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Novel ophthalmic formulation of myriocin: implications in retinitis pigmentosa.
- Source :
-
Drug delivery [Drug Deliv] 2019 Dec; Vol. 26 (1), pp. 237-243. - Publication Year :
- 2019
-
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.
- Subjects :
- Animals
Ceramides metabolism
Chemistry, Pharmaceutical methods
Drug Carriers chemistry
Drug Delivery Systems methods
Fatty Acids, Monounsaturated chemistry
Lipids chemistry
Mice
Nanostructures chemistry
Ophthalmic Solutions chemistry
Rabbits
Retina metabolism
Retinitis Pigmentosa metabolism
Serine C-Palmitoyltransferase metabolism
Sphingolipids metabolism
Fatty Acids, Monounsaturated pharmacology
Ophthalmic Solutions pharmacology
Retina drug effects
Retinitis Pigmentosa drug therapy
Subjects
Details
- Language :
- English
- ISSN :
- 1521-0464
- Volume :
- 26
- Issue :
- 1
- Database :
- MEDLINE
- Journal :
- Drug delivery
- Publication Type :
- Academic Journal
- Accession number :
- 30883241
- Full Text :
- https://doi.org/10.1080/10717544.2019.1574936