Functional polymeric nanoparticles for dexamethasone loading and release

Poly(phenylacetylene) (PPA) and poly(phenylacetylene-co-acrylic acid) (P(PA-co-AA)), nanoparticles bioconjugated with dexamethasone (DXM) during the synthesis, named PPA@DXM and P(PA-co-AA)@DXM, were prepared by a modified surfactant free emulsion method. The loading was studied as a function of different functionality grades of the copolymer and different amounts of drug, obtaining up to 90% of drug loading for P(PA-co-AA)@DXM with 8/1 PA/AA monomer ratio. The SEM images and DLS measurements showed spheres with average diameters in the range 190-500nm, depending on the content of acrylic acid monomer units in the copolymer and of DXM loading ζ-potential and surface charge density of DXM loaded nanoparticles were also investigated and confirm the charge density modulation in the range 0.62-2.68σ (μC/m2). The results highlight the enhanced capability of our copolymer of hosting DXM, with the advantage of a control of size, surface functionality, charge and release. Moreover we demonstrate for the first time the ability of P(PA-co-AA) DXM loaded nanoparticles to be used in the apoptosis inhibition of human tumor cells (HeLa). On the basis of the results obtained by comparing the effects elicited in HeLa cells by free DXM versus DXM loaded nanoparticles we confirmed the biological efficacy of our preparation. © 2011 Elsevier B.V.