Effect of formulation method, lipid composition and PEGylation on vesicle lamellarity: a small-angle neutron scattering study
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Published version
Author(s)
Type
Journal Article
Abstract
Liposomes are well-established systems for drug delivery and biosensing applications. The design of a liposomal carrier requires careful choice of lipid composition and formulation method. These determine many vesicle properties including lamellarity, which can have a strong effect on both encapsulation efficiency and the efflux rate of encapsulated active compounds. Despite this, a comprehensive study on how the lipid composition and formulation method affect vesicle lamellarity is still lacking. Here, we combine small-angle neutron scattering and cryogenic transmission electron microscopy to study the effect of three different well-established formulation methods followed by extrusion through 100 nm polycarbonate membranes on the resulting vesicle membrane structure. Specifically, we examine vesicles formulated from the commonly used phospholipids 1-palmitoyl-2-oleoyl-sn-glycero-3-phosphocholine (POPC), 1,2-dipalmitoyl-sn-glycero-3-phosphocholine (DPPC) and 1,2-dioleoyl-sn-glycero-3-phosphocholine (DOPC) via film hydration followed by (i) agitation on a shaker or (ii) freeze–thawing, or (iii) the reverse-phase evaporation vesicle method. After extrusion, up to half of the total lipid content is still assembled into multilamellar structures. However, we achieved unilamellar vesicle populations when as little as 0.1 mol % PEG-modified lipid was included in the vesicle formulation. Interestingly, DPPC with 5 mol % PEGylated lipid produces a combination of cylindrical micelles and vesicles. In conclusion, our results provide important insights into the effect of the formulation method and lipid composition on producing liposomes with a defined membrane structure.
Date Issued
2019-05-07
Date Acceptance
2019-03-29
Citation
Langmuir, 2019, 35 (18), pp.6064-6074
ISSN
0743-7463
Publisher
American Chemical Society
Start Page
6064
End Page
6074
Journal / Book Title
Langmuir
Volume
35
Issue
18
Copyright Statement
© 2019 American Chemical Society.
ACS AuthorChoice - This is an open access article published under a Creative Commons Attribution (CC-BY) License, which permits unrestricted use, distribution and reproduction in any medium, provided the author and source are cited.
ACS AuthorChoice - This is an open access article published under a Creative Commons Attribution (CC-BY) License, which permits unrestricted use, distribution and reproduction in any medium, provided the author and source are cited.
Sponsor
Engineering & Physical Science Research Council (E
Medical Research Council (MRC)
Wellcome Trust
Grant Number
EP/K031953/1
538559, MR/P024378/1
098411/Z/12/Z
Subjects
MD Multidisciplinary
Chemical Physics
Publication Status
Published
Date Publish Online
2019-04-12