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Published on: June 18, 2016
Glycosylated liposomes against Helicobacter pylori: behavior in acidic conditions
Pierre-Louis Bardonnet1, Vincent Faivre, Paul Boullanger
1ISPB - Université Lyon I, France.
Abstract:
Helicobacter pylori was isolated in 1982 and confirmed as a gastric pathogenic agent at the end of the 1980s. The present work deals with liposomes formulations in which are incorporated cholesteryl tetraethylene glycol oside as model ligands for H. pylori adhesins. This study is devoted to the behavior of liposomes in gastric conditions. The glycosylated vesicles are stable and the pH of the internal aqueous compartment remains close to 4 even through more acidic conditions are imposed to the external phase (pH 1.2-2). Such a pH gradient depends essentially on the nature of phospholipids used and is not extensively affected by the incorporation of the targeting agent. These aspects are particularly important to the development of liposome formulations against H. pylori, bacteria sensitive to antibiotics which are unstable in very acidic conditions.
Insights
Liposomes containing cholesteryl tetraethylene glycol oside show stability in acidic gastric conditions. This pH gradient is crucial for developing effective liposome formulations against Helicobacter pylori.
Area of Science:
- Biochemistry
- Microbiology
- Pharmaceutical Sciences
Background:
- Helicobacter pylori, identified in 1982, was confirmed as a gastric pathogen in the late 1980s.
- Developing effective treatments for H. pylori is challenging due to its pathogenicity and the instability of some therapeutic agents in acidic environments.
Purpose of the Study:
- To investigate the behavior of liposomes formulated with cholesteryl tetraethylene glycol oside in simulated gastric conditions.
- To assess the stability and pH gradient of these glycosylated liposomes for potential H. pylori therapeutic applications.
Main Methods:
- Formulation of liposomes incorporating cholesteryl tetraethylene glycol oside as model ligands for H. pylori adhesins.
- Evaluation of liposome stability and internal pH under highly acidic external conditions (pH 1.2-2).
Main Results:
- The glycosylated liposomes exhibited stability in acidic environments.
- A significant pH gradient was maintained, with the internal aqueous compartment pH remaining near 4.
- This pH gradient was primarily dependent on the phospholipid composition and minimally affected by the incorporated targeting agent.
Conclusions:
- The developed liposomes demonstrate stability and a crucial pH gradient in simulated gastric conditions.
- These findings are significant for advancing liposome-based drug delivery systems targeting H. pylori.
- The stability of these formulations is advantageous for delivering antibiotics sensitive to highly acidic environments.
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