Nuclear drug delivery for cancer chemotherapy

J Control Release. 2011 Oct 30;155(2):227-36. doi: 10.1016/j.jconrel.2011.07.041. Epub 2011 Aug 6.


Nanosystems with unique physical and biological properties have been extensively explored for cancer targeted intracellular delivery of small-molecular chemotherapeutic drugs to increase their therapeutic efficacies and to minimize their side effects. A large number of anticancer drugs are DNA-toxins that bind nuclear DNA or its associated enzymes to exert their cytotoxicity to cancer cells. After entering tumor cells, they need to be further delivered to the nucleus for actions. Herein, we discuss the biological barriers and summarize recent progress of nuclear drug delivery for cancer chemotherapy, emphasizing strategies that appear useful for design of vehicles capable of delivering drugs to the nucleus, particularly for in vivo applications. The existing obstacles or problems that need to be overcome before successful applications of nuclear drug delivery for cancer chemotherapy are also discussed.

Publication types

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

MeSH terms

  • Animals
  • Antineoplastic Agents / administration & dosage*
  • Antineoplastic Agents / pharmacokinetics
  • Antineoplastic Agents / therapeutic use
  • Cell Membrane / metabolism
  • Cell Nucleus / metabolism*
  • Chemistry, Pharmaceutical
  • Cytosol / metabolism
  • Drug Carriers / chemistry
  • Drug Delivery Systems*
  • Drug Resistance, Multiple
  • Drug Resistance, Neoplasm
  • Endocytosis
  • Humans
  • Nanoparticles / chemistry*
  • Neoplasms / drug therapy
  • Neoplasms / metabolism*


  • Antineoplastic Agents
  • Drug Carriers