LAUSR

Abstract The aim of this work was to study the preparation process and the in vitro release of human serum albumin nanoparticles stabilized by Gantrez® ES-425, which was loaded with antiangiogenic drugs (suramin and bevacizumab). Nanoparticles were prepared by coacervation and stabilized with Gantrez®ES-425(Nps-Ga). As control, albumin nanoparticles cross-linked with glutaraldehyde (Nps-Glu) were prepared. Nps-Ga displayed a mean size of about 210 nm whereas Nps-Glu showed a mean size of 158 nm. For suramin-loaded nanoparticles, the stabilization process did not show any significant effect on the drug with neither glutaraldehyde nor Gantrez®. On the contrary, for bevacizumab, only nanoparticles stabilized with Gantrez® displayed important payloads (97 μg/mg nanoparticle) of the active form of the antibody. For nanoparticles with glutaraldehyde, only a very low amount of the loaded bevacizumab remained active. Regarding the in vitro release studies, suramin showed a release mechanism influenced by the type of stabilizing agent. Finally, bevacizumab released from Nps-Ga was characterized by a small burst effect followed by a sustained release rate. In summary, albumin nanoparticles stabilized by polymer coating were successfully obtained and are a promising delivery system for the topical treatment of CNV.