ENTRAPMENT OF BETA-LACTAMS ANTIBIOTICS IN POLYETHYLCYANOACRYLATE NANOPARTICLES - STUDIES ON THE POSSIBLE IN-VIVO APPLICATION OF THIS COLLOIDAL DELIVERY SYSTEM

Polyethylcyanoacrylate (PECA) nanoparticles were prepared in the presence of three different non-ionic surfactants: Triton X-100, Tween 80 and Pluronic F68. The influence of the surfactant, employed during the nanoparticle preparation process, on drug loading, size and storage stability was evaluated. The amount of Cefaclor (CFR) and Cefsulodin (CFN) entrapped in the colloidal system was not influenced by the presence of the three different surfactants, achieving a mean loading value of about 1.6% (w/w). PECA nanoparticles prepared in the presence of Tween 80 and Pluronic F68 and entrapping the two drugs showed no dependence of the mean particle size on the various components present in the polymerization medium. Only the system obtained in the presence of Triton X-100 showed an increase in particle size compared to the nanoparticles prepared in the absence of the active compound. Storage at room temperature, as dried powder, caused a drastic increase in size and polydispersity index values of the PECA nanoparticles containing CFN or CFR. The PECA nanoparticle colloidal suspensions prepared in the presence of Pluronic F68 provided much greater values of the retention capability for CFN and CFR, followed by the systems prepared in the presence of Tween 80 and Triton X-100, respectively. For each nanoparticle formulation, the retention of CFR was higher than that of CFN. The permeability through a biological membrane model was greater for CFN loaded nanoparticles than for the free drug. In contrast, no noticeable difference was observed between free CFR and that loaded in PECA nanoparticles, prepared with Pluronic F68 or Triton X-100. Only the system prepared in the presence of Tween 80 showed a high diffusion rate of CFR compared to the free drug.