Formulation and Evaluation of Colon Targeted Ciprofloxacin Microspheres

Abstract

In the present study, Colon-targeted Ciprofloxacin hydrochloride microspheres were formulated and their in vitro properties were assessed to determine whether or not the antibiotic could be delivered to the colon. By utilizing span-80 as an emulsifying agent, ciprofloxacin hydrochloride microspheres for colon targeting were prepared using the emulsion-solvent evaporation method. According to the preliminary trial findings, the ratio of drug to polymer had an impact on the microspheres' properties. The Ciprofloxacin: Eudragit S-100+HPMC 6cps ratio of 1:1, 1:2, 1:3, 1:4, 1:5, and 1:6 were used to make the colon targeting microspheres, in which the ratio of Eudragit S-100 to HPMC was always 1:1. The combination of Eudragit S-100 and HPMC demonstrated increased release lag time and regulated release rate, which improved protection of the drug-containing core. For the majority of the formulations examined, zero-order release followed a time delay caused by the hydrogel's swelling/retarding behaviour before the medication started to come out of the microspheres. The colon-targeting microspheres were also tested for micrometrics, particle size and surface properties, percentage drug content, encapsulation effectiveness, and in vitro drug release study in the three different pH environments (0.1 N HCL, Phosphate buffer pH 6.8 and Phosphate buffer pH 7.4) for 12 hours. The kinetics of drug release in vitro and the drug release mechanism of the microspheres were further investigated. With a particle size of 58.9 m, an almost spherical shape, and free-flowing characteristics, the best formulation batch had the highest drug entrapment efficiency of 86.81%. It was followed by a zero-order rate release with a non-fiction-diffusion mechanism, which had an 82.77% drug release rate.