Polymer-cysteamine conjugates: new mucoadhesive excipients for drug delivery?

Int J Pharm. 2002 Mar 2;234(1-2):91-9. doi: 10.1016/s0378-5173(01)00955-3.

Abstract

In the present study, the features of two new thiolated polymers--the so-called thiomers--were investigated. Mediated by a carbodiimide cysteamine was covalently attached to sodium carboxymethylcellulose (Na-CMC) and neutralised polycarbophil (Na-PCP). Depending on the weight-ratio polymer to cysteamine during the coupling reaction, the resulting CMC-cysteamine conjugate and PCP-cysteamine conjugate showed in maximum 43 +/- 15 and 138 +/- 22 micromole thiol groups per g polymer (mean +/- S.D.; n=3), respectively, which were used for further characterisation. Tensile studies carried out with the CMC-cysteamine conjugate on freshly excised porcine intestinal mucosa displayed no significantly (P<0.01) improved mucoadhesion, whereas, the mucoadhesive properties of the PCP-cysteamine conjugate were increased 2.5-fold compared with the unmodified polymer. The swelling behaviour of the CMC-cysteamine conjugate was uninfluenced by the covalent attachment of the sulfhydryl compound. In contrast the swelling behaviour of the PCP-cysteamine conjugate was improved significantly (P<0.01) versus unmodified PCP. Furthermore, in aqueous solutions the disintegration time of tablets based on the CMC- and PCP-cysteamine conjugates was prolonged 1.5 and 3.2-fold, respectively, in comparison to tablets containing the corresponding unmodified polymers. According to these results, especially the PCP-cysteamine conjugate represents a promising new pharmaceutical excipient for various drug delivery systems.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Acrylic Resins / chemistry
  • Adhesives / chemistry*
  • Carboxymethylcellulose Sodium / chemistry
  • Cysteamine / chemistry*
  • Drug Carriers
  • Drug Delivery Systems*
  • Mucous Membrane / metabolism
  • Polymers / chemistry*
  • Solubility
  • Sulfhydryl Compounds / chemistry
  • Tablets
  • Tensile Strength

Substances

  • Acrylic Resins
  • Adhesives
  • Drug Carriers
  • Polymers
  • Sulfhydryl Compounds
  • Tablets
  • Cysteamine
  • calcium polycarbophil
  • Carboxymethylcellulose Sodium