July 2018
Volume 59, Issue 9
Open Access
ARVO Annual Meeting Abstract  |   July 2018
Sustained Release, Biodegradable PEA Implants for Intravitreal Delivery of the ROCK/PKC Inhibitor AR-13503
Author Affiliations & Notes
  • Angela Glendenning
    Aerie Pharmaceuticals, Durham, North Carolina, United States
  • Karen Crews
    Aerie Pharmaceuticals, Durham, North Carolina, United States
  • Jill Sturdivant
    Aerie Pharmaceuticals, Durham, North Carolina, United States
  • Mitchell A deLong
    Aerie Pharmaceuticals, Durham, North Carolina, United States
  • Casey Kopczynski
    Aerie Pharmaceuticals, Durham, North Carolina, United States
  • Cheng-Wen Lin
    Aerie Pharmaceuticals, Durham, North Carolina, United States
  • Footnotes
    Commercial Relationships   Angela Glendenning, Aerie Pharmaceuticals (E); Karen Crews, Aerie Pharmaceuticals (E); Jill Sturdivant, Aerie Pharmaceuticals (E); Mitchell deLong, Aerie Pharmaceuticals (E); Casey Kopczynski, Aerie Pharmaceuticals (E); Cheng-Wen Lin, Aerie Pharmaceuticals (E)
  • Footnotes
    Support  None
Investigative Ophthalmology & Visual Science July 2018, Vol.59, 5672. doi:
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      Angela Glendenning, Karen Crews, Jill Sturdivant, Mitchell A deLong, Casey Kopczynski, Cheng-Wen Lin; Sustained Release, Biodegradable PEA Implants for Intravitreal Delivery of the ROCK/PKC Inhibitor AR-13503. Invest. Ophthalmol. Vis. Sci. 2018;59(9):5672.

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

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Abstract

Purpose : Aerie has developed a library of kinase inhibitors for the treatment of ocular and other diseases. AR-13503 is a potent Rho kinase (ROCK) and protein kinase C (PKC) inhibitor under development for the treatment of diabetic macular edema (DME) and neovascular age-related macular degeneration (nAMD). Its physicochemical and pharmacological properties are well suited for posterior segment diseases. The purpose of this work was to identify a compatible sustained release technology that provides a 4 to 6 month duration of drug release following intravitreal injection.

Methods : AR-13503 was incorporated with various biodegradable poly-lactic-co-glycolic acid (PLGA) and polyester amide (PEA) polymers. PLGA/AR-13503 implants were manufactured by PRINT® technology. PEA/AR-13503 implants were manufactured by solvent casting and injection molding. Both PLGA/AR-13503 and PEA/AR-13503 implants were manufactured to dimensions compatible with injection through a 27-gauge needle. In vitro drug release and chemical stabilities were assessed at pH 7.4 at 37°C and analyzed by HPLC.

Results : PLGA polymers were chemically incompatible with AR-13503, whereas the PEA polymer showed excellent compatibility with AR-13503. PEA polymer implants containing AR-13503 provided a zero-order sustained drug release with minimal initial burst on Day 1 (<2%). Linear drug release was sustained in vitro for over 100 days.

Conclusions : Aerie developed a biodegradable implant for AR-13503 using a novel PEA polymer that provides sustained drug release for more than 100 days. These results support further development of the AR-13503 PEA implant for the treatment of DME and nAMD.

This is an abstract that was submitted for the 2018 ARVO Annual Meeting, held in Honolulu, Hawaii, April 29 - May 3, 2018.

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