Synthesis and characterization of amoxicillin-loaded polymeric nanocapsules as a drug delivery system targeting...

Helicobacter pylori (H. pylori) is well known as the main cause of gastritis, gastroduodenal ulcers, gastric mucosa-associated lymphoid tissue lymphoma, and gastric cancer. Approximately 50% of the world's population is infected with H. pylori. In Egypt, a high prevalence of H. pylori infections has been reported in the general population. This study aimed to prepare amoxicillin-loaded poly (ɛ-caprolactone) nanocapsules to increase its gastric stability and therapeutic activity of the molecule against H. pylori.

In this study, we used the water-oil-water double-emulsion technique to prepare spherical-shaped polymeric nanocapsules containing amoxicillin trihydrate as the core substance and biodegradable biocompatible poly (ɛ-caprolactone) as the shell material.

The encapsulation efficiency obtained was 97.2% ± 0.8%. The hydrodynamic diameter of the prepared nanocapsules was 287 ± 8 nm with a positive zeta potential. In vitro release studies indicated that the polymeric nanocapsules showed decreased release percentages at pH 1.2, simulating the gastric fluid while relatively increased release at pH 7.0 where the H. pylori reside. The in vitro antibacterial assay showed better efficiency for amoxicillin nanocapsules than for the uncapsulated free amoxicillin, no efficiency was detected for the PCL nanocapsules indicated that the antibacterial due to amoxicillin alone. Cytotoxicity studies demonstrated less cytotoxicity for the polymeric nanocapsules in comparison with amoxicillin.

In conclusion, we have demonstrated that biodegradable polymeric nanocapsules are useful drug delivery agents for increasing the gastric stability and therapeutic activity of amoxicillin trihydrate against H. pylori.