PMID- 30208574 OWN - NLM STAT- PubMed-not-MEDLINE LR - 20200930 IS - 2227-9059 (Print) IS - 2227-9059 (Electronic) IS - 2227-9059 (Linking) VI - 6 IP - 3 DP - 2018 Sep 11 TI - Aflibercept Nanoformulation Inhibits VEGF Expression in Ocular In Vitro Model: A Preliminary Report. LID - 10.3390/biomedicines6030092 [doi] LID - 92 AB - Age-related macular degeneration (AMD) is one of the leading causes of blindness in the United States, affecting approximately 11 million patients. AMD is caused primarily by an upregulation of vascular endothelial growth factor (VEGF). In recent years, aflibercept injections have been used to combat VEGF. However, this treatment requires frequent intravitreal injections, leading to low patient compliance and several adverse side effects including scarring, increased intraocular pressure, and retinal detachment. Polymeric nanoparticles have demonstrated the ability to deliver a sustained release of drug, thereby reducing the necessary injection frequency. Aflibercept (AFL) was encapsulated in poly lactic-co-glycolic acid (PLGA) nanoparticles (NPs) via double emulsion diffusion. Scanning electron microscopy showed the NPs were spherical and dynamic light scattering demonstrated that they were uniformly distributed (PDI < 1). The encapsulation efficiency and drug loading were 75.76% and 7.76% respectively. In vitro release studies showed a sustained release of drug; 75% of drug was released by the NPs in seven days compared to the full payload released in 24 h by the AFL solution. Future ocular in vivo studies are needed to confirm the biological effects of the NPs. Preliminary studies of the proposed aflibercept NPs demonstrated high encapsulation efficiency, a sustained drug release profile, and ideal physical characteristics for AMD treatment. This drug delivery system is an excellent candidate for further characterization using an ocular neovascularization in vivo model. FAU - Kelly, Shannon J AU - Kelly SJ AD - Department of Pharmaceutical Sciences, College of Pharmacy, University of South Florida, Tampa, FL 33612, USA. shannonk@health.usf.edu. FAU - Hirani, Anjali AU - Hirani A AD - Department of Pharmaceutical Sciences, College of Pharmacy, University of South Florida, Tampa, FL 33612, USA. ahirani@gmail.com. FAU - Shahidadpury, Vishal AU - Shahidadpury V AD - Department of Pharmaceutical Sciences, College of Pharmacy, University of South Florida, Tampa, FL 33612, USA. vpury89@gmail.com. FAU - Solanki, Aum AU - Solanki A AD - Department of Pharmaceutical Sciences, College of Pharmacy, University of South Florida, Tampa, FL 33612, USA. solankia@health.usf.edu. FAU - Halasz, Kathleen AU - Halasz K AD - Department of Pharmaceutical Sciences, College of Pharmacy, University of South Florida, Tampa, FL 33612, USA. halaszk@health.usf.edu. FAU - Varghese Gupta, Sheeba AU - Varghese Gupta S AD - Department of Pharmaceutical Sciences, College of Pharmacy, University of South Florida, Tampa, FL 33612, USA. svarghes@health.usf.edu. FAU - Madow, Brian AU - Madow B AD - Department of Ophthalmology, College of Medicine, University of Florida, Jacksonville, FL 32209, USA. Brian.madow@jax.ufl.edu. FAU - Sutariya, Vijaykumar AU - Sutariya V AD - Department of Pharmaceutical Sciences, College of Pharmacy, University of South Florida, Tampa, FL 33612, USA. vsutariy@health.usf.edu. LA - eng GR - 2016/USF College of Pharmacy/ PT - Journal Article DEP - 20180911 PL - Switzerland TA - Biomedicines JT - Biomedicines JID - 101691304 PMC - PMC6165497 OTO - NOTNLM OT - PLGA OT - aflibercept OT - age-related macular degeneration OT - nanoparticles OT - vascular endothelial growth factor COIS- The authors declare no conflicts of interest. The funders had no role in the design of the study; in the collection, analyses, or interpretation of data; in the writing of the manuscript, and in the decision to publish the results. EDAT- 2018/09/14 06:00 MHDA- 2018/09/14 06:01 PMCR- 2018/09/11 CRDT- 2018/09/14 06:00 PHST- 2018/08/08 00:00 [received] PHST- 2018/08/28 00:00 [revised] PHST- 2018/09/06 00:00 [accepted] PHST- 2018/09/14 06:00 [entrez] PHST- 2018/09/14 06:00 [pubmed] PHST- 2018/09/14 06:01 [medline] PHST- 2018/09/11 00:00 [pmc-release] AID - biomedicines6030092 [pii] AID - biomedicines-06-00092 [pii] AID - 10.3390/biomedicines6030092 [doi] PST - epublish SO - Biomedicines. 2018 Sep 11;6(3):92. doi: 10.3390/biomedicines6030092.