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Binapani Mahaling, Dhirendra Katti; Design of a Non-Invasive Core-shell Nanoparticulate Drug Delivery System for Posterior Part of the Eye. Invest. Ophthalmol. Vis. Sci. 2013;54(15):5050.
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Providing drug molecules to the posterior part of the eye in therapeutic concentration and for adequate durations is difficult because of barrier properties of different layers of the eye. The differential permeability towards hydrophilic or hydrophobic molecules and surface charge of different layers of the eye further complicates the matter. Hence, the purpose of this study was to develop a noninvasive core-shell nanoparticle-based drug delivery system for targeting the posterior part of the eye. It was hypothesized that a nanoparticulate system with a hydrophobic core and a hydrophilic shell can potentially overcome the barriers due to the preferential permeability of hydrophilic molecules in the outer and hydrophobic molecules in the inner layers of the eye.
Nanoparticle cores of poly(lactic acid) (PLA) were coated with a chitosan (CHI) shell. CHI was chosen due to hydrophilic nature and its potential to overcome the tear fluid barrier because of its positive charge, bioadhesive and permeability enhancing properties. PLA and coumarin loaded PLA nanoparticles were synthesized by emulsion solvent evaporation method and modified with chitosan by adsorption followed by chemical crosslinking. Coumarin loaded PLA and PLA-CHI formulations were administered as eye drops onto the eye of C57BL/6J mice with PBS, PLA and PLA-CHI nanoparticles as controls. At predetermined time points mice were euthanized. The eyes were then enucleated, fixed, sectioned and analyzed under a fluorescence microscope.
Fluorescence was detected in coumarin loaded PLA and PLA-CHI particles in retina indicating the penetration of nanoparticles across the layers up to the retina, whereas, the control groups showed no fluorescence in retina. The levels of fluorescence observed for PLA-CHI core-shell nanoparticles was higher than that of PLA nanoparticles at the retina indicating the possible role of PLA-CHI in enhancing penetration.
These results suggest that PLA-CHI core-shell nanoparticles show potential to be developed as a non-invasive drug delivery system for posterior part of the eye.
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