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

Novel ophthalmic formulation of myriocin: implications in retinitis pigmentosa

Chiara Bianca Maria Platania  1 , Michele Dei Cas  2 , Simona Cianciolo  3 , Annamaria Fidilio  1 , Francesca Lazzara  1 , Rita Paroni  2 , Rosario Pignatello  3   4 , Enrica Strettoi  5 , Riccardo Ghidoni  2 , Filippo Drago  1   6 , Claudio Bucolo  1   6
Affiliations

Novel ophthalmic formulation of myriocin: implications in retinitis pigmentosa

Chiara Bianca Maria Platania et al. Drug Deliv. 2019 Dec.

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.

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Figures

Figure 1.
Figure 1.
Myriocin (topically administered as a myriocin-NLC) distribution in rabbit vitreous and retina. *p < .05 mouse retina vs. rabbit vitreous and retina. **p < .05 rabbit vitreous vs. rabbit retina.
Figure 2.
Figure 2.
Ceramides (A) and dihydroceramides (B) levels in the retina after topical administration of the myriocin-NLC. Ceramide or dihydroceramide range in control animals is represented by two dotted lines. *p < .05 **p < .001 Myr-NLC rabbits vs. vehicle-treated group.
See this image and copyright information in PMC

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