Application of Quality by Design Approach in Development of Cefixime Trihydrate Loaded Gastro-retent

Abstract

Cefixime is an antibiotic that belongs to the 3rd generation cephalosporin antibacterial and acts by interrupting the cell wall synthesis of bacteria. It is a weakly acidic drug primarily absorbed through the stomach and upper intestine as a unionized drug. The drug is incompletely absorbed from GIT, leading to poor bioavailability. The current research focuses on developing gastro-retentive mucoadhesive microspheres loaded with cefixime trihydrate. The drug remains in the unionized form in acidic pH, showing enhanced absorption through the stomach. Mucoadhesive microspheres of cefixime trihydrate were prepared using HPMC K15M and Carbopol 971P as carrier polymer and mucoadhesive polymer, respectively. The formulation was prepared by using the spray drying technique. Further, the in-vitro evaluation of the mucoadhesive property of cefixime microspheres was done on the goat stomach mucosa. The study showed a strong mucoadhesion of 82% for an extended period of gastroprotection up to 6 hours. The in-vitro drug release study of microspheres was performed using 0.1 N HCl. The prepared formulation exhibited extended release for up to 8 hours. It is concluded from the above studies that the current formulation has been elicited prolonged gastric residence time as well as extended-release and provided an opportunity for better and enhanced absorption of the drug. Thus, the formulation may be projected for better therapeutic value, probably by improving the bioavailability of the experimental drugs.