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Issue 10, 2017
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Characterization of drug encapsulation and retention in archaea-inspired tetraether liposomes

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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.

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

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Publication details

The article was received on 31 des. 2016, accepted on 13 feb. 2017 and first published on 13 feb. 2017


Article type: Communication
DOI: 10.1039/C6OB02832B
Citation: Org. Biomol. Chem., 2017,15, 2157-2162
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    Characterization of drug encapsulation and retention in archaea-inspired tetraether liposomes

    G. Leriche, J. L. Cifelli, K. C. Sibucao, J. P. Patterson, T. Koyanagi, N. C. Gianneschi and J. Yang, Org. Biomol. Chem., 2017, 15, 2157
    DOI: 10.1039/C6OB02832B

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