The entrapment of fluoroquinolones, perfloxacine mesilate (PFX) and ofloxacin (OFX),
in polyalkylcyanoacrylate (PECA) nanoparticles could offer some advantages for their
biological application; for examples, increasing their bioavailability, controlling
the drug time-release in blood, and reducing the formation of bacterial resistance.
To load these two drugs in PECA polymeric bulk, the incorporation or adsorption method
was performed. These two methods were capable of influencing nanoparticle size, molecular
weight, release profile, and drug-polymer association. The incorporation method, particularly
for the OFX system, achieved PECA nanoparticle suspensions with a mean size value
three times higher than that obtained in the absence of the drug. In contrast, negligible
changes were observed for PFX systems. This preparation process also influenced the
nanoparticle storage stability. The molecular weight values of the various nanoparticle
preparations were also influenced; that is, the PFX-loaded systems showed an enhancement
in the average molecular weight values, whereas a reduction was observed for OFX-loaded
systems. The adsorption method showed no particular difference in particle size, molecular
weight, and storage stability compared with nanoparticles prepared without the drugs.
The nanoparticle loading capacity was higher for the colloidal systems obtained following
the incorporation preparation procedure. The release of drug from the nanoparticles
was biphasic for both preparation processes. The fluoro-quinolone-loaded nanoparticles
showed an enhancement of the antimicrobial activity against standard bacteria strains
from 2- to 50-fold compared with the free drugs.