Next Article in Journal
Phytochemicals and Enzyme Inhibitory Capacities of the Methanolic Extracts from the Italian Apple Cultivar Mela Rosa dei Monti Sibillini
Previous Article in Journal
Echinacea purpurea (L.) Moench: Chemical Characterization and Bioactivity of Its Extracts and Fractions
Previous Article in Special Issue
Oral l-Cysteine Supplementation Enhances the Long Term-Effect of Topical Basic Fibroblast Growth Factor (bFGF) in Reducing the Corneal Haze after Photorefractive Keratectomy in Myopic Patients
Open AccessArticle

Ocular Co-Delivery of Timolol and Brimonidine from a Self-Assembling Peptide Hydrogel for the Treatment of Glaucoma: In Vitro and Ex Vivo Evaluation

1
Department of Pharmaceutical Technology, School of Pharmacy, Aristotle University of Thessaloniki, GR-54124 Thessaloniki, Greece
2
Foundation for Research and Technology Hellas, Institute of Chemical Engineering and High Temperature Chemical Processes, GR-26504 Patras, Greece
3
Department of Materials Science, University of Patras, GR-26504 Patras, Greece
4
Department of Food Science and Technology, School of Agriculture, Aristotle University, GR-54124 Thessaloniki, Greece
5
Department of Oral Medicine/Pathology, School of Dentistry, Aristotle University of Thessaloniki, GR-54124 Thessaloniki, Greece
6
Laboratory of Pharmaceutical Analysis, Department of Pharmaceutical Technology, School of Pharmacy, Aristotle University of Thessaloniki, GR-54124 Thessaloniki, Greece
*
Author to whom correspondence should be addressed.
Pharmaceuticals 2020, 13(6), 126; https://doi.org/10.3390/ph13060126
Received: 21 May 2020 / Revised: 16 June 2020 / Accepted: 20 June 2020 / Published: 21 June 2020
(This article belongs to the Special Issue Advances in Ocular Pharmacology)
Effective pharmacotherapy during glaucoma treatment depends on interventions that reduce intraocular pressure (IOP) and retain the IOP lowering effect for sufficient time so as to reduce dosing frequency and enhance patient adherence. Combination anti-glaucoma therapy and dosage forms that increase precorneal residence time could therefore constitute a promising therapeutic intervention. The in-situ gel forming self-assembling peptide ac-(RADA)4-CONH2 was evaluated as carrier for the ocular co-delivery of timolol maleate (TM) and brimonidine tartrate (BR). The hydrogel’s microstructure and mechanical properties were assessed with atomic force microscopy and rheology, respectively. Drug diffusion from the hydrogel was evaluated in vitro in simulated tear fluid and ex vivo across porcine corneas and its effect on the treated corneas was assessed through physicochemical characterization and histological analysis. Results indicated that TM and BR co-delivery affected hydrogel’s microstructure resulting in shorter nanofibers and a less rigid hydrogel matrix. Rapid and complete release of both drugs was achieved within 8 h, while a 2.8-fold and 5.4-fold higher corneal permeability was achieved for TM and BR, respectively. No significant alterations were induced in the structural integrity of the corneas treated with the hydrogel formulation, suggesting that self-assembling peptide hydrogels might serve as promising systems for combination anti-glaucoma therapy. View Full-Text
Keywords: self-assembling peptide hydrogel; glaucoma; timolol maleate/brimonidine tartrate combination; ex vivo ocular permeability self-assembling peptide hydrogel; glaucoma; timolol maleate/brimonidine tartrate combination; ex vivo ocular permeability
Show Figures

Graphical abstract

MDPI and ACS Style

Taka, E.; Karavasili, C.; Bouropoulos, N.; Moschakis, T.; Andreadis, D.D.; Zacharis, C.K.; Fatouros, D.G. Ocular Co-Delivery of Timolol and Brimonidine from a Self-Assembling Peptide Hydrogel for the Treatment of Glaucoma: In Vitro and Ex Vivo Evaluation. Pharmaceuticals 2020, 13, 126.

Show more citation formats Show less citations formats
Note that from the first issue of 2016, MDPI journals use article numbers instead of page numbers. See further details here.

Article Access Map by Country/Region

1
Search more from Scilit
 
Search
Back to TopTop