Abstract
N-(2-Hydroxypropyl)methacrylamide (HPMA) copolymer-lectin conjugates were investigated for potential use as targeted oral drug carriers for treatment of inflammatory conditions such as colitis. Wheat germ agglutinin (WGA)-HPMA copolymer and peanut agglutinin (PNA)-HPMA copolymer and fluorescein isothiocyanate (FITC)-labeled WGA- and PNA-HPMA copolymer conjugates were synthesized. Conjugate dissociation constants (K d ) for lectin-carbohydrate binding determined by frontal affinity chromatography indicated that no activity reduction of the lectins occurred during the synthesis of these conjugates. K d values measured were in good agreement with literature findings for similar lectin-carbohydrate interactions, on the order of 10 -5 M -1 . Biorecognition of these conjugates by healthy rat intestinal tissue resulted in differential HPMA copolymer-lectin conjugate binding patterns in the same tissue. HPMA copolymer-WGA conjugate showed strong binding in the healthy rat intestinal tissues, while the HPMA copolymer-PNA conjugate showed minimal, but specific binding. This differential binding suggests that site-specific drug delivery via specific lectin recognition may be feasible for treatment of colon inflammation or cancer.
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