Berberine-Loaded Targeted Nanoparticles as Specific Helicobacter Pylori Eradication Therapy: In Vitro and In Vivo Study

Abstract

Aim: The aim of this work was to develop fucose-conjugated nanoparticles and control the release of berberine, and demonstrate that these particles come into contact with Helicobacter pylori and enhance the suppressive effect of berberine on H. pylori growth. Materials & methods: Fucose–chitosan/heparin nanoparticle-encapsulated berberine was prepared and delivery efficiency was monitored by confocal laser scanning microscopy. Anti-H. pylori activities were investigated by determining the calculated bacterial colonies and immunohistochemistry staining analysis. Results: Analysis of a simulated gastrointestinal medium indicated that the proposed drug carrier effectively controls the release of berberine, which interacts specifically at the site of H. pylori infection, and significantly increases berberine’s suppressive effect on H. pylori growth. In an in vivo study, the berberine-loaded fucose-conjugated nanoparticles exhibited an H. pylori clearance effect. Conclusion: These findings indicate that berberine-loaded fucose-conjugated nanoparticles exert an H. pylori clearance effect and effectively reduce gastric inflammation in an H. pylori-infected animal study.

Original submitted 19 November 2013; Revised submitted 4 March 2014

Keywords::

• berberine
• fucose-conjugated nanoparticle
• gastric inflammation
• Helicobacter pylori
• heparin

Financial & competing interests disclosure

This work was supported by grants from the National Science Council (NSC100-2628-E-039-003-MY3) and China Medical University (CMU-101-S-22). The Leica SP2 Confocal Spectral microscopy (Leica, Solms, Germany) and ZS90 Zetasizer (Malvern Instruments, Malvern, UK) apparatus supported by the Medical Research Core Facilities Center, Office of Research and Development, China Medical University (Shenyang, China), were gratefully acknowledged. The authors have no other relevant affiliations or financial involvement with any organization or entity with a financial interest in or financial conflict with the subject matter or materials discussed in the manuscript apart from those disclosed.

No writing assistance was utilized in the production of this manuscript.

Ethical conduct of research

The authors state that they have obtained appropriate institutional review board approval or have followed the principles outlined in the Declaration of Helsinki for all human or animal experimental investigations. In addition, for investigations involving human subjects, informed consent has been obtained from the participants involved.

Additional information

Funding

This work was supported by grants from the National Science Council (NSC100-2628-E-039-003-MY3) and China Medical University (CMU-101-S-22). The Leica SP2 Confocal Spectral microscopy (Leica, Solms, Germany) and ZS90 Zetasizer (Malvern Instruments, Malvern, UK) apparatus supported by the Medical Research Core Facilities Center, Office of Research and Development, China Medical University (Shenyang, China), were gratefully acknowledged. The authors have no other relevant affiliations or financial involvement with any organization or entity with a financial interest in or financial conflict with the subject matter or materials discussed in the manuscript apart from those disclosed. No writing assistance was utilized in the production of this manuscript.