Phenylboronic acid modified mucoadhesive nanoparticle drug carriers facilitate weekly treatment of experimentallyinduced dry eye syndrome

Dry Eye Disease: A Review of Epidemiology in Taiwan, and its Clinical Treatment and Merits

“…PLA-b-Dex-g-PBA NPs (mean diameter = 35.6 ± 7.4) encapsulating up to 12 wt.% of CsA can target the mucous membrane. These demonstrate promising treatment of DED by showing no signs of physical irritation or inflammatory responses after 1 and 12 weeks treatment in an animal model with once a week dosage [208]. Cationized NPs constructed by gelatin and a plasmid coding a modified MUC5AC protein (pMUC5AC) can induce the expression of modified MUC5A and decrease CD4+ T-cell infiltration, and consequently improve the clinical signs [209].…”

Delivery strategies for treatment of age-related ocular diseases: From a biological understanding to biomaterial solutions

“…Thus, topical administration of eye drops for drug delivery to the posterior segment of the eye constitutes a non-invasive approach that may provide significant benefit, but remains challenging due to multiple drainage and biological barriers, including blinking and rapid dispersion of eye drops. To counteract the fast clearing of eye drops, nanoparticles have been modified on the surface with phenylboronic acid and shown to sustain the release of cyclosporin-A for up to 5 days [242]. Solutions might also come from annexin-functionalized nanocarriers which have demonstrated significant uptake and transcytosis of liposomal drug carriers across corneal epithelial barriers [88].…”

Nanoparticles for drug delivery to the anterior segment of the eye

“…Furthermore, the HA coated PCL/BKC nanospheres delivered much more CsA in the cornea than the uncoated PCL/BKC nanospheres (11.4–23.0 vs. 5.9–15.5 ng/mg tissue) 4 h post-topical administration. Phenylboronic acid that can form a complex with cis -diol groups of sugar units, such as sialic acid, ample in mucin at physiological pH [148, 149], [added comma] was used to functionalize the surface of poly( D,L -lactide)- b -dextran nanoparticles to increase the precorneal residence time of the nanoparticles [150]. The surface functionalization with phenylboronic acid led to change in the size and zeta potential of the nanoparticles from 45.8 to 28.6 nm and −2.63 to −31.3 mV, respectively; and high mucin binding of the nanoparticles: 1.18 ± 0.02 mg per mg nanoparticles, which was much greater that the values attained with other types of mucoadhesive nanoparticles such as chitosan-based nanoparticles (~ 0.25 mg per mg nanoparticles) and thiolated nanoparticles (~ 0.13 mg per mg nanoparticles).…”

“…Slit-lamp examination and histopathology observations in rabbits demonstrated that phenylboronic acid surface functionalized poly( D,L -lactide)- b -dextran nanoparticles (~35.6 nm) loaded with and without CsA (12% loading) did not show any detectable irritation or inflammatory reactions after weekly administration for up to 12 weeks. The nanoparticles sustained release CsA for 5 days in vitro , and the released CsA showed efficacy in treating experimental dry eye-induced mice in vivo : once a week administration of CsA loaded nanoparticles achieved both the elimination of inflammatory infiltrates and recovery of the ocular surface, whereas thrice a day administration of commercial product Restasis ® (Cyclosporine Ophthalmic Emulsion, 0.05%) only showed clearance of the inflammatory processes [150]. Table 10 summarizes various drug-loaded polyester nanoparticles and their characteristics.…”