Liposomal Formulation of Retinoids Designed for Enzyme Triggered Release

Palle Jacob Pedersen, Sidsel Kramshøj Adolph, Arun Kumar Subramanian, A. Arouri, Thomas Lars Andresen, O.G. Mouritsen, Robert Madsen, M.W. Madsen, Günther H.J. Peters, Mads Hartvig Clausen

Research output: Contribution to journalJournal articleResearchpeer-review


The design of retinoid phospholipid prodrugs is described based on molecular dynamics simulations and cytotoxicity studies of synthetic retinoid esters. The prodrugs are degradable by secretory phospholipase A(2) IIA and have potential in liposomal drug delivery targeting tumors. We have synthesized four different retinoid phospholipid prodrugs and shown that they form particles in the liposome size region with average diameters of 94-118 nm. Upon subjection to phospholipase A(2), the lipid prodrugs were hydrolyzed, releasing cytotoxic retinoids and lysolipids. The formulated lipid prodrugs displayed IC50 values in the range of 3-19 mu M toward HT-29 and Colo205 colon cancer cells in the presence of phospholipase A(2), while no significant cell death was observed in the absence of the enzyme.
Original languageEnglish
JournalJournal of Medicinal Chemistry
Issue number9
Pages (from-to)3782-3792
Number of pages11
Publication statusPublished - 2010


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