Enhanced antiviral activity of acyclovir loaded into β-cyclodextrin-poly(4-acryloylmorpholine) conjugate nanoparticles

Novel polymeric nanoparticles based on a β-cyclodextrin-poly(4-acryloylmorpholine) monoconjugate (β-CD-PACM), a tadpole-shaped polymer in which the β-CD ring is the hydrophilic head and the PACM chain the amphiphilic tail, were prepd. by the solvent injection technique. Acyclovir-loaded nanoparticles were prepd. from inclusion complexes of Acyclovir with β-CD-PACM. Both unloaded and drug-loaded nanoparticles were characterized in terms of particle size distribution, morphol., zeta potential, drug loading and in vitro drug release rate. The antiviral activity of Acyclovir loaded into β-CD-PACM nanoparticles against two clin. isolates of HSV-1 was evaluated and found to be remarkably superior compared with that of both the free drug and a sol. β-CD-PACM complex reported in a previous paper. Fluorescent nanoparticles loaded with coumarin 6 were also prepd. in order to investigate the nanoparticle cell uptake by confocal laser microscopy. It was found that the nanoparticles are internalized in cells and locate in the perinuclear compartment.