A novel approach to achieve semi-sustained drug delivery to the eye through asymmetric loading of soft contact lenses

Sarmout, Malake; Xiao, Yutang; Hu, Xiao; Rakhmetova, Aiym; Koole, Leo H.

doi:10.1016/j.heliyon.2023.e16916

Cited by 1 publication

(3 citation statements)

References 44 publications

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“…Spectrophotometric analysis of voriconazole was done according to the literature [9,36]. We verified that the absorption maximum is at 256 nm (PBS, pH 7.4) and that there is proportionality (Lambert-Beer law) between extinction and voriconazole concentration up to 80 mg/mL; a linear calibration line was constructed.…”

Section: Drug Release In Vitromentioning

confidence: 91%

“…This was achieved by slowly dripping 200 µL of STF every 5 min. The eyes were maintained in this condition for a total of 2 h [9,38]. Following that, the eyes were removed from the water bath, and the drug-loaded rings were carefully removed.…”

Section: Ex-vivo Assessment With Porcine Eyesmentioning

confidence: 99%

“…Hence, this is an important field of research. Much is to be expected from new innovative formulations that support sustained topical delivery of antimicrobial or antifungal agents close to corneal ulcers, as has been emphasized in numerous papers and reviews on the subject [9][10][11][12][13]. Such strategies almost inevitably revolve around biocompatible polymeric biomaterials, which should be engineered such that they will serve as a temporary reservoir for the drug, protect the drug against degradation as long as it resides within the depot, make sure that the drug is delivered locally in a predictable and sustained manner, and compensate (by sustained delivery) for efflux of the drug from the site of the lesion due to tear fluid flow across the surface of the cornea.…”

Section: Introductionmentioning

confidence: 99%

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Sustained Release of Voriconazole Using 3D-Crosslinked Hydrogel Rings and Rods for Use in Corneal Drug Delivery

Rakhmetova,

Yi,

Sarmout

et al. 2023

Gels

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Corneal disorders and diseases are prevalent in the field of clinical ophthalmology. Fungal keratitis, one of the major factors leading to visual impairment and blindness worldwide, presents significant challenges for traditional topical eye drop treatments. The objective of this study was to create biocompatible 3D-crosslinked hydrogels for drug delivery to the cornea, intending to enhance the bioavailability of ophthalmic drugs. Firstly, a series of flexible and porous hydrogels were synthesized (free-radical polymerization), characterized, and evaluated. The materials were prepared by the free-radical polymerization reaction of 1-vinyl-2-pyrrolidinone (also known as N-vinylpyrrolidone or NVP) and 1,6-hexanediol dimethacrylate (crosslinker) in the presence of polyethylene glycol 1000 (PEG-1000) as the porogen. After the physicochemical characterization of these materials, the chosen hydrogel demonstrated outstanding cytocompatibility in vitro. Subsequently, the selected porous hydrogels could be loaded with voriconazole, an antifungal medication. The procedure was adapted to realize a loading of 175 mg voriconazole per ring, which slightly exceeds the amount of voriconazole that is instilled into the eye via drop therapy (a single eye drop corresponds with approximately 100 mg voriconazole). The voriconazole-loaded rings exhibited a stable zero-order release pattern over the first two hours, which points to a significantly improved bioavailability of the drug. Ex vivo experiments using the established porcine eye model provided confirmation of a 10-fold increase in drug penetration into the cornea (after 2 h of application of the hydrogel ring, 35.8 ± 3.2% of the original dose is retrieved from the cornea, which compares with 3.9 ± 1% of the original dose in the case of eye drop therapy). These innovative hydrogel rods and rings show great potential for improving the bioavailability of ophthalmic drugs, which could potentially lead to reduced hospitalization durations and treatment expenses.

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Section: Drug Release In Vitromentioning

confidence: 91%

Section: Ex-vivo Assessment With Porcine Eyesmentioning

confidence: 99%