Prodrugs pp 1083-1110 | Cite as

Formulation Challenges of Prodrugs

  • Robert G. Strickley
  • Reza Oliyai
Part of the Biotechnology: Pharmaceutical Aspects book series (PHARMASP, volume V)


This chapter aims to review and highlight some examples of challenges and limitations of formulating prodrugs for clinical and commercial development. The reader should note that the existing literature on the formulation and pharmaceutical development of prodrugs is somewhat limited as pharmaceutical companies tend to not publish pharmaceutical development data. While the prodrug strategy has been used to overcome various drug delivery issues, it tends to present various formulation challenges. These challenges arise from various physicochemical properties of the prodrug as compared to the parent drug such as:
  • Lack of chemical stability, often the drug-promoiety linker

  • Potential for the formation of degradation by-products that are reactive intermediates resulting in secondary degradation pathways

  • Aqueous solubility

  • Aqueous solubility of degradation products

  • Disruption of solid state crystallinity

  • •|Polymorphism


Benzyl Alcohol Adefovir Dipivoxil Ester Prodrug Testosterone Enanthate Testosterone Undecanoate 


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© American Association of Pharmaceutical Scientists 2007

Authors and Affiliations

  • Robert G. Strickley
  • Reza Oliyai

There are no affiliations available

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