Novel Lutein Loaded Lipid Nanoparticles on Porcine Corneal Distribution

Abstract

Topical delivery has the advantages including being user friendly and cost effective. Development of topical delivery carriers for lutein is becoming an important issue for the ocular drug delivery. Quantification of the partition coefficient of drug in the ocular tissue is the first step for the evaluation of delivery efficacy. The objectives of this study were to evaluate the effects of lipid nanoparticles and cyclodextrin (CD) on the corneal lutein accumulation and to measure the partition coefficients in the porcine cornea. Lipid nanoparticles combined with 2% HPβCD could enhance lutein accumulation up to 209.2 ± 18 (μg/g) which is 4.9-fold higher than that of the nanoparticles. CD combined nanoparticles have 68% of drug loading efficiency and lower cytotoxicity in the bovine cornea cells. From the confocal images, this improvement is due to the increased partitioning of lutein to the corneal epithelium by CD in the lipid nanoparticles. The novel lipid nanoparticles could not only improve the stability and entrapment efficacy of lutein but also enhance the lutein accumulation and partition in the cornea. Additionally the corneal accumulation of lutein was further enhanced by increasing the lutein payload in the vehicles.

Physicochemical Properties of Lutein-Loaded Microcapsules and Their Uptake via Caco-2 Monolayers

“…Not only can the poor stability of lutein exposed to outside environment lead to a loss of bright yellow color and bioactivity, but also can lead to loss of product quality and poor consumer acceptance [ 13 ]. In order to increase the physicochemical stability, bioavailability and solubility of lutein in aqueous media, a lot of efforts have been paid utilizing various approaches such as self-nanoemulsifying drug delivery systems (SNEDDS) technology [ 13 , 14 , 15 ], liposomal delivery [ 16 , 17 , 18 ], nanoemulsion [ 13 , 19 ], nanocapsules [ 20 ], encapsulation with polysaccharide [ 21 , 22 , 23 , 24 , 25 , 26 ].…”

Topical ophthalmic lipid nanoparticle formulations (SLN, NLC) of indomethacin for delivery to the posterior segment ocular tissues

“…Based on trans-scleral transport studies, the higher permeability across several static layers of ocular tissues (sclera, Bruch’s membrane-choroid, RPE, and neural retina) demonstrates the diffusional ability of drugs to the back of the eye through the conjunctival-scleral pathway [51, 52]. To investigate drug delivery to the posterior ocular segments, scleral diffusion of IN was assessed in trans-SCR experiments.…”

Ophthalmic Nanosystems with Antioxidants for the Prevention and Treatment of Eye Diseases

“…A natural carotenoid pigment, lutein, was also incorporated in several nanosystems. Liu et al combined lutein loaded lipid nanocarriers (NLCs) with 2% β-cyclodextrins (Table 1) using the hot sonication method and they obtained an increase of the EE and lower cytotoxicity in the bovine cornea cells [40]. Bodoki et al reported lutein loaded PLGA NPs preparation.…”