In-situ forming gels containing fluorometholone-loaded polymeric nanoparticles for ocular inflammatory conditions

Yozgatlı

Drug Development Research

2020

Ocular allergy is one of the most common disorders of the eye surface. The conventional eye drops lack of therapeutic efficacy due to low ocular bioavailability and decreased drug residence time on eye surface. Hence, the present research work aimed to formulate, optimize, and evaluate the in situ gel for ophthalmic drug delivery. The prepared in situ gel formulations were evaluated for clarity, pH, gelling capacity, viscosity, osmolality, in vitro release study, and kinetic evaluation. ex vivo corneal permeation/penetration study using goat and in vivo studies on rabbits were also performed. Fourier‐transformed infrared spectroscopy was also applied to study possible interactions between drug and polymers. The formulations found to be stable, nonirritant, and showed sustained release of the drug for a period of up to 24 hr with no ocular damage. The developed in situ gels loaded with tetrahydrozoline are alternative and promising ocular candidates for the treatment of allergic conjunctivitis.

Section: Resultssupporting

confidence: 87%

In vitro–in vivo evaluation of tetrahydrozoline‐loaded ocular in situ gels on rabbits for allergic conjunctivitis management

Yozgatlı

Drug Development Research

2020

“…After 30 min, 50 µL of sodium araquidonate 0.5% were applied. Inflammation was measured every 30 min and the ocular inflammation score (OII) was calculated as reported elsewhere [29].…”

Section: Prevention Of In Vivo Ocular Inflammationmentioning

confidence: 99%

Dexibuprofen Biodegradable Nanoparticles: One Step Closer towards a Better Ocular Interaction Study

et al. 2020

Self Cite

Ocular inflammation is one of the most prevalent diseases in ophthalmology, which can affect various parts of the eye or the surrounding tissues. Non-steroidal anti-inflammatory drugs (NSAIDs) such as ibuprofen, are commonly used to treat ocular inflammation in the form of eye-drops. However, their bioavailability in ocular tissues is very low (less than 5%). Therefore, drug delivery systems such as biodegradable polymeric PLGA nanoparticles constitute a suitable alternative to topical eye administration, as they can improve ocular bioavailability and simultaneously reduce drug induced side effects. Moreover, their prolonged drug release can enhance patient treatment adherence as they require fewer administrations. Therefore, several formulations of PLGA based nanoparticles encapsulating dexibuprofen (active enantiomer of Ibuprofen) were prepared using the solvent displacement method employing different surfactants. The formulations have been characterized and their interactions with a customized lipid corneal membrane model were studied. Ex vivo permeation through ocular tissues and in vivo anti-inflammatory efficacy have also been studied.

“…Although most ocular corticosteroids induce glaucoma by increasing intraocular pressure in prolonged treatment, FMT has a significantly lower risk of causing this disease [7][8][9]. Nowadays, new strategies such as the encapsulation of corticosteroids in polymeric nanoparticles (NPs) of average size smaller than 300 nm and nanostructured gels have shown their capacity to increase the precorneal residence time and reach tissues of the posterior segment of the eye [10][11][12][13][14]. Moreover, the objective in ocular pharmacotherapy is to prevent drug inactivation by cytochrome P450, and its elimination by efflux transports and multidrug resistance proteins [15,16].…”

mentioning

confidence: 99%

Ocular Penetration of fluorometholone-loaded PEG-PLGA Nanoparticles Functionalized With cell-penetrating Peptides

González-Pizarro

Parrotta

Vera

et al. 2019

Nanomedicine (Lond.)

Self Cite

Aim: Development of fluorometholone-loaded PEG-PLGA nanoparticles (NPs) functionalized with cell-penetrating peptides (CPPs) for the treatment of ocular inflammatory disorders. Materials & methods: Synthesized polymers and peptides were used for elaboration of functionalized NPs, which were characterized physicochemically. Cytotoxicity and ability to modulate the expression of proinflammatory cytokines were evaluated in vitro using human corneal epithelial cells (HCE-2). NPs uptake was assayed in both in vitro and in vivo models. Results: NPs showed physicochemical characteristics suitable for ocular administration without evidence of cytotoxicity. TAT-NPs and G2-NPs were internalized and displayed anti-inflammatory activity in both HCE-2 cells and mouse eye. Conclusion: TAT-NPs and G2-NPs could be considered a novel strategy for the treatment of ocular inflammatory diseases of the anterior and posterior segment.