Characterization of drug encapsulation and retention in archaea-inspired tetraether liposomes

Geoffray Leriche, Jessica L. Cifelli, Kevin C. Sibucao, Joseph P. Patterson, Takaoki Koyanagi, Nathan C. Gianneschi, Jerry Yang*

*Corresponding author for this work

Research output: Contribution to journalArticlepeer-review

16 Scopus citations

Abstract

The passive leakage of small molecules across membranes is a major limitation of liposomal drug formulations. Here, we evaluate the leakage of 3 clinically used chemotherapeutic agents (cytarabine, methotrexate and vincristine) encapsulated in liposomes comprised of a synthetic, archaea-inspired, membrane-spanning tetraether lipid. Liposomes comprised of the pure tetraether lipid exhibited superior retention of both a neutrally and positively charged drug (up to an ∼9-fold decrease in the rate of drug leakage) compared to liposomes formed from a commercial diacyl lipid, while exhibiting a similar retention of a negatively charged drug that did not appreciably leak from either type of liposome. We also demonstrate that liposomes made of the archaea-inspired lipid can be used for the delivery of encapsulated small molecules into living cells.

Original languageEnglish (US)
Pages (from-to)2157-2162
Number of pages6
JournalOrganic and Biomolecular Chemistry
Volume15
Issue number10
DOIs
StatePublished - 2017

ASJC Scopus subject areas

  • Biochemistry
  • Physical and Theoretical Chemistry
  • Organic Chemistry

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