pH-sensitive microcapsules containing clarithrocin-loaded lipid nanoarriers for the treatment of H. pylori in gastric deseases.

SÁNCHEZ MEJÍA, SOFIA VALERIA; ARRUA, EVA CAROLINA; TRINCADO, VALERIA; MORALES, JAVIER

Encuentro; 6ta Reunión Internacional de Ciencias Farmacéuticas (RICiFa 2020+1); 2021

Helicobacter pylori (H. pylori) is a bacterium involved in the pathogenesis of severe gastric diseases being the most frequent cause of infection-induced cancer worldwide(1). H. pylori colonizes the gastric mucosa increasing its pH from 1-3 to 5-7. Antimicrobial agents, as clarithromycin (CLA), are essential to eradicate H. pylori infection(2). Thus, the objective of this research is to develop and characterize CLA-loaded lipid nanocarriers (CLA-LNC), incorporate them into alginate-carrageenan microcapsules for pH-specific localized release of CLA, determine the entrapment efficiency (%EE) and the in vitro release at pH 2 and pH 4.CLA-LNC were successfully developed by the phase inversion-based process. The physicochemical characteristics of CLA-LNC such as size (110.2nm), PdI (0.022) and zeta potential (-16.96mV) suggest a stable system with suitable characteristics for drug delivery. pH-sensitive alginate-carrageenan microcapsules containing CLA-LNC were obtained by complex coacervation. The %EE of CLA in the LNC was 85.73% and microcapsules were able to encapsulate 76.87% of CLA-LNC revealing a high incorporation of CLA in both systems. Moreover the poor release of CLA from microcapsules at pH 2 (about 20%), and the effective release at pH 7.4 suggest that this is a promising formulation for the administration of CLA to H. pylori treatment in gastric diseases.