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Efficacy of Loteprednol Etabonate Drug Delivery System in Suppression of in vitro Retinal Pigment Epithelium Activation

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Choroidal neovascularization (CNV) is the growth of abnormal blood vessels in the choroid layer of the eye; it is a pathophysiological characteristic of wet age-related macular degeneration (AMD). Current clinical treatment utilizes frequent intravitreal injections, which can result in retinal detachment and increased ocular pressure. The purpose of the current study is to develop a novel drug delivery system of loteprednol etabonateencapsulated PEGylated PLGA nanoparticles incorporated into the PLGA-PEG-PLGA thermoreversible gel for treatment of AMD. The proposed drug delivery system was characterized for drug release, cytotoxicity studies and vascular endothelial growth factor (VEGF) suppression efficacy studies using ARPE-19 cells. The nanoparticles showed uniform size distribution with mean size of 168.60±23.18 nm and exhibited sustained drug release. Additionally, the proposed drug delivery system was non-cytotoxic to ARPE-19 cells and significantly reduced VEGF expression as compared to loteprednol etabonate solution. These results suggest the proposed drug delivery system can be used for further work in an animal model of experimental AMD with reduced intravitreal administration frequency.

Keywords: Choroidal neovascularization; PLGA nanoparticles; VEGF; loteprednol etabonate; thermoreversible gel

Document Type: Research Article

Publication date: December 1, 2014

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  • Pharmaceutical Nanotechnology publishes original manuscripts, reviews, thematic issues, rapid technical notes and commentaries that provide insights into the synthesis, characterisation and pharmaceutical (or diagnostic) application of materials at the nanoscale. The nanoscale is defined as a size range of below 1 µm. Scientific findings related to micro and macro systems with functionality residing within features defined at the nanoscale are also within the scope of the journal. Manuscripts detailing the synthesis, exhaustive characterisation, biological evaluation, clinical testing and/ or toxicological assessment of nanomaterials are of particular interest to the journal’s readership. Articles should be self contained, centred around a well founded hypothesis and should aim to showcase the pharmaceutical/ diagnostic implications of the nanotechnology approach. Manuscripts should aim, wherever possible, to demonstrate the in vivo impact of any nanotechnological intervention. As reducing a material to the nanoscale is capable of fundamentally altering the material’s properties, the journal’s readership is particularly interested in new characterisation techniques and the advanced properties that originate from this size reduction. Both bottom up and top down approaches to the realisation of nanomaterials lie within the scope of the journal.
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