The effects of addition of functional monomers and molecular imprinting on dual drug release from intraocular lens material

[Display omitted] •Drug release from intraocular lenses (IOLs) materials was optimized by monomer addition.•Addition of methacrylic acid (MAA) to the IOL monomer mixture was the best solution.•Molecular imprinting of drugs did not led to improvements compared to functional monomer addition.•Drug-loa...

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Veröffentlicht in:International journal of pharmaceutics 2021-05, Vol.600, p.120513-120513, Article 120513
Hauptverfasser: Topete, Ana, Barahona, Isabel, Santos, Luís F., Pinto, Carlos A., Saraiva, Jorge A., Paula Serro, Ana, Saramago, Benilde
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Sprache:eng
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Zusammenfassung:[Display omitted] •Drug release from intraocular lenses (IOLs) materials was optimized by monomer addition.•Addition of methacrylic acid (MAA) to the IOL monomer mixture was the best solution.•Molecular imprinting of drugs did not led to improvements compared to functional monomer addition.•Drug-loaded MAA-IOLs delivered moxifloxacin and diclofenac at therapeutic levels.•Drug-loaded MAA-IOLs revealed to be non-cytotoxic and non-irritant. Although cataract surgery is considered a safe procedure, post-surgery complications such as endophthalmitis and ocular inflammation, may occur. To prevent this, antibiotics and anti-inflammatories are prescribed in the form of eye drops during the post-operatory period, but they lead to a low drug bioavailability in target tissues. The objective of this work is to develop an intraocular lens (IOL) material to deliver simultaneously one antibiotic, moxifloxacin (MXF), and one anti-inflammatory, diclofenac (DFN), in therapeutic concentrations to prevent both complications. The IOL material was modified through the incorporation of functional monomers, as well as molecular imprinting with both drugs using the same functional monomers, namely acrylic acid (AA), methacrylic acid (MAA), 4-vinylpiridine (4-VP) and a combination of MAA + 4-VP. The best results were obtained with MAA. Molecular imprinting did not influence the drug release, except with AA. Application of a mathematical model predicted that the released MXF and DFN concentrations would stay above the pre-determined MIC of S. aureus and S. epidermidis and the minimum values of IC50 of COX-1 and COX-2, for 9 and 14 days, respectively. Antibacterial tests showed that the released antibiotic remained active. The physical properties of the drug-loaded MAA-hydrogel remained adequate. The developed system proved to be non-irritant and non-cytotoxic.
ISSN:0378-5173
1873-3476
DOI:10.1016/j.ijpharm.2021.120513