Abstract
In this research; the release of 5-Fluorouracil (5-FU) from different ionically crosslinked alginate (Alg) beads was investigated by using Fe3+, Al3+, Zn2+, and Ca2+, ions as crosslinking agent. The prepared beads were characterized by Fourier Transform Infrared Spectroscopy (FTIR) Differential Scanning Calorimetry (DSC) and Scanning Electron Micros-copy (SEM). The drug release studies were carried out at three pH values 1.2, 6.8 and 7.4 respectively each for two hours. The effects of the preparation conditions as crosslinker type, drug/polymer (w/w) ratio, crosslinker concentration and time of exposure to crosslinker on the release of 5-FU were investigated for 6 hours at 37℃. It was observed that 5-FU release from the beads followed the order of Fe > Zn > Al > Ca-Alg and increased with increasing drug/polymer ratio. At the end of 6 hours, the highest 5-FU release was found to be 90% (w/w) for Fe-Alg beads at the drug/polymer ratio of 1/8 (w/w), crosslinker concentration of 0.05 M, exposure time of 10 minutes respectively. The swelling measurements of the beads supported the release results. Release kinetics was described by Fickian and non-Fickian approaches.
Highlights
5-Fluorouracil (5-FU) is one of the most widely used agents in cancer theraphy
The prepared beads were characterized by Fourier Transform Infrared Spectroscopy (FTIR) Differential Scanning Calorimetry (DSC) and Scanning Electron Microscopy (SEM)
In the present study we have aimed to increase the strength of alginate beads so that after passing through stomach they can stand for a longer time period in intestinal medium conditions
Summary
5-Fluorouracil (5-FU) is one of the most widely used agents in cancer theraphy. Since its active form inhibits DNA synthesis by inhibiting the normal production of thymidine. Calcium-alginate beads or microparticles when exposed to highly acidic (pH: 1.2) environment of stomach may result in insoluble alginic acid form causing reduction in their degree of crosslinking the beads degrades in a very short time after arriving to colon (pH: 6.8, 7.4) For this reason Arıca et al [27] and Sure-. In the present study we have aimed to increase the strength of alginate beads so that after passing through stomach they can stand for a longer time period in intestinal medium conditions For this reason we have tried different metal ions as Fe3+, Al3+, Zn2+, Ca2+ for the crosslinking of alginate matrix, tried to find most suitable cation for the crosslinking and evaluated the physicochemical properties of the beads prepared. There is no study concerning the use of these ions in the delivery of 5-FU from the alginate matrix
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