Cosmetic-Derived Mannosylerythritol Lipid-B-Phospholipid Nanoliposome: An Acid-Stabilized Carrier for Efficient Gastromucosal Delivery of Amoxicillin for In Vivo Treatment of Helicobacter pylori

Wu, YP; Geng, JY; Cheng, XH; Yang, Y; Yu, Y; Wang, LL; Dong, QJ; Chi, Z; Liu, CG

Abstract

Helicobacter pylori infection is a leading cause of gastritis and peptic ulcer. Current treatments for H. pylori are limited by the increase in antibiotic-resistant strains and low drug delivery to the infection site, indicating the need for effective delivery systems of antibiotics. Although liposomes are the most successful drug delivery carriers that have already been applied commercially, their acidic stability still stands as a problem. Herein, we developed a novel nanoliposome using cosmetic raw materials of mannosylerythritol lipid-B (MEL-B), soy bean lecithin, and cholesterol, namely, LipoSC-MELB. LipoSC-MELB exhibited enhanced stability under the simulated gastric-acid condition, owing to its strong intermolecular hydrogen-bond interactions caused by the incorporation of MEL-B. Moreover, amoxicillin-loaded LipoSC-MELB (LipoSC-MELB/AMX) had a particle size of approximately 100 nm and exhibited sustained drug release under varying pH conditions (pH 3-7). Besides, LipoSC-MELB/AMX exhibited significantly higher anti-H. pylori and anti-H. pylori biofilm activity as compared with free AMX. Furthermore, LipoSC-MELB was able to carry AMX across the barriers of gastric mucus and H. pylori biofilms. Remarkably, in vivo assays indicated that LipoSC-MELB/AMX was effective in treating H. pylori infection and its associated gastritis and gastric ulcers. Overall, the findings of this study showed that LipoSC-MELB was effective for gastromucosal delivery of amoxicillin to improve its bioavailability for the treatment of H. pylori infection.

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