Article ID | Journal | Published Year | Pages | File Type |
---|---|---|---|---|
599676 | Colloids and Surfaces B: Biointerfaces | 2014 | 9 Pages |
•A new nanoparticulate system for foscarnet delivery was prepared and characterized.•Nanoparticles were obtained by ionotropic gelation of chitosan induced by foscarnet.•Nanoparticles were also further crosslinked by glutaraldehyde.•The stability of this system in phosphate buffer saline was determined.•Its in vitro antiviral activity against infected lung fibroblasts cells was investigated.
A new nanoparticulate system for foscarnet delivery was prepared and evaluated. Nanoparticles were obtained by ionotropic gelation of chitosan induced by foscarnet itself, acting as an ionotropic agent in a manner similar to tripolyphosphate anion. A Doehlert design allowed finding the suitable experimental conditions. Nanoparticles were between 200 and 300 nm in diameter (around 450 nm after redispersion). Nanoparticle size increased after 5 h, but no size increase was observed after 48 h when nanoparticles were crosslinked with glutaraldehyde. Zeta potential values of noncrosslinked and crosslinked nanoparticles were between 20 and 25 mV, while drug loading of noncrosslinked nanoparticles was about 40% w/w (55% w/w for crosslinked nanoparticles). Nanoparticle yield was around 25% w/w. Crosslinked nanoparticles showed a controlled drug release. Foscarnet released from nanoparticles maintained the antiviral activity of the free drug when tested in vitro against lung fibroblasts (HELF) cells infected with HCMV strain AD-169. Moreover, nanoparticles showed no toxicity on non-infected HELF cells. These nanoparticles may represent a delivery system that could improve the therapeutic effect of foscarnet.
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