期刊
DRUG DELIVERY
卷 26, 期 1, 页码 237-243出版社
TAYLOR & FRANCIS LTD
DOI: 10.1080/10717544.2019.1574936
关键词
Nanostructured lipid carriers; ocular drug delivery; myriocin; retinitis pigmentosa
资金
- Piano Triennale per la Ricerca - Linea Intervento 2, University of Catania, Italy
- Research Center Aldo Ravelli, University of Milan
- PhD program in Molecular and Translational Medicine of the University of Milan, Italy
- Fondazione Roma
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.
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