Abstract
<p><strong>Objective: </strong>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<strong>.</strong></p><p><strong>Methods: </strong>The effects of ciprofloxacin-cholate complex and pegylated ciprofloxacin-cholate complex were evaluated<strong>. </strong>LD<sub>50</sub> 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.</p><p><strong>Results: </strong>The LD<sub>50</sub> 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.</p><p><strong>Conclusion: </strong>The biochemical, hematological and histology results showed complexation did not increase adverse effects of ciprofloxacin. The PEGYlated complex showed higher AUC and C<sub>max </sub>peak than the uncomplexed drug, hence more therapeutic benefits.</p>
Highlights
Ciprofloxacin is a broad-spectrum antibacterial second generational class of fluoroquinolones that is widely used in the treatment of serious infections in higher animals [1]
This study focuses on the formation of ciprofloxacin-cholate complex and modifying the ciprofloxacin complex by conjugate chemistry, binding inert molecules such as Polyethylene glycol (PEG) to ciprofloxacin cholate complex to a prolonged residence in the body and decreased degradation by metabolic enzymes
The result of the toxicity studies on the ciprofloxacin-cholate complex; effects of the ciprofloxacin-cholate complex on the packed cell volume; red blood cells count; haemoglobin count; white blood cells count; ALT level; AST level; alkaline phosphates (ALP) level; albumin level are presented in fig. 1 and tables 1 to 9 respectively
Summary
Ciprofloxacin is a broad-spectrum antibacterial second generational class of fluoroquinolones that is widely used in the treatment of serious infections in higher animals [1]. According to Santo and co-workers [2], the use of ciprofloxacin in the treatment of infections is associated with most common adverse effects that include gastrointestinal tract disturbance, central nervous system disorder and hematological system disorder. According to {3}, Ciprofloxacin in the treatment of infections is associated with the most common adverse effects which include the gastrointestinal tract, central nervous system, and hematological system effects. Experiment using animal models and clinical experience showed that Ciprofloxacin-induced cardiotoxicity marked by increase QT and QTC interval and prolonged action potential duration. This increases the risk of arrhythmia (tosarde de points).
Sign-in/Register to view highlights & summary Talk to us
Join us for a 30 min session where you can share your feedback and ask us any queries you have
Schedule a callMore From: International Journal of Pharmacy and Pharmaceutical Sciences
Disclaimer: All third-party content on this website/platform is and will remain the property of their respective owners and is provided on "as is" basis without any warranties, express or implied. Use of third-party content does not indicate any affiliation, sponsorship with or endorsement by them. Any references to third-party content is to identify the corresponding services and shall be considered fair use under The CopyrightLaw.
