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Liver-targeted delivery based on prodrug: passive and active approaches

Jiaqi Chen1, Yingrui Yao1, Xiaoran Mao1

  • 1Key Laboratory of Therapeutic Substance of Traditional Chinese Medicine, Tianjin University of Traditional Chinese Medicine, Tianjin, China.

Journal of Drug Targeting
|July 29, 2024
PubMed
Abstract

Insights

Liver-targeted prodrugs enhance treatment efficacy and reduce side effects for liver diseases by utilizing passive and active targeting strategies. Future research should optimize drug design and targeting efficiency for clinical success.

Area of Science:

  • Pharmacology
  • Drug Delivery Systems
  • Hepatology

Background:

  • The liver is a primary drug target, but liver diseases like NAFLD and HCC pose global health challenges.
  • Current treatments lack specificity, leading to suboptimal efficacy and increased side effects.
  • Non-alcoholic fatty liver disease (NAFLD) and hepatocellular carcinoma (HCC) are significant health concerns.

Purpose of the Study:

  • To review advancements in liver-targeted prodrug design.
  • To focus on passive and active targeting strategies for improved therapeutic outcomes.
  • To offer insights into developing effective liver-targeted therapies.

Main Methods:

  • Systematic literature search across major scientific databases (PubMed, Web of Science, etc.).
  • Focus on targeting mechanisms including the Enhanced Permeability and Retention (EPR) effect and tumor microenvironment.
  • Inclusion of active targeting via specific transporters and receptors.

Main Results:

  • Passive targeting leverages the EPR effect and tumor characteristics for drug enrichment.
  • Active targeting utilizes specific ligands to bind liver surface receptors for precise delivery.
  • Successful examples include small molecules, peptides, antibodies, and nanoparticles as carriers.

Conclusions:

  • Liver-targeted prodrugs significantly improve treatment efficacy and reduce side effects.
  • Future work requires balancing targeting strategies and optimizing drug design for clinical use.
  • Developing novel targeting molecules and understanding liver-specific receptors are key.
Keywords:
Liver-targeted prodrugsactive and passive targeting strategiesconjugatesdrug delivery systemsself- assemblies

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