A pro-drug is a dormant derivative of a parent molecule of pharmacological importance which necessitates immediate or enzymatic transformation within the body to release its active drug form. They are proved to be more beneficial due to their target selectivity and biological activity. Nowadays, drugs 5-7% of the drugs accepted worldwide and about one-third of drugs approved each year are pro-drugs. Pectin is an edible plant polysaccharide present in plants which was widely utilized for construction of specific drug delivery systems. The main problem faced in drug delivery absence of site specificity of drug release at specific time. Recently, enzymes were used to design sharp-witted drug delivery system that becomes as an emerging field due to its specific advantages which includes substrate specificity and maximum selectivity under minor conditions. Pectinases or pectinolytic enzymes are catalysts which breakdown pectin through hydrolysis or elimination reactions. A Pectinolytic enzyme helps in the controlled release of drug certain time period with site specificity. This review gives the overview on the action of pectinase on different pectin substrates and its combination with ions and other derivatives coating for controlled and specific colonic drug delivery system. © RJPT. All rights reserved.