Development of Lecithin Nanoparticle Formulation as Rifampicin Delivery System

The inability of antimicrobial agents to penetrate a target cell presents a limitation to the intracellular treatment of latent bacterial infection. The localization of bacterial pathogens, such as Staphylococcus aureus , within the cell protects them from pathogen inactivation and decreases the efficiency of antimicrobial agent. This study aims to develop an intracellular transport of rifampicin using nanoparticles formed from lecithin and artinM (NP-AM). The nanoparticles were formed through the dispersal of lipid-phase mixture consisting of lecithin, oleic acid, and rifampicin mixed with water and stabilized using an emulsifying agent. ArtinM was absorbed to the surface of the nanoparticles through ionic interaction. The optimal formula was determined using the Box-Behnken design based on the lecithin and oleic acid, rifampicin, and polysorbate 80 concentrations as the experimental variables and the particle diameter, entrapment efficiency (EE), and drug loading (DL) as the response variable. The optimum formulation produced a particle diameter of 298.8±35.2 nm with a polydispersity index of 0.307±0.062, an EE of 47.2±5.5%, and a DL of 13.0±2.5%. The NP-AM released the loaded rifampicin at pH between 5.2-7.4 and able to penetrate fibroblast cells in vitro . The artinM conjugated lecithin nanoparticles is potential vehicles as rifampicin delivery system for intracellular bacterial pathogen therapy.