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In vitro behavior of marine lipid-based liposomes. Influence of pH, temperature, bile salts, and phospholipase A2

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Lipids

Abstract

To deliver polyunsaturated fatty acids (PUFA) by the oral route, liposomes based on a natural mixture of marine lipids were prepared by filtration and characterized in media that mimic gastrointestinal fluids. First the influence of large pH variations from 1.5–2.5 (stomach) to 7.4 (intestine) at the physiological temperature (37°C) was investigated. Acidification of liposome suspensions induced instantaneous vesicle aggregation, which was partially reversible when the external medium was further neutralized. Simultaneously, complex morphological bilayer rearrangements occurred, leading to the formation of small aggregates. These pH- and temperature-dependent structural changes were interpreted in terms of osmotic shock and lipid chemical alterations, i.e., oxidation and hydrolysis, especially in the first hours of storage. Besides, oxidative stability was closely related to the state of liposome aggregation and the supramolecular organization (vesicles or mixed micelles). The effects of bile salts and phospholipase A2 (PLA2) on the liposome structures were also studied. Membrane solubilization by bile salts was favored by preliminary liposome incubation in acid conditions. PLA2 showed a better activity on liposome structures than on the corresponding mixed lipid-bile salt micelles. As a whole, in spite of slight morphological modifications, vesicle structures were preserved after an acid stress and no lipid oxidation products were detected during the first 5 h of incubation. Thus, marine lipids constituted an attractive material for the development of liposomes as potential oral PUFA supplements.

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Abbreviations

BS:

bile salt

cmc:

critical micellar concentration

DHA:

docosahexaenoic acid

EPA:

eicosapentaenoic acid

GC:

gas chromatography

GEC:

gel exclusion chromatography

LPC:

lysophosphatidylcholine

LPL:

lysophosphatidylethanolamine

OD:

optical density

PC:

phosphatidylcholine

PE:

phosphatidylethanolamine

PLA2 :

phospholipase A2

PL:

phospholipids

PUFA:

polyunsaturated fatty acids

QELS:

quasi-elastic light scattering

TG:

triglycerides

TLC:

thin-layer chromatography

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Authors and Affiliations

  1. ISTAB, Laboratoire de Lipochimie Alimentaire, Université Bordeaux I, Avenue des Facultés, F-33405, Talence Cedex, France

    Fabienne Nacka, Maud Cansell & Bernard Entressangles

Authors
  1. Fabienne Nacka
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  2. Maud Cansell
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  3. Bernard Entressangles
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Correspondence to Maud Cansell.

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Nacka, F., Cansell, M. & Entressangles, B. In vitro behavior of marine lipid-based liposomes. Influence of pH, temperature, bile salts, and phospholipase A2 . Lipids 36, 35–42 (2001). https://doi.org/10.1007/s11745-001-0665-0

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  • DOI: https://doi.org/10.1007/s11745-001-0665-0

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