An pH-responsive liposome for the targeted treatment of Helicobacter pylori

Objectives With the increase of <i>Helicobacter pylori</i> (<i>H. pylori</i>) drug resistance, it is increasingly difficult to cure <i>H. pylori</i> fundamentally. Frequent and excessive use of antibiotics can lead to disturbances in the intestinal flora and even inflammatory bowel disease, so new drugs are urgently needed. Luteolin (LUT) has been found to have antimicrobial effects, but its water solubility is very low, and the antimicrobial effect is not ideal. To improve the water solubility of LUT and enhance its antibacterial activity, we encapsulated it with liposomes and coated it with chitosan quaternary ammonium salts to increase its targeting and acid responsiveness. Results Compared with LUT, H-L-NPs solubility is significantly improved, and the MIC is reduced by 1024 times, which is also effective against drug-resistant strains. The effect of <i>in vivo</i> treatment is significantly better than that of clinical triple therapy. In addition, H-L-NPs have the advantages of high safety and specificity, which can target the treatment of gastric <i>H. pylori</i> and maintain the diversity of intestinal microbiota, and <i>H. pylori</i> is not easy to develop drug resistance, making it a very promising anti-<i>H. pylori</i> lead. In conclusion, H-L-NPs greatly improved the antimicrobial activity of LUT <i>in vivo</i> and <i>in vitro</i>, and possessed the antimicrobial advantages of high targeting, acid responsiveness, specificity, and low toxicity. It is a kind of <i>anti-H. pylori</i> agent with a broad application prospect.