Prodrug-based intracellular delivery of anticancer agents

L Bildstein1, C Dubernet, P Couvreur

  • 1UMR CNRS 8612, IFR 141-ITFM, Faculté de Pharmacie, University Paris-Sud, Châtenay-Malabry 92296, France.

Insights

Anticancer prodrugs utilize altered cell uptake and intracellular release for enhanced drug delivery. This review highlights design strategies for efficient delivery of polymer, protein, and lipid-based prodrugs.

Area of Science:

  • Biochemistry
  • Pharmacology
  • Nanotechnology

Background:

  • Prodrugs are widely used anticancer agents.
  • Existing reviews lack focus on cellular uptake and intracellular release mechanisms.

Purpose of the Study:

  • To review anticancer prodrugs focusing on cellular uptake and intracellular drug release.
  • To highlight prodrug design for efficient intracellular drug delivery.

Main Methods:

  • Review of literature on parenterally administered anticancer prodrugs.
  • Analysis of prodrugs based on synthetic polymers, proteins, and lipids.
  • Discussion of chemical basis, uptake, activation, and clinical results.

Main Results:

  • Prodrug conjugation alters cell uptake pathways.
  • Intracellular drug release mechanisms are crucial for efficacy.
  • Design considerations impact intracellular drug delivery efficiency.

Conclusions:

  • Prodrug design is key for effective anticancer therapy.
  • Understanding cellular interactions enhances prodrug development.
  • Targeting strategies and stimuli-responsive systems show promise.

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