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. 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.

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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

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