Design and development of cefdinir niosomes for oral delivery

Abstract

Objective: The aim of the present study was to develop nonionic surfactant based vesicles (niosomes) to improve poor and variable oral bioavailability of cefdinir. Materials and Methods: Cefdinir niosomes were formulated by sonication method using varying concentration of surfactant (span 60), with and without soya lecithin, but the cholesterol ratio was kept constant in all the formulations. The influence of formulation variables such as surfactant concentration, soya lecithin presence or absence were optimized for size and entrapment efficiency. Drug excipient interaction studies were performed using FTIR, indicating compatibility of excipients with drug. Results: The highest entrapment efficiency (74.56%) was observed when span 60, cefdinir, cholesterol and soya lecithin were used in the ratio of 5:1:1:1. The zeta sizer of the niosomal formulations showed the size range between 190 nm-1140 nm. The photomicrography showed round shape of vesicles and further nano size of niosomes was confirmed by scanning and transmission electron microscopy. The optimized niosomal formulations (F11 and F6) exhibited sustained in-vitro release of 94.91% and 94.07% respectively upto 12 h. The ex-vivo permeation studies of optimized formulation revealed that the niosomal dispersion improved cefdinir permeability across goat intestinal membrane as compared to plain drug solution and marketed suspension (Adcef®). Antimicrobial activity studies revealed that the niosomes potentiated bacteriostatic activity of cefdinir as compared to Adcef®. Conclusion: The niosomal formulation could be one of the promising delivery system for cefdinir with improved oral bioavailability and controlled drug release profile.

Keywords

• Cefdinir
• cephalosporin
• niosomes
• permeation
• stability
• vesicular drug delivery