John Garner

mPEG-PLA from PolySciTech used in development of phospho-sulindac loaded nanoparticles for ocular treatment.

Blog Post created by John Garner on Feb 4, 2019

2019 Stony Brook sulindac ocular delivery polyscitech.jpg

Delivery of medicines to the ocular region is difficult as most systemic administrations have relatively poor transport to the eyes relative to the rest of the body and any local administration (eye-drops) is washed away quickly by the tear-action of the yes. Recently, researchers at Stony Brook University used mPEG-PLA (AK005) from PolySciTech (www.polyscitech.com) to generate nanoparticles for ocular application. This research holds promise to improve the longevity and efficacy of ocular medications. Read more: Wen, Ziyi, Natsuko Muratomi, Wei Huang, Liqun Huang, Jinfeng Ren, Jennifer Yang, Yogeeta Persaud et al. "The ocular pharmacokinetics and biodistribution of phospho-sulindac (OXT-328) formulated in nanoparticles: Enhanced and targeted tissue drug delivery." International journal of pharmaceutics 557 (2019): 273-279. https://www.sciencedirect.com/science/article/pii/S037851731830975X

“Abstract: We studied the pharmacokinetics, biodistribution and metabolism of phospho-sulindac (PS), a novel agent efficacious in the treatment of dry eye, formulated in nanoparticles (PS-NPs) following its topical administration to the eye of New Zealand White rabbits. The nanoparticles were spherical with effective diameter = 108.9 ± 41.7 nm, zeta potential = −21.70 ± 3.78 mV, drug loading = 7%, and entrapment efficiency = 46.4%. Of the total PS delivered topically to the eye, >95% was retained in the anterior segment, predominantly in the cornea (Cmax = 101.3 μM; Tmax = 1 h; T1/2 = 2.6 h; area AUC0–16h = 164.4 µM·h) and conjunctiva (Cmax = 89.4 μM; Tmax = 0.25 h; T1/2 = 3.1 h; AUC0–16h = 63.5 µM·h), the tissues most affected by dry eye disease. No PS or its metabolites were detected in the systemic circulation. PS was metabolized to PS sulfide and PS sulfone; all three molecules were hydrolyzed to sulindac, which was converted to sulindac sulfide and sulindac sulfone. A solution formulation of PS provided lower PS levels in ocular tissues but higher levels of PS metabolites, compared to PS-NPs. Therefore, NPs represent an effective formulation for the topical ocular administration of PS for anterior segment diseases, such as dry eye disease.”

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