Ocular Delivery of PACAP1-27 Protects the Retina From Ischemic Damage in Rodents

Invest Ophthalmol Vis Sci. 2016 Dec 1;57(15):6683-6691. doi: 10.1167/iovs.16-20630.

Abstract

Purpose: Pituitary adenylate cyclase activating polypeptide (PACAP) is neuroprotective in neuronal injuries. Bilateral common carotid artery occlusion (BCCAO) causes chronic hypoperfusion-induced degeneration in the rat retina, where we proved the retinoprotective effect of intravitreal PACAP. Although this route of administration is a common clinical practice in several diseases, easier routes are clinically important. Our aim was to investigate the potential retinoprotective effects of PACAP eye drops in BCCAO-induced ischemic retinopathy.

Methods: After performing BCCAO in rats, the right eyes were treated with PACAP1-27 eye drops (1 μg/drop, 2 × 1 drops/day for 5 days), containing different vehicles: saline, water for injections, thiomersal or benzalkonium solution for ophthalmic use (SOCB). Histology and immunohistochemistry were performed 2 weeks after surgery, while molecular analysis was performed 24 hours after BCCAO. Passage of PACAP1-27 through the ocular layers was tested with radioactive PACAP-SOCB in mice.

Results: Bilateral common carotid artery occlusion led to a severe degeneration of all retinal layers. Solution for ophthalmic use was the most effective vehicle for delivering PACAP (PACAP-SOCB), significantly ameliorating BCCAO-induced damage. The massive upregulation of GFAP was not observed in retinas treated with PACAP-SOCB eye drops. PACAP-SOCB treatment also increased activation of the protective Akt and ERK1/2 in hypoperfused retinas. The cytokine profile showing upregulation in different cytokines was attenuated by PACAP-SOCB. Radioactive PACAP reached the retina when delivered in SOCB-containing eye drops.

Conclusions: PACAP1-27, delivered in the SOCB vehicle as eye drops, was retinoprotective in ischemic retinopathy, providing the basis for future therapeutic administration.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Animals
  • Blotting, Western
  • Cytokines / metabolism
  • Disease Models, Animal
  • Dose-Response Relationship, Drug
  • Ependymoglial Cells / pathology
  • Immunohistochemistry
  • Ischemia / complications*
  • Ischemia / diagnosis
  • Ischemia / drug therapy
  • Male
  • Mice
  • Neurotransmitter Agents / administration & dosage
  • Ophthalmic Solutions
  • Pituitary Adenylate Cyclase-Activating Polypeptide / administration & dosage*
  • Rats
  • Rats, Wistar
  • Retina / drug effects*
  • Retina / pathology
  • Retinal Degeneration / diagnosis
  • Retinal Degeneration / etiology
  • Retinal Degeneration / prevention & control*
  • Retinal Vessels / drug effects
  • Retinal Vessels / pathology*

Substances

  • Cytokines
  • Neurotransmitter Agents
  • Ophthalmic Solutions
  • Pituitary Adenylate Cyclase-Activating Polypeptide