RT info:eu-repo/semantics/article
T1 Sorbitan ester nanoparticles (SENS) as a novel topical ocular drug delivery system: Design, optimization, and in vitro/ex vivo evaluation
A1 Álvarez Trabado, Jesús
A1 López García, Antonio
A1 Martín Pastor, Manuel
A1 Diebold Luque, María Yolanda
A1 Sánchez, Alejandro
K1 Oftalmología
K1 Pharmacology
K1 Ocular
K1 Cyclosporine
K1 Nanoparticles
K1 Ciclosporina
K1 Nanopartículas
K1 3201.09 Oftalmología
AB 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 for Sandimmun®. In ex vivo stimulated lymphocytes, both formulations demonstrated the same reduction in IL-2 levels as Sandimmun®
PB Elsevier
SN 0378-5173
YR 2018
FD 2018
LK https://uvadoc.uva.es/handle/10324/64867
UL https://uvadoc.uva.es/handle/10324/64867
LA eng
NO International Journal of Pharmaceutics, 2018, vol. 546, issues 1–2, p. 20-30
NO Producción Científica
DS UVaDOC
RD 07-ago-2024