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Summary
Lipid DNA nanoparticles (NPs) exhibit an intrinsic affinity to the ocular surface and can be loaded by hybridization with fluorophore-DNA conjugates or with the anti-glaucoma drug travoprost by hybridizing an aptamer that binds the medication. In the travoprost-loaded NPs (Trav-NPs), the drug is bound by specific, non-covalent interactions, not requiring any chemical modification of the active pharmaceutical ingredient. Fluorescently labeled Trav-NPs show a long-lasting adherence to the eye, up to sixty minutes after eye drop instillation. Biosafety of the Trav-NPs was proved and in vivo. Quantification of ex vivo and in vivo travoprost delivery via LC–MS revealed that Trav-NPs enable delivery of at least twice the amount of the drug at every investigated time-point compared to pristine drug. The data successfully shows the applicability of a DNA-based drug delivery system in the field of ophthalmology for the treatment of a major retinal eye disease, i.e. glaucoma.
Graphical
Introducing hydrophobic chains at the nucleobase uracil enables the automated solid-phase synthesis of amphiphilic DNA strands, which self-assemble into spherical nano-objects. These Lipid DNA nanoparticles (NPs) exhibit an intrinsic affinity to the ocular surface and were loaded with the anti-glaucoma medication travoprost by hybridizing a specific aptamer that binds the drug. The NP were evaluated for adhesion, drug-uptake and biosafety with rats and mouse in vivo and ex vivo with porcine tissue. The NPs successfully delivered the drug to the ocular surface and revealed improved efficacy compared to the free drug.Download : Download high-res image (325KB)Download : Download full-size image
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Institution2; University of Groningen; RWTH Aachen University
