PhD Scientific Days 2024

Budapest, 9-10 July 2024

Poster Session B - Pharmaceutical Sciences and Health Technologies 1.

Development of Levofloxacin-loaded Electrospun Nanofibrous Ocular Insert for the Treatment of Antibacterial Conjunctivitis

Author(s)

Houssam Abboud1, Eszter Farkas1, Nándor Nagy1, Balázs Pinke32, Romána Zelkó11, Adrienn Kazsoki11
1: Semmelweis University
2: Budapest University of Technology and Economics,

Text of the abstract

Introduction: Ocular inserts are significant candidates used to overcome the disadvantages of ophthalmic conventional dosage forms, particularly regarding infection treatment. Levofloxacin stands out among of the used drugs due to its wide antibacterial spectrum and low cytotoxicity, making it a crucial criterion for ocular inserts. Therefore, Levofloxacin can be a suitable option for formulations of ocular inserts.
Aims: This work aimed to prepare levofloxacin-containing, polyvinyl alcohol (PVA)--based ocular insert by electrospinning using different excipients. Moreover, to investigate how the different molecular weights of PVA and the other excipients affect the fibers' characteristics and the drug profile release.
Methods: PVA (Mowiol® 18-88 and 40-88) was chosen as the base of the electrospun samples. Poloxamer 407 was added as a mucoadhesive-enhancing agent. The total polymer concentration was set at 3 levels: 10, 12, and 14 % (w/w). Hydroxypropyl beta-cyclodextrin (HP-β-CD) was used in a 1:1, 1:1.5 mol ratio to increase the solubility of the drug. The morphological analysis of the samples was performed by Scanning Electron Microscopy and their solid phase characterization by Fourier transform infrared spectroscopy (FT-IR) and X-ray diffraction (XRD). The dissolution study was performed in phosphate buffer (pH 7.4). The drug concentration was determined by UV-vis spectroscopy.
Results: The morphological test confirmed the fibrous structure of all the produced samples. The FT-IR spectra showed the formulation of amorphous solid dispersion which was confirmed by X-ray diffraction measurements. The drug release from the nanofibrous samples was fast and complete. By increasing each cyclodextrin amount and PVA molecular weight, slightly prolonged (but also very fast) drug dissolution was achieved. In the case of the formulations of Mowiol® 18-88 eye irritation test was carried out on the chorioallantois membrane of fertilized eggs and showed eye irritation in the case of the 1:1,5 mol ratio of drug: CD.
Conclusion: The Mowiol® 18-88 based formulation with a 1:1 drug: HP-β-CD mol ratio could be suitable for the treatment of antibacterial conjunctivitis.
Funding: This project was supported by ÚNKP-23-4-II-SE-22 New National Excellence Program of the Ministry for Culture and Innovation from the source of the National Research, Development, and Innovation Fund.