Format

Send to

Choose Destination
Drug Deliv. 2019 Dec;26(1):237-243. doi: 10.1080/10717544.2019.1574936.

Novel ophthalmic formulation of myriocin: implications in retinitis pigmentosa.

Author information

1
a Department of Biomedical and Biotechnological Sciences, School of Medicine , University of Catania , Catania , Italy.
2
b Department of Health Sciences , University of Milano , Milano , Italy.
3
c Drug Sciences Department , University of Catania , Catania , Italy.
4
d NANO-i - Research Center on Ocular Nanotechnology University of Catania , Catania , Italy.
5
e CNR Neuroscience Institute , Pisa , Italy.
6
f Center for Research in Ocular Pharmacology-CERFO, University of Catania , Catania , Italy.

Abstract

Myriocin is an antibiotic derived from Mycelia sterilia, and is a potent inhibitor of serine palmitoyltransferase, the enzyme involved in the first step of sphingosine synthesis. Myriocin, inhibiting ceramide synthesis, has a great potential for treatment of diseases characterized by high ceramide levels in affected tissues, such as retinitis pigmentosa (RP). Drug delivery to the retina is a challenging task, which is generally by-passed through intravitreal injection, that represents a risky invasive procedure. We, therefore, developed and characterized an ophthalmic topical nanotechnological formulation based on a nanostructured lipid carrier (NLC) and containing myriocin. The ocular distribution of myriocin in the back of the eye was assessed both in rabbits and mice using LC-MS/MS. Moreover, rabbit retinal sphingolipid and ceramides levels, after myriocin-NLC (Myr-NLC) eye drops treatment, were assessed. The results demonstrated that Myr-NLC formulation is well tolerated and provided effective levels of myriocin in the back of the eye both in rabbits and mice. We found that Myr-NLC eye drops treatment was able to significantly decrease retinal sphingolipid levels. In conclusion, these data suggest that the Myr-NLC ophthalmic formulation is suitable for pharmaceutical development and warrants further clinical evaluation of this eye drops for the treatment of RP.

KEYWORDS:

Nanostructured lipid carriers; myriocin; ocular drug delivery; retinitis pigmentosa

PMID:
30883241
PMCID:
PMC6419690
DOI:
10.1080/10717544.2019.1574936
[Indexed for MEDLINE]
Free PMC Article

Supplemental Content

Full text links

Icon for Taylor & Francis Icon for PubMed Central
Loading ...
Support Center