Polycaprolactone based nano-carrier for co-administration of moxifloxacin and rutin and its In-vitro evaluation for sepsis

Abstract

Clinically, complicated intra-abdominal infections (cIAIs) covers a broad spectrum peritonitis to acute appendicitis mainly associated with perforations in ischemic bowel. Antibiotics involved in treatment of cIAIs, possibly involved in pathophysiological initiation of sepsis by destructing the cell wall of microorganism and liberation of lipopolysaccharides (LPS) from bacterial cell. The present work is designed for fabrication of polycaprolactone (PCL) nanoparticles (NPs) for delivery of moxifloxacin (MOX) as antibiotic and rutin (RT) as adjuvant co-administered using PCL by nano-precipitation technique, followed by lyophilisation and In-vitro evaluation in J774 cell line. Preparation of polymeric NPs was by using certain modifications in nano-precipitation technique and certain process parameters were optimized. Stable NPs were then analysed for In-vitro cell line studies. Stable NPs had 173.63 nm ± 3.90 mean particle size, 0.107 ± 0.004 polydispersity, −22.63 ± 0.55 mV zeta potential, 7.49 ± 0.31% and 72.64 ± 1.06% drug loading and entrapment efficiency and sustained In-vitro release for 48 h. Antimicrobial activity of free MOX and PCL NPs of MOX against E. coli had correlation with In-vitro release studies. Cell viability studies on J774, THP1 and RAW 264.7 cell lines at various concentrations of PCL loaded NPs had more than 96.0% of cell viability. Cell uptake studies on J774 cell line confirmed phagocytosis mechanism of prepared PCL loaded nanoparticles. In-vitro cell line studies concluded that PCL loaded NPs of MOX and RT are safer for administration and In-vitro cellular uptake studies have provided a brief on potential of NPs for cellular uptake.