Improving the therapeutic index of drugs is a major impetus for innovation in many therapeutic areas such as cancer, infective and inflammatory diseases. A number of macromolecular drug delivery systems are under investigation to circumvent the limitations in improving the potential of drugs with respect to penetration and targeting to the diseased tissue. In the present study, permeability of ceftriaxone sodium has been improved by preparing alginate beads using a blend of absorption enhancers. The extent of enhancement was found to be highly dependent on the absorption enhancer’s species used. The results of in-vitro pharmacokinetic studies show that the use of absorption enhancers to enhance bioavailability of ceftriaxone offers a viable method to deliver them by oral route. Several approaches have been made in recent years to overcome the problems associated with GI degradation of cephalosporins owing to which only parenteral formulation is available for the drug like ceftriaxone. The research work is an approach towards designing oral dosage form of ceftriaxone sodium by using absorption enhancers whose results are promising.