Development of ciprofloxacin gel and antibacterial activity of ciprofloxacin on pseudomonas aeruginosa

Abstract

In this research, the topical gel of ciprofloxacin HCl- HP- ß-CD inclusion complex was prepared and evaluated for physical and chemical stabilities and antimicrobial activity. The observed AL type phase solubility diagram and the observed fluorescence enhancement of ciprofloxacin HCl in the presence of HP- ß-CD indicated that ciprofloxacin HCl- HP- ß-CD inclusion complex was formed. Ciprofloxacin HCl and ciprofloxacin lactate could form inclusion complex with HP- ß-CD at the same extent. Thus, ciprofloxacin HCl was chosen for complex formation in further studies due to its low cost. To prepared ciprofloxacin HCl gels, ciprofloxacin HCl inclusion complex was incorporated in gel bases making from 18% w/w Poloxamer 407 and 1% Carbopol ETD 2020. Poloxamer 407 gel containing 0.15 mg/g of ciprofloxacin HCl inclusion complex showed better physical and chemical stability than the product making from 1% Carbopol ETD 2020 after photo stress. In the dark at 40 ºC, gradually loss of ciprofloxacin HCl in Poloxamer 407 and Carbopol ETD 2020 gels were estimated to be 16 and 26 %, respectively, over 3 months. At ambient temperature in the dark, ciprofloxacin HCl inclusion complex in Poloxamer 407 preparation was more stable than ciprofloxacin HCl inclusion complex Carbopol ETD 2020 gels. The release studies through a membrane (Spectrapor® MWCO 1,000) showed that the complex solution and the ciprofloxacin-complex-Poloxamer 407 gel preparation could release free ciprofloxacin. It was found that ciprofloxacin HCl could be released from its complex and gel. The release profile was described by Higuchi model. The release rate constant from gel was found to be 2.82 mg cm-2 hr-½. The in vitro antimicrobial activity against 29 clinical isolates of Pseudomonas aeruginosa showed that inclusion complex ciprofloxacin HCl gel could inhibit all ciprofloxacin susceptible strains of P.aeruginosa.