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Liposome formulations of hydrophobic drugs


Schwendener, Reto A; Schott, Herbert (2017). Liposome formulations of hydrophobic drugs. In: D'Souza, Gerard G M. Liposomes, Methods and Protocols, Second Edition. New York, NY, USA: Springer, 73-82.

Abstract

Here we report methods of preparation for liposome formulations containing lipophilic drugs. In contrast to the encapsulation of water soluble compounds into the entrapped aqueous volume of a liposome, drugs with lipophilic properties are incorporated into the phospholipid bilayer membrane. Water-soluble molecules, for example cytotoxic or antiviral nucleosides can be transformed into lipophilic compounds by attachment of long alkyl chains, allowing their stable incorporation into liposome membranes and taking advantage of the high loading capacity lipid bilayers provide for lipophilic molecules. We created a new class of cytotoxic drugs by chemical transformation of the hydrophilic drugs cytosine-arabinoside (ara-C), 5-fluoro-deoxyuridine (5-FdU), and ethinylcytidine (ETC) into lipophilic compounds and their formulation in liposomes.The concept of chemical modification of water-soluble molecules by attachment of long alkyl chains and their stable incorporation into liposome bilayer membranes represent a very promising method for the development of new drugs not only for the treatment of tumors or infections but also for many other diseases.

Abstract

Here we report methods of preparation for liposome formulations containing lipophilic drugs. In contrast to the encapsulation of water soluble compounds into the entrapped aqueous volume of a liposome, drugs with lipophilic properties are incorporated into the phospholipid bilayer membrane. Water-soluble molecules, for example cytotoxic or antiviral nucleosides can be transformed into lipophilic compounds by attachment of long alkyl chains, allowing their stable incorporation into liposome membranes and taking advantage of the high loading capacity lipid bilayers provide for lipophilic molecules. We created a new class of cytotoxic drugs by chemical transformation of the hydrophilic drugs cytosine-arabinoside (ara-C), 5-fluoro-deoxyuridine (5-FdU), and ethinylcytidine (ETC) into lipophilic compounds and their formulation in liposomes.The concept of chemical modification of water-soluble molecules by attachment of long alkyl chains and their stable incorporation into liposome bilayer membranes represent a very promising method for the development of new drugs not only for the treatment of tumors or infections but also for many other diseases.

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Additional indexing

Item Type:Book Section, refereed, original work
Communities & Collections:04 Faculty of Medicine > Institute of Molecular Cancer Research
07 Faculty of Science > Institute of Molecular Cancer Research
Dewey Decimal Classification:570 Life sciences; biology
610 Medicine & health
Uncontrolled Keywords:Liposomes Lipophilic drugs Lipophilic ara-C drugs NOAC Duplex drugs
Language:English
Date:2017
Deposited On:13 Feb 2017 11:09
Last Modified:08 Dec 2017 23:12
Publisher:Springer
Series Name:Methods in Molecular Biology
Number:1522
ISSN:1064-3745
ISBN:978-1-4939-6591-5
Additional Information:The final publication is available at Springer via https://doi.org/10.1007/978-1-4939-6591-5_6
Publisher DOI:https://doi.org/10.1007/978-1-4939-6591-5_6
PubMed ID:27837531

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