Abstract
Purpose :
Age-related macular degeneration (AMD) is one of the major causes of blindness in elderly people. AMD is a neurodegenerative disease affecting the posterior segment of the eye. Lutein, a carotenoid with anti-oxidant properties has shown neuroprotective properties in the retina. Drug delivery to the posterior segment of the eye is challenging due to blood retinal barrier. Retinal pigment epithelium (RPE) expresses folate receptors which selectively uptake folic acid by active transport. Therefore, the purpose of this study is to enhance uptake of lutein by formulating lutein loaded PLGA-PEG-FOL nanoparticles.
Methods :
Lutein loaded PLGA and PLGA-PEG-FOL nanoparticles were prepared using double emulsion solvent evaporation method. Size, zeta potential and polydispersity index were determined using Zetasizer Nano ZS (Malvern Instruments, U.K.). Lutein encapsulation efficiency (%EE) and drug loading (%DL) capacity in freeze dried nanoparticles was measured using HPLC. Differential scanning calorimetry (DSC) was used to confirm the encapsulation of lutein. Scanning electron microscopy revealed that nanoparticles were spherical in shape. Selective uptake of lutein in ARPE-19 cells is underway in our laboratory.
Results :
Mean diameter (±SD) of lutein loaded nanoparticles formulated using PLGA and PLGA-PEG-FOL was 132.6 ± 1.041 nm and 188.0 ± 4.058 nm, respectively. %EE and %DL of lutein-PLGA nanoparticles was 48.82 ± 15.50 and 9.76 ± 3.10%, respectively, whereas, it was 72.87 ± 7.22% and 14.57 ± 1.44% for PLGA-PEG-FOL nanoparticles. DSC results confirmed that lutein was encapsulated into the nanoparticles.
Conclusions :
We have successfully formulated lutein encapsulated PLGA and PLGA-PEG-FOL nanoparticles with particle size <200 nm. Both the formulations showed good encapsulation and drug loading. Other characterizations and evaluations such as in-vitro release profile and cellular uptake are underway.
This abstract was presented at the 2019 ARVO Annual Meeting, held in Vancouver, Canada, April 28 - May 2, 2019.