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Leflunomide biodegradable microspheres intended for intra-articular administration: Development, anti-inflammatory

Doaa Ahmed El-Setouhy1, Nevine Shawky Abdelmalak1, Shady E Anis2

  • 1Pharmaceutics and Industrial Pharmacy Deptartment, Faculty of Pharmacy, Cairo University, Cairo, Egypt.

International Journal of Pharmaceutics
|September 23, 2015
PubMed

Insights

Intraarticular leflunomide microspheres offer prolonged drug release and reduced inflammation in arthritis models. This novel formulation demonstrates biocompatibility and improved anti-inflammatory effects compared to oral administration.

Area of Science:

  • Pharmacology
  • Biomaterials Science
  • Rheumatology

Background:

  • Leflunomide is a disease-modifying anti-rheumatic drug (DMARD) used for treating inflammatory conditions.
  • Current administration methods may lead to systemic side effects and suboptimal drug delivery to target joints.
  • Microsphere formulations offer potential for localized, sustained drug delivery.

Purpose of the Study:

  • To develop and characterize leflunomide-loaded biodegradable microspheres for intraarticular injection.
  • To evaluate the in vivo efficacy and biocompatibility of the optimized microsphere formulation in an arthritis rat model.

Main Methods:

  • Eight leflunomide microsphere formulations were prepared using polylactide-co-glycolide (PDLG) and polycaprolactone (PLC) via solvent evaporation.
  • Formulations were characterized for encapsulation efficiency, particle size, drug release kinetics, and morphology (SEM).
  • In vivo studies involved intraarticular injection of the optimized formulation (F6) into arthritis-induced rats and comparison with oral administration of Avara® (leflunomide). Inflammation markers (NF-κB) and histopathology were assessed.

Main Results:

  • Optimized microsphere formulation F6 (PDLG 5010) exhibited suitable particle size and prolonged drug release.
  • Intraarticular injection of F6 significantly reduced inflammation in arthritic rats, comparable to oral Avara®.
  • Histopathological analysis of F6-treated joints showed minimal inflammatory cell infiltration and no angiogenesis, indicating superior local anti-inflammatory effects and biocompatibility.

Conclusions:

  • Biodegradable leflunomide microspheres are a viable formulation for intraarticular injection, providing sustained drug release.
  • The intraarticular microsphere formulation demonstrates significant anti-inflammatory efficacy and improved local tissue response compared to oral leflunomide.
  • The study confirms the biocompatibility of the PDLG polymer for intraarticular drug delivery applications.
Keywords:
Dinalouis@hotmail.comHistopathologyIntraarticular injectionLeflunomideMicrospheresNuclear kappa factorPolycaprolactone

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