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KMID : 0525720100150040216
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Journal of Chitin and Chitosan
2010 Volume.15 No. 4 p.216 ~ p.222
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Evaluation of Chitosan-Metal-Tetracycline Complexes as A Polymeric Antibacterial Agent with Prolonged Activity
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Yum Soo-Hwan
Kim Ji-Hye
Hong Sung-Chae
Jung Yun-Jin
Kim Young-Mi
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Abstract
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To develop a polymeric drug having controlled-release properties, chitosan-metal-tetracycline ternary complexes (CMTC) were prepared using Cu(II), Zn(II), Mg(II) and Ca(II) as metals. Coupling of tetracycline (Tc) was examined varying concentration, temperature, pH and metal/Tc ratio, and properties of drug-release and prolongation of antimicrobial activity were investigated. Coupling of Tc to chitosan was carried out by one-bath process. Binding was favored at initial pH 4 and lower temperature and the maximal binding of Tc was observed on treatment at 4.6 mM Tc-metal complexes regardless of metals. While an increase of Zn(II) concentration to 9.2 mM did not affect binding amount of Tc, such increase diminished binding of Tc to chitosan for Cu(II). Binding amount of Tc was on the order of Zn(II) > Cu(II)>>Mg(II), Ca(II). The degree of the Tc release, which was examined by batch and flow method, was greater for chitosan-Zn(II)-tetracycline complex (CZTC) than chitosan-Cu(II)-tetracycline complex (CCTC). The Tc release became greater as pH decreased or temperature increased. Antimicrobial activities were tested against G(+) Bacillus subtillis NA-1 and G(?) Escherichia coli TG-1 by employing ditch plate method. CZTC and CCTC showed prolonged activity compared to free Tc, whose activity was more prolonged for CTZC. Our data suggest that chitosan is of use as a polymeric matrix for controlled release of drugs to form a chelate with metals such as Cu(II) and Zn(II).
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KEYWORD
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Chitosan, Tetracycline, polymeric antimicrobial agent, prolonged activity, chelation
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