Synergism of polysaccharide polymers in antihistamine eye drops: Influence on physicochemical properties and in vivo efficacy.

Autor: Račić A; Department of Pharmaceutical Technology and Cosmetology, University of Banja Luka, Faculty of Medicine, Save Mrkalja 14, 78000 Banja Luka, Bosnia and Herzegovina. Electronic address: andjelka.racic@med.unibl.org., Jurišić Dukovski B; R&D, PLIVA Croatia Ltd., TEVA Group Member, Prilaz baruna Filipovića 29, 10000 Zagreb, Croatia. Electronic address: bisera.jurisicdukovski@pliva.com., Lovrić J; Department of Pharmaceutical Technology, University of Zagreb, Faculty of Pharmacy and Biochemistry, Ante Kovačića 1, 10000 Zagreb, Croatia. Electronic address: jasmina.lovric@pharma.unizg.hr., Dobričić V; Department of Pharmaceutical Chemistry, University of Belgrade-Faculty of Pharmacy, Vojvode Stepe 450, 11221 Belgrade, Serbia. Electronic address: vladimir.dobricic@pharmacy.bg.ac.rs., Vučen S; School of Pharmacy, University College Cork, Cork, Ireland. Electronic address: svucen@ucc.ie., Micov A; Department of Pharmacology, University of Belgrade-Faculty of Pharmacy, Vojvode Stepe 450, 11221 Belgrade, Serbia. Electronic address: ana.micov@pharmacy.bg.ac.rs., Stepanović-Petrović R; Department of Pharmacology, University of Belgrade-Faculty of Pharmacy, Vojvode Stepe 450, 11221 Belgrade, Serbia. Electronic address: radica.stepanovic@pharmacy.bg.ac.rs., Tomić M; Department of Pharmacology, University of Belgrade-Faculty of Pharmacy, Vojvode Stepe 450, 11221 Belgrade, Serbia. Electronic address: maja.tomic@pharmacy.bg.ac.rs., Pecikoza U; Department of Pharmacology, University of Belgrade-Faculty of Pharmacy, Vojvode Stepe 450, 11221 Belgrade, Serbia. Electronic address: uros.pecikoza@pharmacy.bg.ac.rs., Bajac J; Department of Chemical Engineering, University of Novi Sad, Faculty of Technology Novi Sad, Bulevar cara Lazara 1, 21000 Novi Sad, Serbia. Electronic address: ilicj@uns.ac.rs., Krajišnik D; Department of Pharmaceutical Technology and Cosmetology, University of Belgrade-Faculty of Pharmacy, Vojvode Stepe 450, 11221 Belgrade, Serbia. Electronic address: danina.krajisnik@pharmacy.bg.ac.rs.
Jazyk: angličtina
Zdroj: International journal of pharmaceutics [Int J Pharm] 2024 Apr 25; Vol. 655, pp. 124033. Date of Electronic Publication: 2024 Mar 23.
DOI: 10.1016/j.ijpharm.2024.124033
Abstrakt: The incorporation of polymers into drug delivery vehicles has been shown to be a useful approach to prolong the residence time of drugs in the precorneal tear film and to improve penetration into biological membranes. The main objective of this research was to formulate novel viscous eye drops with ketotifen as the active ingredient, containing the polysaccharides: chitosan (MCH), hydroxypropyl guar gum (HPG) and hyaluronic acid (SH) alone and in combination as functional polymers. DSC and FT-IR techniques showed the compatibility between ketotifen and polymers. Physicochemical and rheological analysis at ambient and simulated physiological conditions, as well as the evaluation of mucoadhesive properties showed that vehicles containing combinations of polymers have suitable physicochemical and functional properties with demonstrated synergism between combined polymers (MCH and HPG i.e. SH and HPG). The drug permeability was successfully estimated in vitro using HCE-T cell-based models. MTT cytotoxicity assay demonstrates that the tested formulations were non-toxic and well tolerated. In vivo preclinical study on mice revealed that both vehicles containing mixed polymers enhanced and prolonged the antipruritic/analgesic-like effect of ophthalmic ketotifen. Based on these results, both combinations of polysaccharide polymers, especially SH-HPG, could be considered as potential new carriers for ketotifen for ophthalmic use.
Competing Interests: Declaration of competing interest The authors declare that they have no known competing financial interests or personal relationships that could have appeared to influence the work reported in this paper.
(Copyright © 2024 Elsevier B.V. All rights reserved.)
Databáze: MEDLINE
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