The aim of this work was to evaluate the influence of the composition and the application of an imprinting technique on the loading capability of weakly crosslinked hydroxyethyl methacrylate (HEMA) hydrogels, with a view to their use as reloadable soft contact lenses for administration of timolol. Hydrogels were prepared by dissolution of ethylene glycol dimethacrylate (EGDMA, 10 mM) in HEMA with or without methacrylic acid (MAA) or methyl methacrylate (MMA; 100-400 mM) and with or without timolol maleate (10 mg/mL), initiation of polymerization by addition of 2,2'-azo-bis(isobutyronitrile) (AIBN, 10 mM), injection in molds, and curing in an oven at 50-70 degrees C. Unreacted reagents were removed by boiling. The dry hydrogels were clear and fully polymerized with smooth, poreless surfaces and presented optimal mechanical properties. The hydrogels were then characterized by determination of their swelling and timolol release kinetics in 0.9% NaCl, phosphate buffer (pH 7.4) and artificial lacrimal fluid, and of the timolol loading capacity of both nonimprinted hydrogels and de-timololized imprinted hydrogels at various pHs. Both water uptake and timolol release exhibited Fickian kinetics, except in the case of hydrogels made with 400 mM MAA. Timolol diffusion into 0.9% NaCl from HEMA or HEMA/MMA was slow; release from HEMA/MAA into phosphate buffer or lacrimal fluid was faster and increased with the MAA content of the polymer. Timolol loading was significant for HEMA/MAA hydrogels (imprinted or not) at pH 5.5-7.5, and specially for imprinted hydrogels containing 100 mM MAA, which absorb 12 mg timolol/g dry hydrogel. The results indicate that the incorporation of MAA as comonomer increases the timolol loading capacity to therapeutically useful levels while retaining appropriate release characteristics.
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http://dx.doi.org/10.1002/jps.10209 | DOI Listing |
Adv Mater
January 2025
Department of Chemical Engineering & Applied Chemistry, University of Toronto, 200 College Street, Toronto, ON, M5S 3E5, Canada.
Colloidal drug aggregates (CDAs) are challenging in drug discovery due to their unpredictable formation and interference with screening assays. These limitations are turned into a strategic advantage by leveraging CDAs as a drug delivery platform. This study explores the deliberate formation and stabilization of CDAs for local ocular drug delivery, using a modified smallmolecule glaucoma drug.
View Article and Find Full Text PDFInt J Pharm
December 2024
Guangdong Provincial Key Laboratory for Research and Evaluation of Pharmaceutical Preparations, College of Pharmacy, Guangdong Pharmaceutical University, Guangzhou 510006, PR China. Electronic address:
PLoS One
December 2024
Department of Social and Clinical Pharmacy, Faculty of Pharmacy in Hradec Králové, Charles University in Prague, Prague, Czech Republic.
Free radical polymerization technique was used to formulate Poloxamer-188 based hydrogels for controlled delivery. A total of seven formulations were formulated with varying concentrations of polymer, monomer ad cross linker. In order to assess the structural properties of the formulated hydrogels, Fourier Transform Infrared Spectroscopy (FTIR), Thermogravimetric analysis (TGA), Differential Scanning Calorimetry (DSC), Scanning electron microscopy (SEM), and X-ray diffraction (XRD) were carried out.
View Article and Find Full Text PDFInt J Biol Macromol
October 2024
Research Center for Pharmaceutical Nanotechnology, Biomedicine Institute, Tabriz University of Medical Sciences, Tabriz, Iran.
Drug Deliv Transl Res
July 2024
Nanotechnology Research Center, Medical Basic Sciences Research Institute, Ahvaz Jundishapur University of Medical Sciences, Ahvaz, Iran.
Due to the small capacity of the eye cavity and the rapid drainage of liquid into the nasolacrimal duct, patients must frequently administer the drops. Nanoparticles (NPs) and in situ gel systems have each proven their ability to achieve eye retention independently. In this study, timolol-loaded chitosan-carbomer NPs were prepared using the polyelectrolyte complexation method, and incorporated into a pH-responsive in situ gel system made of carbomer.
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