title: Electrospun formulations of acyclovir, ciprofloxacin and cyanocobalamin for ocular drug delivery.
abstract: Two series of fibers containing the active ingredients acyclovir, ciprofloxacin and cyanocobalamin, and combinations of these drugs, were prepared by electrospinning. One set used the hydrophilic poly(vinylpyrrolidone) (PVP) as the filament-forming polymer, while the other used the slow-dissolving poly(ε-caprolactone) (PCL). The fibers were found to have cylindrical morphologies, although there was evidence for solvent occlusion with the PVP systems and for some drug particles in the PCL materials. The active ingredients were generally present in the amorphous physical form in the case of PVP, but evidence of crystallinity was observed with PCL. The existence of intermolecular interactions between the drugs and polymers was proven using simple molecular modeling calculations. Drug release from the various fibers was tested in a validated in vitro outflow model of the eye, and the fiber formulations found to be capable of extending drug release. We thus conclude that electrospun matrices such as those prepared in this work have potential for use as intravitreal implants.
authors.affiliation: Department of Pharmaceutical Technology, Belgorod State University, 85 Pobeda Street, Belgorod 308001, Russia; UCL School of Pharmacy, University College London, 29-39 Brunswick Square, London WC1N 1AX, UK.
authors.forename: Alexandra
authors.initials: A
authors.lastname: Baskakova
authors.affiliation: UCL School of Pharmacy, University College London, 29-39 Brunswick Square, London WC1N 1AX, UK.
authors.forename: Sahar
authors.initials: S
authors.lastname: Awwad
authors.affiliation: UCL School of Pharmacy, University College London, 29-39 Brunswick Square, London WC1N 1AX, UK; Department of Chemical Engineering, University of Alcalá, E-28871 Alcalá de Henares, Madrid, Spain.
authors.forename: Jennifer Quirós
authors.initials: JQ
authors.lastname: Jiménez
authors.affiliation: UCL School of Pharmacy, University College London, 29-39 Brunswick Square, London WC1N 1AX, UK.
authors.forename: Hardyal
authors.initials: H
authors.lastname: Gill
authors.affiliation: Department of Pharmaceutical Technology, Belgorod State University, 85 Pobeda Street, Belgorod 308001, Russia.
authors.forename: Oleg
authors.initials: O
authors.lastname: Novikov
authors.affiliation: NIHR Biomedical Research Centre, Moorfields Eye Hospital and UCL Institute of Ophthalmology, London EC1V 9EL, UK.
authors.forename: Peng T
authors.initials: PT
authors.lastname: Khaw
authors.affiliation: UCL School of Pharmacy, University College London, 29-39 Brunswick Square, London WC1N 1AX, UK.
authors.forename: Steve
authors.initials: S
authors.lastname: Brocchini
authors.affiliation: Department of Pharmaceutical Technology, Belgorod State University, 85 Pobeda Street, Belgorod 308001, Russia. Electronic address: ezhilyakova@bsu.edu.ru.
authors.forename: Elena
authors.initials: E
authors.lastname: Zhilyakova
authors.affiliation: UCL School of Pharmacy, University College London, 29-39 Brunswick Square, London WC1N 1AX, UK. Electronic address: g.williams@ucl.ac.uk.
authors.forename: Gareth R
authors.initials: GR
authors.lastname: Williams
mesh_terms: D000212:Acyclovir / Q000008:administration & dosage / Q000737:chemistry*; D060433:Administration, Ophthalmic; D000900:Anti-Bacterial Agents / Q000008:administration & dosage / Q000737:chemistry; D000998:Antiviral Agents / Q000008:administration & dosage / Q000737:chemistry; D002939:Ciprofloxacin / Q000008:administration & dosage / Q000737:chemistry*; D004339:Drug Compounding; D016503:Drug Delivery Systems; D065546:Drug Liberation; D005123:Eye / Q000378:metabolism; D011091:Polyesters / Q000008:administration & dosage / Q000737:chemistry; D011205:Povidone / Q000008:administration & dosage / Q000737:chemistry; D014805:Vitamin B 12 / Q000008:administration & dosage / Q000737:chemistry*; D014803:Vitamin B Complex / Q000008:administration & dosage / Q000737:chemistry
chemical_list: D000900:Anti-Bacterial Agents; D000998:Antiviral Agents; D011091:Polyesters; D014803:Vitamin B Complex; C016240:polycaprolactone; D002939:Ciprofloxacin; D011205:Povidone; D014805:Vitamin B 12; D000212:Acyclovir
keywords: Acyclovir (Pubchem ID: 2022); Antivirals; Ciprofloxacin (2764); Cyanocobalamin (5311498); Electrospinning; Fibers; Half-life; In vitro; Ocular drug delivery; Posterior segment; Sustained release