Targeted prodrugs in oral drug delivery: The modern molecular biopharmaceutical approach

Arik Dahan, Mustafa Khamis, Riad Agbaria, Rafik Karaman

Research output: Contribution to journalReview articlepeer-review

66 Scopus citations


Introduction: The molecular revolution greatly impacted the field of drug design and delivery in general, and the utilization of the prodrug approach in particular. The increasing understanding of membrane transporters has promoted a novel 'targeted-prodrug' approach utilizing carrier-mediated transport to increase intestinal permeability, as well as specific enzymes to promote activation to the parent drug. Areas covered: This article provides the reader with a concise overview of this modern approach to prodrug design. Targeting the oligopeptide transporter PEPT1 for absorption and the serine hydrolase valacyclovirase for activation will be presented as examples for the successful utilization of this approach. Additionally, the use of computational approaches, such as DFT and ab initio molecular orbital methods, in modern prodrugs design will be discussed. Expert opinion: Overall, in the coming years, more and more information will undoubtedly become available regarding intestinal transporters and potential enzymes that may be exploited for the targeted modern prodrug approach. Hence, the concept of prodrug design can no longer be viewed as merely a chemical modification to solve problems associated with parent compounds. Rather, it opens promising opportunities for precise and efficient drug delivery, as well as enhancement of treatment options and therapeutic efficacy.

Original languageEnglish
Pages (from-to)1001-1013
Number of pages13
JournalExpert Opinion on Drug Delivery
Issue number8
StatePublished - 1 Aug 2012


  • DFT and ab initio calculations
  • Membrane transporters
  • Molecular biopharmaceutics
  • Passive/active intestinal permeability
  • Prodrug activation
  • Targeted prodrug approach

ASJC Scopus subject areas

  • Pharmaceutical Science


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