title: Release profile and transscleral permeation of triamcinolone acetonide loaded nanostructured lipid carriers (TA-NLC): in vitro and ex vivo studies.
abstract: 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.
authors: Department of Physical Chemistry, Faculty of Pharmacy, University of Barcelona, Barcelona, Spain.
authors: Joana
authors: J
authors: Araújo
authors: Maria L
authors: ML
authors: Garcia
authors: Mireia
authors: M
authors: Mallandrich
authors: Eliana B
authors: EB
authors: Souto
authors: Ana C
authors: AC
authors: Calpena
mesh_terms: D000818:Animals; D003692:Delayed-Action Preparations / Q000008:administration & dosage / Q000737:chemistry*; D007166:Immunosuppressive Agents / Q000008:administration & dosage / Q000493:pharmacokinetics; D066298:In Vitro Techniques; D008055:Lipids / Q000737:chemistry*; D008081:Liposomes / Q000737:chemistry; D053769:Nanocapsules / Q000008:administration & dosage / Q000737:chemistry*; D049329:Nanostructures / Q000737:chemistry* / Q000648:ultrastructure; D010539:Permeability; D011817:Rabbits; D012590:Sclera / Q000737:chemistry / Q000378:metabolism*; D014222:Triamcinolone Acetonide / Q000008:administration & dosage* / Q000493:pharmacokinetics*
chemical_list: D003692:Delayed-Action Preparations; D007166:Immunosuppressive Agents; D008055:Lipids; D008081:Liposomes; D053769:Nanocapsules; D014222:Triamcinolone Acetonide