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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| Format: | Article |
| Language: | English |
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MDPI AG
2021-04-01
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| Series: | Pharmaceutics |
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| Online Access: | https://www.mdpi.com/1999-4923/13/4/560 |
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| author | Daniela Chirio Elena Peira Simona Sapino Giulia Chindamo Simonetta Oliaro-Bosso Salvatore Adinolfi Chiara Dianzani Francesca Baratta Marina Gallarate |
| author_facet | Daniela Chirio Elena Peira Simona Sapino Giulia Chindamo Simonetta Oliaro-Bosso Salvatore Adinolfi Chiara Dianzani Francesca Baratta Marina Gallarate |
| author_sort | Daniela Chirio |
| collection | DOAJ |
| 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. |
| first_indexed | 2024-03-10T12:17:16Z |
| format | Article |
| id | doaj.art-575ecb3c8dec468288dc4742b169c143 |
| institution | Directory Open Access Journal |
| issn | 1999-4923 |
| language | English |
| last_indexed | 2024-03-10T12:17:16Z |
| publishDate | 2021-04-01 |
| publisher | MDPI AG |
| record_format | Article |
| series | Pharmaceutics |
| spelling | doaj.art-575ecb3c8dec468288dc4742b169c1432023-11-21T15:46:34ZengMDPI AGPharmaceutics1999-49232021-04-0113456010.3390/pharmaceutics13040560A New Bevacizumab Carrier for Intravitreal Administration: Focus on StabilityDaniela Chirio0Elena Peira1Simona Sapino2Giulia Chindamo3Simonetta Oliaro-Bosso4Salvatore Adinolfi5Chiara Dianzani6Francesca Baratta7Marina Gallarate8Department of Drug Science and Technology, University of Torino, Via P. Giuria 9, 10125 Torino, ItalyDepartment of Drug Science and Technology, University of Torino, Via P. Giuria 9, 10125 Torino, ItalyDepartment of Drug Science and Technology, University of Torino, Via P. Giuria 9, 10125 Torino, ItalyDepartment of Drug Science and Technology, University of Torino, Via P. Giuria 9, 10125 Torino, ItalyDepartment of Drug Science and Technology, University of Torino, Via P. Giuria 9, 10125 Torino, ItalyDepartment of Drug Science and Technology, University of Torino, Via P. Giuria 9, 10125 Torino, ItalyDepartment of Drug Science and Technology, University of Torino, Via P. Giuria 9, 10125 Torino, ItalyDepartment of Drug Science and Technology, University of Torino, Via P. Giuria 9, 10125 Torino, ItalyDepartment of Drug Science and Technology, University of Torino, Via P. Giuria 9, 10125 Torino, ItalyBevacizumab (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.https://www.mdpi.com/1999-4923/13/4/560lipid nanoparticlesmicroemulsionbevacizumabstructure stabilitybiocompatibilityintravitreal injection |
| spellingShingle | Daniela Chirio Elena Peira Simona Sapino Giulia Chindamo Simonetta Oliaro-Bosso Salvatore Adinolfi Chiara Dianzani Francesca Baratta Marina Gallarate A New Bevacizumab Carrier for Intravitreal Administration: Focus on Stability Pharmaceutics lipid nanoparticles microemulsion bevacizumab structure stability biocompatibility intravitreal injection |
| 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 | lipid nanoparticles microemulsion bevacizumab structure stability biocompatibility intravitreal injection |
| url | https://www.mdpi.com/1999-4923/13/4/560 |
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