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KMID : 0369820060360060371
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Jorunal of Korean Pharmaceutical Sciences
2006 Volume.36 No. 6 p.371 ~ p.375
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A polymeric Antibacterial agent with Sustained Anti-bacterial Activity : Cellulose Xanthate-metal-neomycin Complexs
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Kim In-ho
Jung Yun-Jin
Kim Young-Mi
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Abstract
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Neomycin coupled to a polymer matrix via a metal linker was prepared and evaluated for prolonging antibacterial activity. Microcrystallized cellulose was chemically modified to cellulose xanthate(MCX) to afford metal binding sites. MCX was treated with Cu(Ⅱ), Fe(Ⅲ) or Zn(Ⅱ) followed by reaction with neomycin(Ne). The realease of Ne from MCX-Zn(Ⅱ)-Ne was investigated and its activity duration was measured by ditch plate method. The amount of metal bound to MCX was 0.36 mmol/g matrix, 0.26mmol/g matrix and 0.56mmol/g matrix for Cu(Ⅱ), Zn(Ⅱ) and Fe(Ⅲ), respectively. Ne bound to MCX-metal chelates was 0.006mmol, 0.07mmol and 0.01 mmol per g MCX for Cu(Ⅱ), Zn(Ⅱ) and Fe(Ⅲ), respectively. The Ne released from MCX-Zn(Ⅱ)-Ne was sustained even after seven washes, whereas Ne from NC/Zn(Ⅱ)/Ne mixture was almost completely released in two washes. Antibacterial activity was prolonged with MCX-Zn(Ⅱ)-Ne and MCX-Fe(Ⅲ)-Ne, but not with MCX-Cu(Ⅱ)-Ne when compared with that of free be. Taken together, these results suggest that neomycin coupled to MCX via a proper metal linker has a potential as a polymeric antibacterial agent with sustained activity.
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KEYWORD
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Controlled relsase, Coordinte bond, Polymeric drug, Microcrystallized cellulose, Sustained antibacterial activity, Neomycin
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