
This study reports on L-carnosine phytosomes as an alternative for the prodrug N-acetyl-L-carnosine as a novel delivery system to the lens. L-carnosine was loaded into lipid-based phytosomes and hyaluronic acid (HA)-dispersed phytosomes. L-carnosine-phospholipid complexes (PC) of different molar ratios, 1:1 and 1:2, were prepared by the solvent evaporation method. These complexes were characterized with thermal and spectral analyses. PC were dispersed in either phosphate buffered saline pH 7.4 or HA (0.1% w/v) in phosphate buffered saline to form phytosomes PC1:1, PC1:2, and PC1:2 HA, respectively. These phytosomal formulations were studied for size, zeta potential, morphology, contact angle, spreading coefficient, viscosity, ex vivo transcorneal permeation, and cytotoxicity using primary human corneal cells. L-carnosine-phospholipid formed a complex at a 1:2 molar ratio and phytosomes were in the size range of 380-450 nm, polydispersity index of 0.12-0.2. The viscosity of PC1:2 HA increased by 2.4 to 5-fold compared with HA solution and PC 1:2, respectively; significantly lower surface tension, contact angle, and greater spreading ability for phytosomes were also recorded. Ex vivo transcorneal permeation parameters showed significantly controlled corneal permeation of L-carnosine with the novel carrier systems without any significant impact on primary human corneal cell viability. Ex vivo porcine lenses incubated in high sugar media without and with L-carnosine showed concentration-dependent marked inhibition of lens brunescence indicative of the potential for delaying changes that underlie cataractogenesis that may be linked to diabetic processes.
pharmacy, Medicine (General), Phytosomes, Cell Survival, Static Electricity, Sus scrofa, Carbohydrates, Hyaluronate sodium, chemistry, Eye, Permeability, Ocular delivery, R5-920, Drug Delivery Systems, X-Ray Diffraction, International Journal of Nanomedicine, Lens, Crystalline, Spectroscopy, Fourier Transform Infrared, Animals, Humans, Surface Tension, Hyaluronic Acid, Particle Size, Original Research, Lipoid S 75, L-carnosine, Calorimetry, Differential Scanning, Viscosity, Carnosine, cataract, Liposomes, Solvents
pharmacy, Medicine (General), Phytosomes, Cell Survival, Static Electricity, Sus scrofa, Carbohydrates, Hyaluronate sodium, chemistry, Eye, Permeability, Ocular delivery, R5-920, Drug Delivery Systems, X-Ray Diffraction, International Journal of Nanomedicine, Lens, Crystalline, Spectroscopy, Fourier Transform Infrared, Animals, Humans, Surface Tension, Hyaluronic Acid, Particle Size, Original Research, Lipoid S 75, L-carnosine, Calorimetry, Differential Scanning, Viscosity, Carnosine, cataract, Liposomes, Solvents
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