Abstract

DEVELOPMENT AND EVALUATION OF FLOATING MICROSPHERES OF CEFIXIME FOR ORAL CONTROLLED RELEASE

K. M. Lokamatha Swamy* and Ameer Pasha

ABSTRACT

The current study was aimed to improve the oral bioavailability of cefixime, an orally active antibiotic used to manage various infections, by developing floating microspheres. Cefixime is known to have poor bioavailability due to its slow and incomplete absorption from the gastrointestinal tract (GIT). To address this issue, sodium alginate (SA) as a coating material and combined it with xanthan gum (XG) and guar gum (GG) were emplyoed to enhance gastric residence time. Initially, cefixime microspheres were prepared using SA alone as the coating material. Subsequently, floating microspheres were formulated with a coat comprising SA in combination with XG and GG. Developed floating microspheres were evaluated for percentage yield, drug content, microencapsulation efficiency, swelling index, particle size analysis, floating ability, and in vitro dissolution studies. Fourier-
transform infrared (FTIR) studies confirmed the absence of any drug-polymer interactions. Comparatively, SA:GG microspheres exhibited greater swelling compared to SA:XG microspheres. All batches of cefixime floating microspheres demonstrated excellent floating ability, with a range of 78% to 100% and a floating lag time of ≤ 4 minutes. In vitro drug release from the microspheres was slow and sustained over extended periods of 10 h. The order of drug release retardation among microspheres with different polymers was as follows: SA > SA:GG > SA:XG. The designed floating microspheres of cefixime combining excellent buoyant ability with a suitable drug release pattern proves beneficial for enhancing oral bioavailability. Thus, suitable for controlled release for oral administration and could be compressed into tablets or filled into hard gelatin capsules.

Keywords: Floating microspheres, cefixime, bioavailability, sodium alginate, xanthan gum, gaur gum.