. The dissolution experiments on SLMs confirmed the sustained release profile, delivering 87.82% to 94.92% of piperine at 7.4 pH for 24 h. All developed formulations followed a zero-order kinetic model and the Korsmeyer-Peppas model. Furthermore, the anti-rheumatic potentials of piperine from SLMs were also investigated and compared with diclofenac sodium (the standard treatment) in a rat model. The analysis revealed that PIP significantly reduced the severity of arthritis, as confirmed by the findings of multiple arthritic assessment parameters.

Keywords: Carnauba wax and bees wax; Microparticles; Piperine; Piperine-loaded microparticles; Rheumatoid arthritis.

MeSH terms

  • Alkaloids* / administration & dosage
  • Alkaloids* / chemistry
  • Alkaloids* / pharmacology
  • Animals
  • Antirheumatic Agents / administration & dosage
  • Antirheumatic Agents / chemistry
  • Antirheumatic Agents / pharmacology
  • Arthritis, Rheumatoid* / drug therapy
  • Benzodioxoles* / administration & dosage
  • Benzodioxoles* / chemistry
  • Benzodioxoles* / pharmacology
  • Chemistry, Pharmaceutical / methods
  • Drug Carriers / chemistry
  • Drug Liberation
  • Lipids* / chemistry
  • Male
  • Microspheres
  • Particle Size*
  • Piperidines* / administration & dosage
  • Piperidines* / chemistry
  • Piperidines* / pharmacology
  • Polysorbates / chemistry
  • Polyunsaturated Alkamides* / administration & dosage
  • Polyunsaturated Alkamides* / chemistry
  • Polyunsaturated Alkamides* / pharmacology
  • Rats
  • Rats, Wistar
  • Solubility
  • Waxes* / chemistry

Substances

  • Polyunsaturated Alkamides
  • piperine
  • Benzodioxoles
  • Alkaloids
  • Piperidines
  • Lipids
  • Waxes
  • carnauba wax
  • beeswax
  • Polysorbates
  • Drug Carriers
  • Antirheumatic Agents