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Article

Formulation and Development of Nanofiber-Based Ophthalmic Insert for the Treatment of Bacterial Conjunctivitis

1
Center of Pharmacology and Drug Research & Development, University Pharmacy Department of Pharmacy Administration, Semmelweis University, Hőgyes Endre Street 7-9, H-1092 Budapest, Hungary
2
Department of Anatomy, Histology and Embryology Semmelweis University, Tűzoltó Street 58, H-1094 Budapest, Hungary
3
Department of Medical Microbiology, Semmelweis University, Nagyvárad Square 4, H-1089 Budapest, Hungary
4
Department of Pharmaceutics, Semmelweis University, Hőgyes Endre Street 7, H-1092 Budapest, Hungary
5
Department of Polymer Engineering, Faculty of Mechanical Engineering, Budapest University of Technology and Economics, Műegyetem Rkp. 3, H-1111 Budapest, Hungary
*
Author to whom correspondence should be addressed.
Int. J. Mol. Sci. 2024, 25(17), 9228; https://doi.org/10.3390/ijms25179228 (registering DOI)
Submission received: 12 August 2024 / Revised: 22 August 2024 / Accepted: 23 August 2024 / Published: 25 August 2024

Abstract

A novel ophthalmic delivery system utilizing levofloxacin-loaded, preservative-free, nanofiber-based inserts was investigated. Polyvinyl alcohol (PVA) and Poloxamer 407 (Polox)were employed as matrix materials, while hydroxypropyl-beta-cyclodextrin (HP-β-CD) was a solubilizer. The formulations were prepared via electrospinning and characterized for fiber morphology, drug dissolution, cytotoxicity, and antimicrobial activity. Scanning electron microscopy confirmed uniform fibrous structures. Fourier Transform Infrared spectroscopy and X-ray diffraction analyses demonstrated the amorphous state of levofloxacin within the fibers. In vitro dissolution studies revealed a rapid (within 2 min) and complete drug release, with higher HP-β-CD levels slightly delaying the release. Cytotoxicity tests showed increased HP-β-CD concentrations induced irritation, that was mitigated by sodium hyaluronate. The antimicrobial efficacy of the nanofibers was comparable to conventional eye drops, with lower minimum inhibitory concentrations for most tested strains. The nanofibrous formulation prepared from a PVA–Polox-based viscous solution of the drug :CD 1:1 mol ratio, containing 0.4% (w/w) sodium hyaluronate) was identified as a particularly promising alternative formulation due to its rapid and complete dissolution, good biocompatibility, and effective antimicrobial properties. Its gelling properties indicate that the residence time on the eye surface can be increased, potentially reducing discomfort and enhancing therapeutic outcomes. The nanofibrous formulations enhanced antimicrobial efficacy, providing a preservative-free alternative that minimizes the potential eye irritation that might occur because of the preservative agent and reduces the administrated dose frequency by extending the drug’s retention time on the eye’s surface. Subsequently, it improves patients’ adherence, which would reflect positively on the bioavailability. The levofloxacin-HP-β-CD nanofibers demonstrate promise as an alternative to traditional eye drops, offering advantages in solubility, stability, and patient compliance for ocular infection treatment.
Keywords: electrospinning; nanofiber; ophthalmic insert for bacterial eye infection; solid-state characterization; in vitro dissolution test; antibacterial study; cytotoxicity test electrospinning; nanofiber; ophthalmic insert for bacterial eye infection; solid-state characterization; in vitro dissolution test; antibacterial study; cytotoxicity test

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MDPI and ACS Style

Farkas, E.; Abboud, H.; Nagy, N.; Hofmeister, B.; Ostorházi, E.; Tóth, B.; Pinke, B.; Mészáros, L.; Zelkó, R.; Kazsoki, A. Formulation and Development of Nanofiber-Based Ophthalmic Insert for the Treatment of Bacterial Conjunctivitis. Int. J. Mol. Sci. 2024, 25, 9228. https://doi.org/10.3390/ijms25179228

AMA Style

Farkas E, Abboud H, Nagy N, Hofmeister B, Ostorházi E, Tóth B, Pinke B, Mészáros L, Zelkó R, Kazsoki A. Formulation and Development of Nanofiber-Based Ophthalmic Insert for the Treatment of Bacterial Conjunctivitis. International Journal of Molecular Sciences. 2024; 25(17):9228. https://doi.org/10.3390/ijms25179228

Chicago/Turabian Style

Farkas, Eszter, Houssam Abboud, Nándor Nagy, Bálint Hofmeister, Eszter Ostorházi, Bence Tóth, Balázs Pinke, László Mészáros, Romána Zelkó, and Adrienn Kazsoki. 2024. "Formulation and Development of Nanofiber-Based Ophthalmic Insert for the Treatment of Bacterial Conjunctivitis" International Journal of Molecular Sciences 25, no. 17: 9228. https://doi.org/10.3390/ijms25179228

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