First report on guar gum-MSN (GG-MSN) based colon targeted delivery for possible oral application. Anticancer drug (5FU) was loaded inside MSN through capping by natural carbohydrate guar gum. Biodegradation of GG caps by colon specific enzymes from colonic microflora induced 5FU release. ∼50% release in colonic condition in 4 h; near perfect ‘zero release’ in other GI conditions. In-vitro analysis on colon carcinoma cells in colonic environment showed antiproliferative activity.