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Smart drug delivery against Helicobacter pylori: pectin-coated, mucoadhesive liposomes with antiadhesive activity and antibiotic cargo

  • Applied microbial and cell physiology
  • Published:
Applied Microbiology and Biotechnology Aims and scope Submit manuscript

Abstract

The first step in the development of Helicobacter pylori pathogenicity is the receptor-mediated adhesion to the gastric epithelium. Inhibition of outer membrane proteins of H. pylori (e.g. BabA) by antiadhesive drugs will contribute to reduced recolonization and infection. Pectin from apple inhibits the BabA and LPS-mediated adhesion of H. pylori to human stomach cells. Pectin-coated liposomes with encapsulated amoxicillin were characterized for polydispersity, zeta potential, encapsulation efficiency, stability, and amoxicillin release. Coated liposomes did not influence the viability of AGS and HT29-MTX cells up to 100 μg/mL but exert cytotoxicity against H. pylori at 10 μg/mL. Pectin-coating of liposomes provoked direct interaction and subsequent binding of the particles to surface structures of H. pylori, and interaction with mucus from porcine stomach and mucus secreted by HT29-MTX cells. Laser scanning microscopy of H. pylori and AGS cells together with liposomes indicated co-aggregation. The mucoadhesive effect seems interesting as stomach cells are covered by a mucus layer. H. pylori is able to penetrate and cross the mucin rapidly to reach pH-neutral epithelium to escape the acidic environment, followed by interaction with epithelial cells. In summary, all experimental evidence is consistent with a specific interaction of pectin-coated liposomes with mucins and surface structures of H. pylori. As the coated liposomes show mucoadhesion to the negatively charged mucins, docking to stomach mucin, mucus penetration, and recognition of and adhesion to H. pylori, they can be considered a novel type of multifunctional drug carriers for local antibiotic therapy against H. pylori.

Key points

• Smart, multifunctional mucoadhesive liposomes

• Specific targeting against BabA/LPS of Helicobacter pylori

• Inhibition of bacterial adhesion of H. pylori to human host cells

• Release of antibiotic cargo

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Acknowledgements

The authors thank Prof. Dr. K. Langer, University of Münster, for the HT29-MTX cells and for using Zetasizer.

Funding

The study had been fully financed from intramural grants of the University of Münster (no grant numbers available).

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Authors and Affiliations

  1. Institute of Pharmaceutical Biology and Phytochemistry, University of Münster, Corrensstraße 48, 48149, Münster, Germany

    Maren Gottesmann & Andreas Hensel

  2. School of Food Science and Nutrition, University of Leeds, Leeds, LS2 9JT, UK

    Francisco M. Goycoolea

  3. Institute of Medical Biochemistry, University of Münster, Von-Esmach-Straße, 56, Münster, Germany

    Tim Steinbacher

  4. Institute of Plant Biology and Biotechnology, University of Münster, Schlossplatz 8, 48143, Münster, Germany

    Tamara Menogni

Authors
  1. Maren Gottesmann
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  2. Francisco M. Goycoolea
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  3. Tim Steinbacher
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  4. Tamara Menogni
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  5. Andreas Hensel
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Contributions

MG performed experiments and made substantial contributions to acquisition, analysis, and interpretation of data; TS helped with confocal laser scanning microscopy; TM helped during the liposome preparation; FG was involved in experiments and revised and discussed the MS; AH designed the study and has been involved in drafting and revising the MS.

Corresponding author

Correspondence to Andreas Hensel.

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Gottesmann, M., Goycoolea, F.M., Steinbacher, T. et al. Smart drug delivery against Helicobacter pylori: pectin-coated, mucoadhesive liposomes with antiadhesive activity and antibiotic cargo. Appl Microbiol Biotechnol 104, 5943–5957 (2020). https://doi.org/10.1007/s00253-020-10647-3

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  • DOI: https://doi.org/10.1007/s00253-020-10647-3

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