Preprint Article Version 1 Preserved in Portico This version is not peer-reviewed

Ophthalmic Nanoemulsion Fingolimod Formulation for Topical Application

Version 1 : Received: 19 January 2024 / Approved: 22 January 2024 / Online: 22 January 2024 (10:08:55 CET)

How to cite: Kashikar, R.; Senapati, S.; Dudhipala, N.; Basu, S.K.; Mandal, N.; Majumdar, S. Ophthalmic Nanoemulsion Fingolimod Formulation for Topical Application. Preprints 2024, 2024011525. https://doi.org/10.20944/preprints202401.1525.v1 Kashikar, R.; Senapati, S.; Dudhipala, N.; Basu, S.K.; Mandal, N.; Majumdar, S. Ophthalmic Nanoemulsion Fingolimod Formulation for Topical Application. Preprints 2024, 2024011525. https://doi.org/10.20944/preprints202401.1525.v1

Abstract

The active form of fingolimod (FTY720; FT) is a sphingosine-1-phosphate receptor agonist with potential ocular applications. The goal of the present study was to develop an FT-loaded nanoemulsion (NE; FT-NE) formulation for the efficient and prolonged delivery of FT to the posterior segment of the eye through the topical route. FT-NE formulations were prepared with homogenization followed by probe sonication method. The lead FT-NE formulation (0.15% and 0.3% w/v loading), comprising soybean oil as lipid and Tween® 80 and Poloxamer 188 as surfactants, was further evaluated for in vitro release, surface morphology, filtration sterilization, and stability at refrigerated temperature. The formulation, at both dose levels, showed desirable physicochemical characteristics, a nearly spherical shape with homogenous nanometric size distribution, and was stable for 180 days (last time point checked) at refrigerated temperature post-filtration through polyethersulfone (0.22 µm) membrane. In vitro release studies showed prolonged release, compared with the control FT solution (FT-S), over 24 h. The results from these studies demonstrate that the FT-NE formulation can serve as a viable platform for the ocular delivery of FT through the topical route.

Keywords

Fingolimod; nanoemulsion; ocular drug delivery; sterilization; stability; physicochemical characterization

Subject

Medicine and Pharmacology, Pharmacy

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