ABSTRACT

The objective of the study was to investigate the biodistribution behavior of a fluorescent marker encapsulated in polymeric colloidal nanoparticulate system comprised of PLGA [poly (lactide-co-glycolic acid)] and also to quantify the uptake of fluorescein sodium by brain following intra nasal administration of formulation in vivo. The PLGA nanoparticles were coupled with glutathione, an endogenous transporter, for improving the brain specific delivery of fluorescein sodium by exploring carbodiimide chemistry using EDAC [1-ethyl-3-(3-dimethylaminopropyl)carbodiimide] as linker. The optimized formulation was characterized for in vitro and ex vivo release of fluorescein sodium from the formulation. The mean particle diameter of optimized fluorescein sodium loaded PLGA nanoparticles was found to be 115.25 ± 6.8 and 141.63± 4.5 nm for glutathione conjugated PLGA nanoparticles. The results from in vitro, ex vivo and in vivo studies reveal the significant capability of glutathione in achieving successful brain delivery of PLGA nanoparticles.