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A New Bevacizumab Carrier for Intravitreal Administration: Focus on Stability

Bevacizumab (BVZ) is a monoclonal antibody that binds to human vascular endothelial growth factor A (VEGF-A) and inhibits the interaction between VEGF-A and VEGF receptors, thus blocking the angiogenesis. Repeated intravitreal injections of BVZ for the treatment of ocular pathologies that present an...

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Autores principales: Chirio, Daniela, Peira, Elena, Sapino, Simona, Chindamo, Giulia, Oliaro-Bosso, Simonetta, Adinolfi, Salvatore, Dianzani, Chiara, Baratta, Francesca, Gallarate, Marina
Formato: Online Artículo Texto
Lenguaje:English
Publicado: MDPI 2021
Materias:
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC8071554/
https://www.ncbi.nlm.nih.gov/pubmed/33921167
http://dx.doi.org/10.3390/pharmaceutics13040560
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author Chirio, Daniela
Peira, Elena
Sapino, Simona
Chindamo, Giulia
Oliaro-Bosso, Simonetta
Adinolfi, Salvatore
Dianzani, Chiara
Baratta, Francesca
Gallarate, Marina
author_facet Chirio, Daniela
Peira, Elena
Sapino, Simona
Chindamo, Giulia
Oliaro-Bosso, Simonetta
Adinolfi, Salvatore
Dianzani, Chiara
Baratta, Francesca
Gallarate, Marina
author_sort Chirio, Daniela
collection PubMed
description Bevacizumab (BVZ) is a monoclonal antibody that binds to human vascular endothelial growth factor A (VEGF-A) and inhibits the interaction between VEGF-A and VEGF receptors, thus blocking the angiogenesis. Repeated intravitreal injections of BVZ for the treatment of ocular pathologies that present an excessive proliferation results in a low patience compliance. BVZ is specially indicated for the treatment of diabetic and degenerative retinopathy. In the present study, we designed lipid nanoparticles (NPs) as a BVZ sustained drug delivery system for reducing the frequency of administration. We used a simple and highly efficient procedure, “Cold dilution of microemulsions”, to obtain spherical NPs with mean diameters of 280–430 nm, Zeta potentials between −17 and −31 mV, and drug entrapment efficiencies between 50 to 90%. This study focused on the biochemical and biophysical stabilities of BVZ after entrapment in NPs. SDS-PAGE electrophoretic analysis and circular dichroism, dynamic light scattering, and scanning electron microscopy were used to characterize BVZ-loaded NPs. The biocompatibility was assessed by in vitro cell compatibility studies using the ARPE-19 cell line. Thus, in this work, a stable BVZ-loaded system was obtained. In addition, several studies have shown that BVZ is released slowly from the lipid matrix and that this system is biocompatible. The results are promising and the developed NPs could be exploited to create a new, potentially effective and minimally invasive treatment of intraocular diseases.
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spelling pubmed-80715542021-04-26 A New Bevacizumab Carrier for Intravitreal Administration: Focus on Stability Chirio, Daniela Peira, Elena Sapino, Simona Chindamo, Giulia Oliaro-Bosso, Simonetta Adinolfi, Salvatore Dianzani, Chiara Baratta, Francesca Gallarate, Marina Pharmaceutics Article Bevacizumab (BVZ) is a monoclonal antibody that binds to human vascular endothelial growth factor A (VEGF-A) and inhibits the interaction between VEGF-A and VEGF receptors, thus blocking the angiogenesis. Repeated intravitreal injections of BVZ for the treatment of ocular pathologies that present an excessive proliferation results in a low patience compliance. BVZ is specially indicated for the treatment of diabetic and degenerative retinopathy. In the present study, we designed lipid nanoparticles (NPs) as a BVZ sustained drug delivery system for reducing the frequency of administration. We used a simple and highly efficient procedure, “Cold dilution of microemulsions”, to obtain spherical NPs with mean diameters of 280–430 nm, Zeta potentials between −17 and −31 mV, and drug entrapment efficiencies between 50 to 90%. This study focused on the biochemical and biophysical stabilities of BVZ after entrapment in NPs. SDS-PAGE electrophoretic analysis and circular dichroism, dynamic light scattering, and scanning electron microscopy were used to characterize BVZ-loaded NPs. The biocompatibility was assessed by in vitro cell compatibility studies using the ARPE-19 cell line. Thus, in this work, a stable BVZ-loaded system was obtained. In addition, several studies have shown that BVZ is released slowly from the lipid matrix and that this system is biocompatible. The results are promising and the developed NPs could be exploited to create a new, potentially effective and minimally invasive treatment of intraocular diseases. MDPI 2021-04-15 /pmc/articles/PMC8071554/ /pubmed/33921167 http://dx.doi.org/10.3390/pharmaceutics13040560 Text en © 2021 by the authors. https://creativecommons.org/licenses/by/4.0/Licensee MDPI, Basel, Switzerland. This article is an open access article distributed under the terms and conditions of the Creative Commons Attribution (CC BY) license (https://creativecommons.org/licenses/by/4.0/).
spellingShingle Article
Chirio, Daniela
Peira, Elena
Sapino, Simona
Chindamo, Giulia
Oliaro-Bosso, Simonetta
Adinolfi, Salvatore
Dianzani, Chiara
Baratta, Francesca
Gallarate, Marina
A New Bevacizumab Carrier for Intravitreal Administration: Focus on Stability
title A New Bevacizumab Carrier for Intravitreal Administration: Focus on Stability
title_full A New Bevacizumab Carrier for Intravitreal Administration: Focus on Stability
title_fullStr A New Bevacizumab Carrier for Intravitreal Administration: Focus on Stability
title_full_unstemmed A New Bevacizumab Carrier for Intravitreal Administration: Focus on Stability
title_short A New Bevacizumab Carrier for Intravitreal Administration: Focus on Stability
title_sort new bevacizumab carrier for intravitreal administration: focus on stability
topic Article
url https://www.ncbi.nlm.nih.gov/pmc/articles/PMC8071554/
https://www.ncbi.nlm.nih.gov/pubmed/33921167
http://dx.doi.org/10.3390/pharmaceutics13040560
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