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

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.


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The glycosylation in recombinant monoclonal antibody (rMab) drugs is a major concern in the biopharmaceutical industry as it impacts the drugs' many attributes. Characterization is important but complicated by the intricate structures, microheterogeneity, and the limitations of current tools for structural analysis. In this study, we developed a liquid chromatography-mass spectrometry (LC-MS) N-glycan library based on eight commercial rMab drugs. A library of over 70 structures was developed for the rapid c...
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Most contemporary methods of screening and quantitating controlled substances and therapeutic drugs in biofluids typically require laborious, time-consuming, and expensive analytical workflows. In recent years, our group has worked toward developing microextraction (mu e)-mass spectrometry (MS) technologies that merge all of the tedious steps of the classical methods into a simple, efficient, and low-cost methodology. Unquestionably, the automation of these technologies allows for faster sample throughput, ...
The design and synthesis of a photo-controlled, peptide-based potential drug carrier
Parlak Khalily, Melek; Özçubukçu, Salih (The Scientific and Technological Research Council of Turkey, 2018-01-01)
Our focus in this study is on the design and synthesis of a light-responsive peptide-based nanocarrier in order to develop effective and biocompatible drug delivery systems. The synthesized nanocarrier is basically composed of peptide amphiphiles comprising a micelle forming a Pro-Pro-Pro-Lys-Lys-Lys peptide sequence with an attached anthracene fluorophore Anthracene containing an inner core of the micelle can serve as a storage site for poorly water-soluble drugs. Moreover, anthracenes that come in close p...
Synthesis of spiro-containing 1,4-oxazepines from N-propargylic beta-enaminones
Karadeniz, Eda; Kelgökmen, Yılmaz; Zora, Metin (2018-03-18)
An efficient and general method for the synthesis of spiro‐1,4‐oxazepines and 3,3‐dimethyl‐1,4‐oxazepines is reported. When treated with ZnI2 and AgSbF6 in refluxing DCE, cyclohexane‐embedded N‐propargylic β‐enaminones underwent 7‐exo‐dig cyclization to afford spiro‐1,4‐oxazepines, specifically 12‐methylene‐11‐oxa‐7‐azaspiro[5.6]dodeca‐7,9‐dienes, in good to high yields. Accordingly, N‐(1,1‐dimethyl)propargylic β‐enaminones produced 3,3‐dimethyl‐1,4‐oxazepines. Cyclization was found to be general for a dive...
Controlled doxorubicin delivery from photoresponsive liposomes carrying vitamin A derivatives /
Heper, Senem; Hasırcı, Vasıf Nejat; Hasırcı, Nesrin; Department of Biotechnology (2014)
Drug delivery systems (DDS) have been an attractive approach to eliminate the drawbacks of conventional drug administration. Controlled and photoresponsive drug delivery systems have a special advantage; they deliver drugs more effectively. Liposomes are mostly preferred as drug carriers due to their ability to carry both hydrophilic and hydrophobic drugs, their being non-toxic and non-immunogenic. In this study, photoresponsive liposomes were prepared by incorporating vitamin A derivatives into the lipid b...
Citation Formats
T. Özerkan, “Preparation of chitosan-polyvinylpyrrolidone microspheres and films for controlled release and targeting of 5-fluorouracil,” M.S. - Master of Science, Middle East Technical University, 2007.