Mechanism of tumor-targeted delivery of macromolecular drugs, including the EPR effect in solid tumor and clinical overview of the prototype polymeric drug SMANCS

J Control Release. 2001 Jul 6;74(1-3):47-61. doi: 10.1016/s0168-3659(01)00309-1.


This review article describes three aspects of polymeric drugs. The general mechanism of the EPR (enhanced permeability and retention) effect and factors involved in the effect are discussed, in view of the advantages of macromolecular therapeutics for cancer treatment, which are based on the highly selective EPR-related delivery of drug to tumor. Also described are advantages of more general water-soluble polymeric drugs as primary anticancer agents, using SMANCS as an example. Last, SMANCS/Lipiodol is discussed with reference to the type of formulation for arterial injection with most pronounced tumor selective delivery, as well as its advantages, precautions, and side effects from the clinical standpoint.

Publication types

  • Research Support, Non-U.S. Gov't
  • Review

MeSH terms

  • Amino Acid Sequence
  • Animals
  • Antineoplastic Agents / administration & dosage
  • Antineoplastic Agents / pharmacokinetics
  • Antineoplastic Agents / pharmacology*
  • Drug Delivery Systems*
  • Humans
  • Macromolecular Substances
  • Maleic Anhydrides / administration & dosage
  • Maleic Anhydrides / pharmacokinetics
  • Maleic Anhydrides / pharmacology*
  • Molecular Sequence Data
  • Permeability
  • Polystyrenes / administration & dosage
  • Polystyrenes / pharmacokinetics
  • Polystyrenes / pharmacology*
  • Zinostatin / administration & dosage
  • Zinostatin / analogs & derivatives*
  • Zinostatin / pharmacokinetics
  • Zinostatin / pharmacology*


  • Antineoplastic Agents
  • Macromolecular Substances
  • Maleic Anhydrides
  • Polystyrenes
  • poly(maleic acid-styrene)neocarzinostatin
  • Zinostatin