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Jose A. Cardillo, Alessandro J. Dare, Acacio A. Lima Filho, Anselmo G. Oliveira, Rubens Belfort, Jr.; The Potential of Nanolipossomes-Encapsulated Bevacizumab (Avalong) in Prolong VEGF-Inhibition and Enhancing Choroidal Neovascularization -Targeting Following Intravitreal Injection. Invest. Ophthalmol. Vis. Sci. 2012;53(14):4637.
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To determine the potential of new and optimized bevacizumab-liposomal formulation to improve drug availability, bioactivity and vessels targeting after intravitreal administration.
Bevacizumab was encapsulated into liposomes via the dehydration-rehydration method tested in an animal model. Left eyes of rabbits received liposomal bevacizumab and the right eyes were injected with the conventional soluble formulation. The free drug concentration in aqueous humor and vitreous samples at Days 3, 7, 14, and 29 after the injection was determined by enzyme-linked immune sorbent assay. The comparative inhibitory efficiency of bevacizumab in both conventional and liposomal formulation was determined by analyzing the gene expression of VEGF in human fibroblast cell line. Electronic microscopy (EM) of the retina and electro retinography (ERG) was performed to rule out and potential side effect.
Mean concentration of free bevacizumab in the eyes receiving liposomal bevacizumab compared with the eyes injected with soluble bevacizumab was 7 (24.5 versus 3.5 microg/mL) times higher at Days 29. Mean concentration of free bevacizumab in the aqueous humor of both injected eyes was almost the same at the different intervals. The In vitro inhibitory efficiency of the liposomal-bezacizumab formulation was 6 times greater than the soluble Bevacizumab, possible to its higher cell targeting and affinity. No significant EM or ERG findings were observed.
Optimized pharmacokinetics and physicochemical properties obtained with Bevacizumab in a liposomal formulation, potentially enhancing the intravitreal half-life and its ability to interact with endothelial cells are important factors to consider for the treatment of Choroidal Neovascularization and other angiogenesis-dependent diseases of the eye.
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