Influence of BAKs on tear film lipid layer: In vitro and in silico models

0570868 - ÚFCH JH 2024 RIV NL eng J - Journal Article
Riedlová, Kamila - Saija, Maria Chiara - Olžyńska, Agnieszka - Jurkiewicz, Piotr - Daull, P. - Garrigue, J.-S. - Cwiklik, Lukasz
Influence of BAKs on tear film lipid layer: In vitro and in silico models.
European Journal of Pharmaceutics and Biopharmaceutics. Roč. 186, MAY 2023 (2023), s. 65-73. ISSN 0939-6411. E-ISSN 1873-3441
R&D Projects: GA ČR(CZ) GA21-19854S
Institutional support: RVO:61388955
Keywords : Benzalkonium chloride * Lipid films * Molecular dynamics * Tear film * Tear film lipid layer * Topical ophthalmic formulations
OECD category: Physical chemistry
Impact factor: 4.9, year: 2022
Method of publishing: Limited access

Benzalkonium chloride (BAK) compounds are commonly used in topical ophthalmic products as preservatives and stabilizers. BAK mixtures containing several compounds with different alkyl chain lengths are typically used. However, in chronic eye conditions, such as dry eye disease and glaucoma, the accumulation of adverse effects of BAKs was observed. Hence, preservative-free eye drops formulations are preferred. On the other hand, selected long-chain BAKs, particularly cetalkonium chloride, exhibit therapeutic functions, promoting epithelium wound healing and tear film stability. Nevertheless, the mechanism of BAKs influence on the tear film is not fully understood. By employing in vitro experimental and in silico simulation techniques, we elucidate the action of BAKs and demonstrate that long-chain BAKs accumulate in the lipid layer of the tear film model, stabilizing it in a concentration-dependent fashion. In contrast, short-chain BAKs interacting with the lipid layer compromise the tear film model stability. These findings are relevant for topical ophthalmic drug formulation and delivery in the context of selecting proper BAK species and understanding the dose dependency for tear film stability.
Permanent Link: https://hdl.handle.net/11104/0342196