title: β-Cyclodextrin hydrogels for the ocular release of antibacterial thiosemicarbazones.
abstract: Two types of hydrophilic networks with conjugated beta-cyclodextrin (β-CD) were developed with the aim of engineering useful platforms for the localized release of an antimicrobial 5,6-dimethoxy-1-indanone N4-allyl thiosemicarbazone (TSC) in the eye and its potential application in ophthalmic diseases. Poly(2-hydroxyethyl methacrylate) soft contact lenses (SCLs) displaying β-CD, namely pHEMA-co-β-CD, and super-hydrophilic hydrogels (SHHs) of directly cross-linked hydroxypropyl-β-CD were synthesized and characterized regarding their structure (ATR/FT-IR), drug loading capacity, swelling and in vitro release in artificial lacrimal fluid. Incorporation of TSC to the networks was carried out both during polymerization (DP method) and after synthesis (PP method). The first method led to similar drug loads in all the hydrogels, with minor drug loss during the washing steps to remove unreacted monomers, while the second method evidenced the influence of structural parameters on the loading efficiency (proportion of CD units, mesh size, swelling degree). Both systems provided a controlled TSC release for at least two weeks, TSC concentrations (up to 4000μg/g dry hydrogel) being within an optimal therapeutic window for the antimicrobial ocular treatment. Microbiological tests against P. aeruginosa and S. aureus confirmed the ability of TSC-loaded pHEMA-co-β-CD network to inhibit bacterial growth.
authors.affiliation: The Group of Biomaterials and Nanotechnology for Improved Medicines (BIONIMED), Department of Pharmaceutical Technology, Faculty of Pharmacy and Biochemistry, University of Buenos Aires, Argentina.
authors.forename: Romina J
authors.initials: RJ
authors.lastname: Glisoni
authors.forename: María J
authors.initials: MJ
authors.lastname: García-Fernández
authors.forename: Marylú
authors.initials: M
authors.lastname: Pino
authors.forename: Gabriel
authors.initials: G
authors.lastname: Gutkind
authors.forename: Albertina G
authors.initials: AG
authors.lastname: Moglioni
authors.forename: Carmen
authors.initials: C
authors.lastname: Alvarez-Lorenzo
authors.forename: Angel
authors.initials: A
authors.lastname: Concheiro
authors.forename: Alejandro
authors.initials: A
authors.lastname: Sosnik
mesh_terms: D000900:Anti-Bacterial Agents / Q000008:administration & dosage* / Q000494:pharmacology; D003263:Contact Lenses, Hydrophilic; D004337:Drug Carriers / Q000008:administration & dosage / Q000737:chemistry; D016503:Drug Delivery Systems / Q000379:methods*; D020100:Hydrogels / Q000008:administration & dosage / Q000138:chemical synthesis* / Q000737:chemistry; D008422:Materials Testing / Q000379:methods; D008826:Microbial Sensitivity Tests; D058105:Polymerization; D011550:Pseudomonas aeruginosa / Q000187:drug effects; D013211:Staphylococcus aureus / Q000187:drug effects; D013882:Thiosemicarbazones / Q000008:administration & dosage* / Q000494:pharmacology; D047392:beta-Cyclodextrins / Q000737:chemistry*
chemical_list: D000900:Anti-Bacterial Agents; D004337:Drug Carriers; D020100:Hydrogels; D013882:Thiosemicarbazones; D047392:beta-Cyclodextrins