Lipid-Based Anticancer Prodrugs

  • L. Harivardhan Reddy
  • Patrick Couvreur
Part of the Macromolecular Anticancer Therapeutics book series (CDD&D)


Lipids are biomolecules constituting the principal components of the living cells. Chemical association of drug molecules with lipids may alter their in vivo pharmacokinetics/pharmacodynamics and even, in certain cases, their toxicity profile. Successful design of a lipid–anticancer prodrug highly depends on the lipid’s carbon chain length, on the configuration of the double bonds, and on the location and nature of the covalent linkage with the drug. In general, well–designed lipid–anticancer prodrugs display better cellular penetration, controlled drug release property, better pharmacokinetics, improved tumor accumulation, and better cellular penetration leading to enhanced therapeutic activity and lower toxicity. Thus, the better therapeutic index results from a controlled exposure of the conjugated drug to the biological environment. Noteworthy, in the treatment of cancers, drug resistance is one of the most important clinical concerns. Thus, there is a real need to develop new chemical entities able to bypass the resistance factors, thus displaying an improved therapeutic response. In this context, lipid prodrugs of anticancer agents are important actors in overcoming the resistance to cancers, at least at the preclinical stage. This chapter aims to discuss in detail about the various lipids employed in anticancer drug delivery applications. The current stage of their development either preclinical or clinical is also presented.


Valproic Acid Conjugate Linoleic Acid Anticancer Activity Conjugate Linoleic Acid Isomer Elaidic Acid 
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.



ATP-binding cassette


Adenine nucleotide translocator


1-β-d-Arabinofuranosylcytosine, cytarabine


1-β-d-Arabinofuranosylcytosine triphosphate


Adenosine triphosphate


Butyric acid


Cholesterol–polyethyleneglycol 2000


Conjugated linoleic acid


deoxycytidine kinase




Docosahexaenoic acid


Deoxyribonucleic acid


Essential fatty acid


Eicosapentaenoic acid


Gemcitabine monophosphate


gemcitabine triphosphate


Human epidermal growth factor receptor-2




Low-density lipoprotein


Multidrug resistant


Mitomycin C


Maximal tolerable dose




Nicotinamide adenine dinucleotide


Non-small cell lung cancer


Protein tyrosine kinase


Polyunsaturated fatty acid


Rat natural killer-16


Squalenoyl gemcitabine




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© Springer Science+Business Media, LLC 2010

Authors and Affiliations

  1. 1.Faculté de PharmacieUniversité de Paris-Sud XIChâtenay-Malabry CedexFrance
  2. 2.Sanofi-aventisVitry-sur-seineFrance

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