Long-term stability of bevacizumab repackaged in 1mL polypropylene syringes for intravitreal administration

Ann Pharm Fr. 2012 May;70(3):139-54. doi: 10.1016/j.pharma.2012.03.006. Epub 2012 May 11.

Abstract

Introduction: The anti-angiogenic monoclonal antibody, bevacizumab, is currently used by intravitreal administration as off-label drug to treat age-related macular degeneration or other ophthalmologic diseases. For this purpose, commercial bevacizumab is repackaged in 1mL polypropylene syringes under sterile conditions. However, no complete study on the stability of this hospital-based preparation is available.

Methods: Commercial bevacizumab (25mg/mL; Avastin(®)) was aseptically repackaged in 1mL polypropylene syringes, stored at 4°C, and analyzed within the preparation day (D0), after 30 days (D30) and 90 days (D90). Some syringes were kept for up to 8 months to observe possible instability. Several complementary and stability-indicating analytical methods were used to assess in details the primary, secondary and tertiary structure of the antibody during its conservation: ionic chromatography, size-exclusion chromatography, peptide mapping, 2nd derivative UV and IR spectroscopy, turbidimetry, diffraction laser spectroscopy, thermal denaturation curves, microscopic examination and image analysis.

Results: We clearly demonstrate that the commercial solution of bevacizumab can be safely repackaged in polypropylene syringes and stored up to 3 months at 4°C without alteration of its primary, secondary and tertiary structure. The only difference observed is the contamination of the syringe content by silicone oil microdroplets, which is quite immediate and does not change significantly during the storage in terms of number and size.

Conclusion: Our results support the off-label use of repackaged bevacizumab by intravitreal administration, at least from a pharmaceutical point of view, with a validated stability of 3 months. This stability period is largely enough to practical situations and support current practices, such as in advance or batch preparations, which present major advantages in terms of GMP respect, workload optimization and financial savings.

MeSH terms

  • Angiogenesis Inhibitors / administration & dosage
  • Angiogenesis Inhibitors / analysis*
  • Angiogenesis Inhibitors / chemistry
  • Antibodies, Monoclonal, Humanized / administration & dosage*
  • Antibodies, Monoclonal, Humanized / analysis*
  • Antibodies, Monoclonal, Humanized / chemistry
  • Bevacizumab
  • Chromatography, Gel
  • Drug Compounding
  • Drug Stability
  • Drug Storage
  • Injections
  • Macular Degeneration
  • Nephelometry and Turbidimetry
  • Peptide Mapping
  • Pharmacy Service, Hospital
  • Polypropylenes
  • Spectrophotometry, Infrared
  • Spectrophotometry, Ultraviolet
  • Syringes
  • Temperature
  • Vitreous Body*

Substances

  • Angiogenesis Inhibitors
  • Antibodies, Monoclonal, Humanized
  • Polypropylenes
  • Bevacizumab