Prodrugs pp 541-572 | Cite as

Prodrugs for Liver-targeted Drug Delivery

  • Mark D. Erion
Part of the Biotechnology: Pharmaceutical Aspects book series (PHARMASP, volume V)


The liver is the organ in the body primarily responsible for maintaining a continuous supply of glucose, lipids, and other important metabolic substrates to peripheral tissues (Kahl, 1999). The liver also helps to control the circulating levels of certain amino acids, ketone bodies, free fatty acids, lipoproteins, and some hormones (e.g., insulin, steroids, T3) and plays an important role in the detoxification and excretion of various xenobiotics. Chronic liver diseases such as viral hepatitis and liver cancer, as well as some metabolic diseases associated with the liver such as non-alcoholic steatohepatitis, injure the liver. Chronic liver injury can lead sequentially to impaired liver function, liver failure, and death. Drugs for treating liver diseases are often limited by tolerability and extra-hepatic safety concerns, which prevent their use at maximally effective doses. Targeting drugs to the liver may circumvent some of these limitations and enable more effective therapies. This chapter reviews the liver-targeting strategies explored to date and, more specifically, the strengths and weaknesses of various prodrug strategies used for liver-specific drug delivery.


Bile Acid Adefovir Dipivoxil Vinyl Ketone Bile Acid Transporter Woodchuck Hepatitis Virus 
These keywords were added by machine and not by the authors. This process is experimental and the keywords may be updated as the learning algorithm improves.


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© American Association of Pharmaceutical Scientists 2007

Authors and Affiliations

  • Mark D. Erion
    • 1
  1. 1.Metabasis Therapeutics, Inc.La Jolla

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