April 2014
Volume 55, Issue 13
ARVO Annual Meeting Abstract  |   April 2014
Systemic treatment with glutathione PEGylated liposomal methylprednisolone (2B3-201) improves therapeutic efficacy in a model of ocular inflammation
Author Affiliations & Notes
  • Arie Reijerkerk
    to-BBB technologies BV, Leiden, Netherlands
  • Chantal C Appeldoorn
    to-BBB technologies BV, Leiden, Netherlands
  • Jaap Rip
    to-BBB technologies BV, Leiden, Netherlands
  • Marco de Boer
    to-BBB technologies BV, Leiden, Netherlands
  • Pieter Gaillard
    to-BBB technologies BV, Leiden, Netherlands
  • Footnotes
    Commercial Relationships Arie Reijerkerk, to-BBB technologies BV (E); Chantal Appeldoorn, to-BBB technologies BV (E); Jaap Rip, to-BBB technologies BV (E); Marco de Boer, to-BBB technologies BV (E); Pieter Gaillard, to-BBB technologies BV (E), to-BBB technologies BV (P)
  • Footnotes
    Support None
Investigative Ophthalmology & Visual Science April 2014, Vol.55, 2859. doi:
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      Arie Reijerkerk, Chantal C Appeldoorn, Jaap Rip, Marco de Boer, Pieter Gaillard; Systemic treatment with glutathione PEGylated liposomal methylprednisolone (2B3-201) improves therapeutic efficacy in a model of ocular inflammation. Invest. Ophthalmol. Vis. Sci. 2014;55(13):2859.

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      © ARVO (1962-2015); The Authors (2016-present)

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Purpose: Ocular inflammation is associated with the loss of visual acuity and subsequent blindness. Since their development, glucocorticoids have been the mainstay of therapy for ocular inflammatory diseases. However, the clinical benefit is limited by side effects due to the chronic use and generally high dosage, which is required for effective treatment. We have developed the G-Technology® to provide a means for sustained drug delivery, increased drug half-life, and reduced bodily drug exposure. 2B3-201, glutathione PEGylated liposomal methylprednisolone, has been developed as treatment for neuroinflammatory conditions and was evaluated in ocular inflammation.

Methods: The efficacy of 2B3-201 was investigated in rats with experimental autoimmune uveitis (EAU). Rats received 10 mg/kg of 2B3-201 intravenously at disease onset and at peak of the disease. The same dose of free methylprednisolone served as control treatment. Clinical signs of ocular inflammation were assessed by slit lamp and immunohistochemistry.

Results: Whereas free methylprednisolone was ineffective, two doses of 2B3-201 almost completely abolished clinical signs of EAU. This was further corroborated by immunohistochemical analyses of isolated eyes. 2B3-201 significantly reduced the infiltration of inflammatory cells and subsequent destruction of the retina cell layers.

Conclusions: In this study we are the first to show that systemic treatment with 2B3-201, a glutathione PEGylated liposomal methylprednisolone formulation, resulted in a superior efficacy in rats with EAU. Altogether, our findings hold promise for the development of a safe and more convenient systemic treatment for uveitis.

Keywords: 746 uveitis-clinical/animal model • 487 corticosteroids • 557 inflammation  

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