Sorbitan ester nanoparticles (SENS) as a novel topical ocular drug delivery system: Design, optimization, and in vitro/ex vivo evaluation

International Journal of Pharmaceutics
Jesus Alvarez-TrabadoA Sanchez

Abstract

We explored the potential of two types of sorbitan ester nanoparticles (SENS) as novel tools for topical ocular drug delivery. The optimized SENS formulation (SENS-OPT) consisted of nanoparticles (NPs) of 170.5 nm, zeta potential +33.9 mV, and cyclosporine loading of 19.66%. After hyaluronic acid (HA) coating, the resulting SENS-OPT-HA NPs had a particle size of 177.6 nm and zeta potential of -20.6 mV. The NPs were stable during 3 months of storage at different temperatures and did not aggregate in the presence of protein-enriched simulated lacrimal fluid. There was no toxicity to cultured human corneal epithelial (HCE) cells when exposed to NPs up to 0.4% (w/v). Both NPs were effectively internalized by HCE cells through active mechanisms. Endocytosis of SENS-OPT NPs was caveolin-dependent whereas SENS-OPT-HA NP endocytosis was mediated by HA receptors. HA-receptor-mediated endocytosis may be responsible for the higher cellular uptake of SENS-OPT-HA NPs. After cyclosporine incorporation into the NPs, corneal penetration of this immunosuppressive drug by loaded SENS-OPT NPs was 1.3-fold higher than the commercial reference formulation Sandimmun®. For cyclosporine-loaded SENS-OPT-HA NPs, the penetration was 2.1-fold higher than ...Continue Reading

Citations

Aug 13, 2020·Drug Delivery and Translational Research·Xuefei LiXianggen Wu
Aug 30, 2019·Nanomaterials·Abderrazzaq EssaghraouiSalette Reis
Apr 30, 2021·Carbohydrate Polymers·Xiaodan ZhangQiang Zhu
Jun 23, 2021·Tissue Engineering. Part B, Reviews·Adél HinsenkampIstván Hornyák
Jul 12, 2021·International Journal of Pharmaceutics·Beatriz SilvaLídia Gonçalves

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