Immobilization of alpha-[di-(beta-chloroethyl)-amide]-N-(m-nitrobenzoyl)-D,L-asparagic acid on xanthan

J Biomater Appl. 2003 Oct;18(2):83-94. doi: 10.1177/088532803032827.

Abstract

The paper studies the coupling reaction, through ester-type covalent bonds, of an oxazolone derived from the N-(m-nitrobenzoyl)-L-asparagic acid, the cycle of which is opened with an N-mustard derivative, on xanthan (a polysaccharide of microbian synthesis), in conditions of activation with dicyclohexyl carbodiimide. The coupling product has been characterized through elemental analysis and IR spectroscopy. For the establishment of the capacity of the active principle's controlled release by the polymer-active principle system thus obtained, active principle's release kinetics from the polysaccharide support, in conditions of basic hydrolysis, is studied. In vivo tests realized on mice proved the antitumoral activity of the compounds resulted by chemical bonding of the N-mustard derivative on xanthan.

Publication types

  • Evaluation Study

MeSH terms

  • Administration, Oral
  • Adsorption
  • Animals
  • Aspartic Acid / administration & dosage*
  • Aspartic Acid / analogs & derivatives
  • Aspartic Acid / chemical synthesis*
  • Aspartic Acid / toxicity
  • Carcinoma / drug therapy*
  • Delayed-Action Preparations / administration & dosage*
  • Delayed-Action Preparations / chemical synthesis*
  • Delayed-Action Preparations / toxicity
  • Female
  • Male
  • Mice
  • Nitrogen Mustard Compounds / administration & dosage*
  • Nitrogen Mustard Compounds / chemical synthesis*
  • Nitrogen Mustard Compounds / toxicity
  • Polysaccharides, Bacterial / chemistry*
  • Survival Analysis
  • Treatment Outcome

Substances

  • Delayed-Action Preparations
  • Nitrogen Mustard Compounds
  • Polysaccharides, Bacterial
  • Aspartic Acid
  • xanthan gum