Skip to main page content
U.S. flag

An official website of the United States government

Dot gov

The .gov means it’s official.
Federal government websites often end in .gov or .mil. Before sharing sensitive information, make sure you’re on a federal government site.

Https

The site is secure.
The https:// ensures that you are connecting to the official website and that any information you provide is encrypted and transmitted securely.

Access keys NCBI Homepage MyNCBI Homepage Main Content Main Navigation
. 2024 Jan 11;25(1):9.
doi: 10.1186/s40360-024-00731-z.

Sustain-release lipid-liquid crystal formulations of pexiganan against Helicobacter pylori infection: in vitro evaluation in C57BL/6 mice

Kiarash Ghazvini  1 , Hossein Kamali  2 , Hadi Farsiani  3 , Masoud Yousefi  3 , Masoud Keikha  4
Affiliations

Sustain-release lipid-liquid crystal formulations of pexiganan against Helicobacter pylori infection: in vitro evaluation in C57BL/6 mice

Kiarash Ghazvini et al. BMC Pharmacol Toxicol. .

Abstract

Introduction: The Gram-negative bacterium Helicobacter pylori, H. pylori, is associated with significant digestive disorders. However, the effectiveness of bacterial eradication is declining due to drug resistance. A potent anti-H. pylori activity is shown by the natural antimicrobial peptide pexiganan.

Objective: The current study aimed to evaluate the effectiveness of pexiganan and its lipid-liquid crystals (LLCs) in inducing Helicobacter pylori in mice.

Methods: In this experimental study, H. pylori infection was first induced in C57BL/6 mice. Secondly, the antibacterial efficacy of pexiganan and its LLCs formulations was investigated to eliminate H. pylori infection.

Results: The H. pylori infection could not be completely eradicated by pexiganan peptide alone. However, incorporating pexiganan within the LLC formulation resulted in an increased elimination of H. pylori. Under the H&E strain, the pexiganan-LLCs formulation revealed minimal mucosal alterations and a lower amount of inflammatory cell infiltration in the stomach compared to the placebo.

Conclusion: Clarithromycin was more effective than pexiganan at all tested concentrations. Furthermore, the pexiganan-loaded LLCs exhibited superior efficacy in curing H. pylori infection in a mouse model compared to pexiganan alone. This formulation can enhance H. pylori clearance while mitigating the adverse effects, typically associated with conventional drugs, leading to a viable alternative to current treatment options.

Keywords: C57BL/6; Cure rate: liquid crystal; Helicobacter pylori; Infection.

PubMed Disclaimer

Conflict of interest statement

The authors declare no competing interests.

Figures

Fig. 1
Fig. 1
Images of GDO-based pexiganan-LLCs under a polarized light microscope
Fig. 2
Fig. 2
The cumulative release rate of pexiganan for LLC-GDO in-vitro. Cla: Clarithromycin; Pex: Pexiganan; LLC-Pex: Lipid Liquid Crystal-Pexiganan. Our results suggest that both clarithromycin as well as pexiganan have initial burst release without vehicle; However, pexiganan incorporated within lipid-liquid crystal formulation has slow-release than with no vehicles. As shown, pexiganan and clarithromycin does reach to more than 90% of release before the initial 4 h; While, the lipid liquid crystal has controlled the release of pexignan. In this relation, there are 20% of loaded pexignan was released from lipid liquid crystal formulation
Fig. 3
Fig. 3
The evaluation of gastric bioadhesivity characteristics of pexiganan-LLCs
Fig. 4
Fig. 4
in vivo oral LD50 (median lethal dose) of pexiganan for C57BL/6 mice model
Fig. 5
Fig. 5
the assessment of clearance effectiveness of pexiganan against H. pylori infection based on urease activity tests
Fig. 6
Fig. 6
histopathological alteration grade in mice underwent intervention
See this image and copyright information in PMC

Similar articles

See all similar articles

References

    1. McColl KE. Helicobacter pylori infection. N Engl J Med. 2010;362(17):1597–604. doi: 10.1056/NEJMcp1001110. - DOI - PubMed
    1. Keikha M, Sahebkar A, Yamaoka Y, Karbalaei M. Helicobacter pylori cagA status and gastric mucosa-associated lymphoid tissue lymphoma: a systematic review and meta-analysis. J Health Popul Nutr. 2022;41(1):1–1. doi: 10.1186/s41043-021-00280-9. - DOI - PMC - PubMed
    1. Fan F, Wang Z, Li B, Zhang H. Effects of eradicating Helicobacter pylori on metachronous gastric cancer prevention: a systematic review and meta-analysis. J Eval Clin Pract. 2020;26(1):308–15. doi: 10.1111/jep.13179. - DOI - PubMed
    1. Keikha M, Askari P, Ghazvini K, Karbalaei M. Levofloxacin-based therapy as an efficient alternative for eradicating Helicobacter pylori infection in Iran: a systematic review and meta-analysis. J Global Antimicrob Resist. 2021. - PubMed
    1. Thung I, Aramin H, Vavinskaya V, Gupta S, Park JY, Crowe SE, Valasek MA, et al. The global emergence of Helicobacter pylori antibiotic resistance. Aliment Pharmacol Ther. 2016;43(4):514–33. doi: 10.1111/apt.13497. - DOI - PMC - PubMed