PHARMACOKINETICS, HEMATOLOGICAL AND BIOCHEMICAL EFFECTS OF CIPROFLOXACIN HYDROCHLORIDE-SODIUM CHOLATE COMPLEX

Objective: Ciprofloxacin is a broad spectrum antibiotic widely used in the treatment of infections, but its toxicological effects remains a great challenge. This research emphasized on analyzing the effect of a hydrophobic ion pair complex, involving ciprofloxacin hydrochloride and sodium cholate and also pegylated ciprofloxacin hydrochloride-sodium cholate complex.Methods: The effects of ciprofloxacin-cholate complex and pegylated ciprofloxacin-cholate complex were evaluated. LD50 was determined. The test drugs were orally to twenty-four albino mice, in six groups of four mice, at different doses of 7.14 mg/kg, 14.2 mg/kg and 21.4 mg/kg; and PEG complex, 7.14 and 14.2 mg/kg. Each was administered twice daily for fourteen days. The animal blood samples were subjected to hematological, biochemical tests; and the liver organs were collected. Histopathological examination was carried out on the harvested organs. Pharmacokinetic parameters were determined using the non-compartmental method.Results: The LD50 of the complex was above 5000 mg/kg. The non-significant decrease in PCV and WBC showed the parent drug and its complex are neither anemia inducing nor immunosuppressing; the significant decrease in the average RBCs count in post–treatment of 21.47 mg/kg of the complex could be from physiological changes; the bio-liver makers showed hepatocellular damage. Photomicrograph of the liver sections of mice showed mild areas of hepatocyte degeneration and inflammatory cell infiltrates.Conclusion: The biochemical, hematological and histology results showed complexation did not increase adverse effects of ciprofloxacin. The PEGYlated complex showed higher AUC and Cmax peak than the uncomplexed drug, hence more therapeutic benefits