Abstract

6- O-carboxymethyl chitin (CM-chitin), a water-soluble chitin derivative, was gelled in the presence of 15 to 30 m m iron (III) chloride. At the time of gel formation, a peptidic anticancer drug neocarzinostatin (NCS), was efficiently (>50%) incorporated into the gel in the co-presence of 25 to 50 m m calcium chloride and iron (III) chloride. CM-chitin gel containing NCS was digested by lysozyme in vitro and NCS was released from the gel in both a time- and dosedependent manner. In-vivo studies in mice showed that free NCS was rapidly cleared from the circulation, but NCS released from the gel was detectable in plasma even 48 h after the subcutaneous injection of the gel. Antimetastatic effects of the CM-chitin gel containing NCS were studied in the spontaneous pulmonary metastasis model using Bl6-BL6 melanoma; these results suggest that CM-chitin gels are useful as a sustained-release drug carrier.

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