Preparation and ex vivo evaluation of Microspheres for treatment of Urinary tract infections

Abstract

http://dx.doi.org/10.21276/IJRDPL.22780238.2018.7(6).3164-3171 ABSTRACT: Urinary tract infections (UTI) are the most frequent bacterial infections affecting about 150 million people each year. The most common cause of infections is E. Coli. UTI’s are treated with short course antibiotics. Ofloxacin is a synthetic fluorinated carboxy quinolone that has a broad spectrum of activity against both gram positive & gram-negative bacteria. Multiple doses of ofloxacin are required to attain steady state concentration. The main objective of this study was to prepare and characterize ofloxacin microspheres to prolong the release rate so as to decrease the necessity of multiple dosing especially in patients with UTI. Nine formulations of ofloxacin microspheres were prepared using sodium alginate, sodium CMC and HPMC K 15M in various concentrations. Microspheres were prepared by ionic cross-linking method using calcium chloride as cross-linking agent. The prepared microspheres were evaluated for percentage yield, drug loading, entrapment efficiency, particle size analysis, swelling index, SEM studies, in-vitro dissolution, kinetics of drug release and ex-vivo studies. All the formulations exhibited satisfactory results in evaluations. DSC studies revealed no evidence of interaction between ofloxacin and polymers. Formulation F6 was selected as best formulation as it has good drug loading, percentage yield, entrapment efficiency and sustained the drug release for 8h. Results of ex-vivo studies indicate significant antimicrobial activity of microspheres. All the result demonstrated that ofloxacin microspheres can be effectively used in the treatment of urinary tract infections.