PLGA-PEG-Biotin from PolySciTech used in development of lutein loaded nanoparticle for macular degeneration treatment

 

Macular Degeneration is a progressive disease in which a small central portion of the retina wears down over time. Lutein is a carotenoid with reported anti-inflammatory properties which can improve macular degeneration but has relatively poor absorption/transport. Recently, researchers at High Point University, University of Missouri, and University of the Sciences in Philadelphia used PLGA (AP041) and PLGA-PEG-Biotin (AI167) from PolySciTech (www.polyscitech.com) to create nanoparticles for treating ocular disease. This research holds promise to improve treatments against this blinding disease in the future. Read more: Bolla, Pradeep Kumar, Vrinda Gote, Mahima Singh, Manan Patel, Bradley A. Clark, and Jwala Renukuntla. "Lutein-Loaded, Biotin-Decorated Polymeric Nanoparticles Enhance Lutein Uptake in Retinal Cells." Pharmaceutics 12, no. 9 (2020): 798. https://www.mdpi.com/1999-4923/12/9/798

“Age related macular degeneration (AMD) is one of the leading causes of visual loss and is responsible for approximately 9% of global blindness. It is a progressive eye disorder seen in elderly people (>65 years) mainly affecting the macula. Lutein, a carotenoid, is an antioxidant, and has shown neuroprotective properties in the retina. However, lutein has poor bioavailability owing to poor aqueous solubility. Drug delivery to the posterior segment of the eye is challenging due to the blood–retina barrier. Retinal pigment epithelium (RPE) expresses the sodium-dependent multivitamin transporter (SMVT) transport system which selectively uptakes biotin by active transport. In this study, we aimed to enhance lutein uptake into retinal cells using PLGA–PEG–biotin nanoparticles. Lutein loaded polymeric nanoparticles were prepared using O/W solvent-evaporation method. Particle size and zeta potential (ZP) were determined using Malvern Zetasizer. Other characterizations included differential scanning calorimetry, FTIR, and in-vitro release studies. In-vitro uptake and cytotoxicity studies were conducted in ARPE-19 cells using flow cytometry and confocal microscopy. Lutein was successfully encapsulated into PLGA and PLGA–PEG–biotin nanoparticles (<250 nm) with uniform size distribution and high ZP. The entrapment efficiency of lutein was ≈56% and ≈75% for lutein-loaded PLGA and PLGA–PEG–biotin nanoparticles, respectively. FTIR and DSC confirmed encapsulation of lutein into nanoparticles. Cellular uptake studies in ARPE-19 cells confirmed a higher uptake of lutein with PLGA–PEG–biotin nanoparticles compared to PLGA nanoparticles and lutein alone. In vitro cytotoxicity results confirmed that the nanoparticles were safe, effective, and non-toxic. Findings from this study suggest that lutein-loaded PLGA–PEG–biotin nanoparticles can be potentially used for treatment of AMD for higher lutein uptake. Keywords: lutein; PLGA; PLGA–PEG–biotin; ARPE-19; retina; macular edema; age-related macular degeneration; biotin-decorated nanoparticles; polymeric nanoparticles; targeted therapy”