Sunitinib-Loaded MPEG-PCL Micelles for the Treatment of Age-Related Macular Degeneration

• Published in: Scientia pharmaceutica Vol. 88; no. 3; pp. 30 - 12
• Main Authors: Streets, Jarriaun, Bhatt, Priyanka, Bhatia, Deepak, Sutariya, Vijaykumar
• Format: Journal Article
• Language: English
• Published: Basel MDPI AG 01.07.2020
• Subjects: Age; age-related macular degeneration; Angiogenesis; anti-VEGF; Antibiotics; Cell growth; Copolymers; Drugs; Kinases; Macular degeneration; micelles; MPEG-PCL; Particle size; Patient compliance; Penicillin; Polymers; Solvents; sunitinib; sustained release; Vascular endothelial growth factor; St Louis Missouri; United States > US
• ISSN: 2218-0532; 0036-8709; 2218-0532
• DOI: 10.3390/scipharm88030030

Age-related macular degeneration (AMD) will be responsible for the vision impairment of more than five million late-aged adults in the next 30 years. Current treatment includes frequent intravitreal injections of anti-vascular endothelial growth factor (VEGF) agents. However, there are methods of drug delivery that can decrease the frequency of intravitreal injections by sustaining drug release. MPEG-PCL ((methoxypoly(ethylene glycol) poly(caprolactone)) has been reported as biocompatible and biodegradable. Polymeric micelles of MPEG-PCL can be useful in efficiently delivering anti-VEGF drugs such as sunitinib to the posterior segment of the eye. In this study, the novel micellar formulation exhibited an average dynamic light scattering (DLS) particle size of 134.2 ± 2.3 nm with a zeta potential of −0.159 ± 0.07 mV. TEM imaging further confirmed the nanoscopic size of the micelles. A sunitinib malate (SM)-MPEG-PCL formulation exhibited a sustained release profile for up to seven days with an overall release percentage of 95.56 ± 2.7%. In addition to their miniscule size, the SM-MPEG-PCL formulation showed minimal cytotoxicity onto the ARPE-19 human retinal pigment epithelial cell line, reporting a percent viability of more than 88% for all concentrations tested at time intervals of 24 h. The SM-MPEG-PCL micelles also exhibited exceptional performance during an anti-VEGF ELISA that decreased the overall VEGF protein expression in the cells across a 24–72 h period. Furthermore, it can be concluded that this type of polymeric vehicle is a promising solution to symptoms caused by AMD and improving the management of those suffering from AMD.