The present investigation is carried out to evaluate the transport efficiency of KNPS and normal ketrolac drug in colon cancer cell line (Caco-2 cells). The transport efficiency was determined in the terms of time dependent and concentration dependent. The transport efficiency of the compounds was also tested in two different directions such as apical and basolateral direction in the presence of drug transporters. In according to our results obtained the present investigation, the intracellular concentration of the KNPS and normal ketrolac drug was increased after 7th hour of incubation time (101.885±0.1 nmol/L mg and 116.44±0.1 nmol/L mg) respectively comparing to the concentration recorded at 30 min (29.11±0.1 nmol/L mg). On the other hand, the concentration of the KNPS and normal ketrolac drug was immensely increased at 250 μg/mL is (188.43±0.5 nmol/L mg) and (93.1±0.02 nmol/L mg) respectively. The transport efficiency of the drug in the presence of MK-571 resulted significant intracellular concentration of KNPS and normal ketrolac drug. Comparing to apical direction of drugs inoculation the basal direction inoculation was found significant in the increase in the concentration of KNPS and normal ketrolac drug.