Human serum albumin nanoparticles for ocular delivery of bevacizumab

LUIS DE REDÍN, INÉS; BOIERO, CAROLINA; MARTÍNEZ-OHÁRRIZ, MARÍA CRISTINA; AGÜEROS, MAITE; RAMOS, ROCÍO; PEÑUELAS, IVÁN; ALLEMANDI, DANIEL; LLABOT, JUAN M.; IRACHE, JUAN M.

INTERNATIONAL JOURNAL OF PHARMACEUTICS

ELSEVIER SCIENCE BV

Año: 2018 vol. 541 p. 214 - 214

0378-5173

evacizumab-loaded nanoparticles (B-NP) were prepared by a desolvation process followed by freeze-drying, without any chemical, physical or enzymatic cross-linkage. Compared with typical HSA nanoparticles crosslinked with glutaraldehyde (B-NP-GLU), B-NP displayed a significantly higher mean size (310 nm vs. 180 nm)and a lower negative zeta potential (−15 mV vs. −36 mV). On the contrary, B-NP displayed a high payload of approximately 13% when measured by a specific ELISA, whereas B-NP-GLU presented a very low bevacizumab loading (0.1 μg/mg). These results could be related to the inactivation of bevacizumab after reacting withglutaraldehyde. From B-NP, bevacizumab was released following an initial burst effect, proceeded by a continuous release of bevacizumab at a rate of 6 μg/h. Cytotoxicity studies in ARPE cells were carried out at a single dose up to 72 h and with repeated doses over a 5-day period. Neither bevacizumab nor B-NP altered cell viability even when re