Release profile and transscleral permeation of triamcinolone acetonide loaded nanostructured lipid carriers (TA-NLC): in vitro and ex vivo studies

Nanostructured lipid carriers (NLC) have been developed for sustained release of triamcinolone acetonide (TA), a corticosteroid commonly indicated for macular edema, neovascularization, and other ocular inflammatory disorders. TA-NLC were prepared by high-pressure homogenization and characterized for in vitro release by dialysis bag. Ex vivo permeation profile was assessed using rabbit sclera isolated and mounted in Franz diffusion cells. TA-NLC were placed in episcleral donor compartment and choroidal side was perfused with HEPES buffer. Tissue sections underwent drug wash-out, following analysis by validated RP-HPLC of drug content and perfused fractions collected over 24 hours. Drug release followed one-order kinetics and permeability studies confirmed that TA is able to diffuse across rabbit sclera in sustained profile, following zero-order kinetics. Strong tissue binding was observed, providing a drug depot. These findings are of potential use when designing future TA therapy strategies for ocular diseases of posterior segment.From the Clinical EditorIn this study of triamcinolone acetonide loaded nanosize lipid carriers, potential ophthalmological applications are investigated including its trans-scleral permeation and release profile. Future in vitro studies are anticipated to establish this novel lipid carrier as a future therapeutic option for ocular diseases of the posterior segment.

Graphical AbstractNanostructured Lipid Carriers (NLC) have been developed for sustained release of Triamcinolone Acetonide (TA), a corticosteroid commonly indicated for macular oedema, neovascularization and other ocular inflammatory conditions. Drug release from NLC followed one-order kinetics. Ex vivo permeability studies confirmed that TA is able to diffuse through rabbit sclera in a sustained profile, following a zero-order kinetic model. Strong tissue binding was observed, providing a drug depot.Figure optionsDownload high-quality image (92 K)Download as PowerPoint slide