Lipid conjugated prodrugs for enzyme-triggered liposomal drug delivery to tumors

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For some time we have been developing novel enzyme-triggered prodrugs for drug delivery targeting cancer. The liposomal prodrugs take advantage of the EPR effect to localize to tumors and of the local over-expression of secretory phospholipase A2 in tumors. Compared to conventional liposomal drug delivery systems, our prodrug-lipid conjugates have two main advantages: 1) the drugs are covalently linked to the lipids and thus leakage is circumvented and 2) the lipophilic bilayer of the formulated liposomes effectively shields the drugs from the aqueous environment in vivo. Consequently, the strategy accommodates therapeutic agents with otherwise unfavorable pharmacokinetic properties. We have designed and synthesized different prodrugs, including published examples using capsaicin, chlorambucil and all-trans retinoic acid as the cytotoxic agents. Currently, we are investigating more potent agents targeting nuclear receptors and structural proteins. The presentation will highlight various strategies and recent progress towards improved systems, including chemical synthesis, enzyme activity and cytotoxicity.
Original languageEnglish
JournalAmerican Chemical Society. Abstracts of Papers (at the National Meeting)
Pages (from-to)MEDI 20
Publication statusPublished - 2011
Event242nd National Meeting of the American-Chemical-Society (ACS) - Denver, CO, United States
Duration: 28 Aug 20111 Sep 2011
Conference number: 242


Conference242nd National Meeting of the American-Chemical-Society (ACS)
CountryUnited States
CityDenver, CO
Internet address

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