The prospects of lipidic prodrugs: An old approach with emerging an future

Arik Dahan, Milica Markovic, Aaron Aponick, Ellen M. Zimmermann, Shimon Ben-Shabat

Research output: Contribution to journalReview articlepeer-review

12 Scopus citations


Nowadays, prodrugs are no longer used as a last resort, rather, they are intentionally designed at the early stages of drug development. Lipidic prodrug strategy, where a drug moiety is covalently bound to a lipid carrier, was initially proposed half a century ago, yet, this approach still remains to be explored. Lipidic prodrugs can join physiological lipid metabolic pathways, and hence provide drug targeting via lymphatic transport or site-specific drug release, improve drugs' pharmacokinetic profile, overcome obstacles originating from biological barriers and bypass hepatic first-pass metabolism. Physiological pathways of lipid processing, uses of different lipidic prodrugs and their clinical benefits are overviewed. Overall, lipidic prodrugs present a promising approach for overcoming different obstacles and fulfilling various unmet needs in drug delivery/targeting.

Original languageEnglish
Pages (from-to)2563-2571
Number of pages9
JournalFuture Medicinal Chemistry
Issue number19
StatePublished - 1 Jan 2019


  • biopharmaceutics
  • cholesterol
  • drug delivery
  • fatty acid
  • lipid
  • lymphatic drug transport
  • phospholipid
  • prodrug
  • triglyceride

ASJC Scopus subject areas

  • Molecular Medicine
  • Pharmacology
  • Drug Discovery


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