Macromolecular Co-Conjugates of Methotrexate and Ferrocene in the Chemotherapy of Cancer

  • Alain I. Mufula
  • B. A. Aderibigbe
  • Eberhard W. Neuse
  • Hembe E. Mukaya
Article

Abstract

Novel anticancer “as reported by Neuse (Synthetic Polymers as Drug-Delivery Vehicles in Medicine, Hindawi Publishing Corporation, Cairo, 2008) and Mufula (Macromolecular Derivatives of Methotrexate and Ferrocene as Potential Prodrugs in Cancer Chemotherapy, MSc. Dissertation, School of Chemistry, Wits University, Cambridge, 2010)” drugs with enhanced therapeutic effectiveness were synthesized through the concept of drug co-conjugation with polymer carriers. The expected benefits are synergistic effects, which can potentially lead to reduction in doses and side effects caused by high dose of single drug, and the prevention of the development of multi-drug resistance. Multidrug-binding ability of polyaspartamide-type carriers was demonstrated by the co-conjugation with ferrocene and methotrexate (MTX) to the polymer carriers as well as the co-conjugation of ferrocene and folic acid in a two step process involving the HBTU coupling method. The degree of MTX incorporated was found in the range of 10–19% by mass and the degree of Fe found was in the range of 6–13% by mass for the first step of coupling. The degrees MTX, Fe and FA were found to be in the range of 17–27%, 15–16% and 24–26% respectively for the second step.

Keywords

Polymer Amine Carrier Coupling Polyaspartamide Conjugate Co-conjugate 

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Copyright information

© Springer Science+Business Media, LLC 2011

Authors and Affiliations

  • Alain I. Mufula
    • 1
  • B. A. Aderibigbe
    • 1
  • Eberhard W. Neuse
    • 1
  • Hembe E. Mukaya
    • 1
  1. 1.Department of ChemistryUniversity of the WitwatersrandWitsRepublic of South Africa

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