Anticancer double lipid prodrugs: Liposomal preparation and characterization

Research output: Contribution to journalJournal articleResearchpeer-review

The escape of encapsulated anticancer drugs from liposomes by passive diffusion often leads to suboptimal drug concentrations in the cancer tissue, therefore calling for effective trigger mechanisms to release the drug at the target. We investigated mixtures of lipid components that not only form stable liposomes, but also can be turned into active drugs by secretory phospholipase A2 (sPLA2), an enzyme that is upregulated in various cancer cells, without the necessity for conventional liposome drug loading. The liposomes are composed of a novel lipid-based retinoid prodrug premixed with saturated phospholipids. The prodrug is found to be miscible with phospholipids, and the lipid mixtures are shown to form liposomes with the desired size distribution. The preparation procedure, phase behavior, and physicochemical properties of the formed liposomes are described as a function of lipid composition. We show that the premixing of the prodrug with phospholipids can be used to modify the physicochemical properties of liposomal formulations. The results should prove useful for further exploration of the potential for using these novel lipid prodrugs in liposomal formulations for cancer treatment.

Original languageEnglish
JournalJournal of Liposome Research
Volume21
Issue number4
Pages (from-to)296-305
Number of pages10
ISSN0898-2104
DOIs
Publication statusPublished - 1 Dec 2011

    Research areas

  • Anticancer prodrug, Lipid mixture, NBDdithionite interaction, Secretory phospholipase A2 (sPLA2), Triggered drug release

ID: 230975666