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Preparation of chitosan-polyvinylpyrrolidone microspheres and films for controlled release and targeting of 5-fluorouracil

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2007
Özerkan, Taylan
Controlled drug delivery systems deliver drugs at predetermined rates for extended periods. Although there are various types such as capsules, tablets etc, micro and nano spheres are the most commonly used systems. In this study, a set of chitosan-polyvinylpyrrolidone (CH-PVP) microspheres containing different amounts of polyvinylpyrrolidone as semi inter penetrating networks (semi-IPN) were prepared as controlled release systems. Emulsification method was applied for the preparation of microspheres and some of them were conjugated with a monoclonal antibody which is immunoglobulin G (IgG). CH-PVP films were also prepared by solvent casting method with the same composition as in the microspheres and, mechanical and surface properties of the films were examined. Prepared microspheres were characterized by SEM, stereo and confocal microscopes. Some microspheres were loaded with a model chemotherapeutic drug, 5-Fluorouracil (5-FU), and in-vitro release of 5-FU were examined in phosphate buffer solutions (pH 7.4, 0.01 M.) It was shown that for semi-IPN samples release was faster compared to pure CH samples and the total release was achived 30 days for CH:PVP-2:1, CH:PVP-3:1 semi-IPNs and CH microspheres and 27 days for CH:PVP-1:1 semi-IPN microspheres. The antibody conjugated microspheres were targeted to MDA-MB (human causasian breast carcinoma cancer cells and coculture cells in culture medium. For the CH-PVP films, it was obtained that as the amount of PVP increased, hydrophobicity as well as mechanical strength of the system was decreased.