The role of lipid geometry in designing liposomes for the solubilisation of poorly water soluble drugs

Ali, M. Habib; Moghaddam, Behfar; Kirby, Daniel J.; Mohammed, Afzal R. and Perrie, Yvonne (2012). The role of lipid geometry in designing liposomes for the solubilisation of poorly water soluble drugs. International journal of pharmaceutics, in pre ,

Abstract

Liposomes are well recognised for their ability to improve the delivery of a range of drugs. More commonly they are applied for the delivery of water-soluble drugs, but given their structural attributes they can also be employed as solubilising agents for low solubility drugs as well as drug targeting agents. To further explore the potential of liposomes as solubilising agents, we have investigated the role of bilayer packaging in promoting drug solubilisation in liposome bilayers. The effect of alkyl chain length and symmetry was investigated to consider if using 'mis-matched' phospholipids could be used to create 'voids' within the bilayers, and enhance bilayer loading capacity. Lipid packing was investigated using Langmuir studies, which demonstrated that increasing the alkyl chain length enhanced lipid packing, with condensed monolayer forming, whilst asymmetric lipids formed less condensed monolayers. However this more open packing did not translate into improved drug loading, with the longer chain, condensed bilayers formed from long-chain, saturated lipids offering higher drug loading capacity. These studies demonstrate that liposomes formulated from longer chain, saturated lipids offer enhanced solubilisation capacity. However the molecular size, rather than lipophilicity, of the drug to be incorporated was also a key factor dominating bilayer incorporation efficiency.

Additional Information: Copyright © 2012. Published by Elsevier B.V.
Uncontrolled Keywords: liposomes, low soluble drugs, Bilayer drug loading, solubilisation, monolayer studies, Pharmaceutical Science
Published Date: 2012

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