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Esculentin 1a derivatives thereof for treatment of microbial keratitis

Anti-infective agentsAntimicrobial peptidesKeratitisNew ophthalmic agentsOcular surface infections

Introduction

The present invention provides for the use of synthetic antimicrobial peptides (AMPs) deriving from the esculentin 1a peptide from frog skin, against ocular infections, directed to their formulation for the topical treatment and prevention of microbial keratitis, a serious infection of the cornea especially in contact lens wearers.

Technical features

The esculentin 1a peptide and its derivatives represent new molecules for the treatment / prevention of microbial keratitis. Thanks to their mechanism of action, these peptides reduce the risk of inducing microbial resistance. Unlike traditional antibiotics, they are active against bacteria, fungi, protozoa and are also immunomodulators. A representative example of the treatment of keratitis includes the use of a peptide solution to be applied locally as eye drops or to be conveyed through the use of nanoparticles or therapeutic contact lenses to allow a prolonged release of peptide over time on the ocular surface and prevent the adhesion of pathogens on the surface of the latter and therefore their transfer to the eye, thus stopping the appearance of infection. The patent is in a preclinical phase: experiments with animal models with keratitis and for the use of antimicrobial contact lenses.

Possible Applications

  • Treatment of microbial keratitis;
  • Restoration of the integrity of the cornea, applied in the form of eye drops or encapsulated in nanoparticles;
  • Encapsulation in a pharmaceutically acceptable “carrier” (for the treatment of keratitis);
  • Covalent conjugation to contact lenses (for the prevention of eye infection).

Advantages

  • Active peptides against bacteria, fungi, protozoa and microbial resistance;
  • Immobilizable peptides on the surface of the contact lens;
  • Reduction of possible infections.