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.
Novel ophthalmic formulation of myriocin: implications in retinitis pigmentosa / C.B.M. Platania, M. Dei Cas, S. Cianciolo, A. Fidilio, F. Lazzara, R. Paroni, R. Pignatello, E. Strettoi, R. Ghidoni, F. Drago, C. Bucolo. - In: DRUG DELIVERY. - ISSN 1071-7544. - 26:1(2019), pp. 237-243.
|Titolo:||Novel ophthalmic formulation of myriocin: implications in retinitis pigmentosa|
DEI CAS, MICHELE VITTORIO (Co-primo) [Writing – Review & Editing]
PARONI, RITA CLARA [Writing – Review & Editing]
GHIDONI, RICCARDO [Supervision]
|Parole Chiave:||myriocin; Nanostructured lipid carriers; ocular drug delivery; retinitis pigmentosa; 3003|
|Settore Scientifico Disciplinare:||Settore BIO/10 - Biochimica|
Settore BIO/12 - Biochimica Clinica e Biologia Molecolare Clinica
|Data di pubblicazione:||2019|
|Digital Object Identifier (DOI):||http://dx.doi.org/10.1080/10717544.2019.1574936|
|Appare nelle tipologie:||01 - Articolo su periodico|
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