Abstract
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.
Highlights
The eye is considered as one of the most sophisticated sensory organs of the human body due to its intricate anatomical structure
Zeta potential results revealed that lutein-loaded PLGA–polyethylene glycol (PEG)–biotin nanoparticles had higher
Results showed that PLGA–PEG–biotin polymer had greater lutein encapsulation compared with the PLGA polymer
Summary
The eye is considered as one of the most sophisticated sensory organs of the human body due to its intricate anatomical structure. The eye can be broadly classified into two segments; i.e., (a) the anterior segment comprising cornea, aqueous humor, conjunctiva, ciliary body, iris, and lens, and (b) the posterior segment consisting of sclera, choroid, Bruch’s membrane, retinal pigment epithelium, retina, optic nerve, and vitreous humor [1,2]. AMD is one of the leading causes of visual loss and is responsible for approximately 9% of global blindness [5]. It is a progressive eye disorder common in the elderly population (>65 years) mainly affecting the macula (central region of the retina) which is responsible for vision [6]. It is hypothesized that antioxidants and anti-inflammatory agents such as carotenoids (lutein, zeaxanthin, α-carotene, β-carotene, lycopene, and β-cryptoxanthin) protect against AMD by absorbing UV light, reducing oxidative stress, and stabilizing cell membranes [9]
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