Two types of sequential extraction process (SEP) for the recovery of bioactive components from Korean red ginseng were examined. As a SEP (normal SEP, nSEP), Korean red ginseng was sequentially treated using hot water and n-hexane for the successive extraction of water-soluble and lipid-soluble components. Also by changing the sequential order of solvents, an alternative SEP (reverse SEP, rSEP) in which n-hexane extraction was followed by hot water extraction, was proposed. Regardless of the sequential order of solvents, the recovery yield of acidic polysaccharide (AP) and crude saponin (CS) showed no significant change. On the other hand, in the rSEP, the lipid-soluble fraction was obtained from red ginseng with an enhanced recovery yield, four times higher than that in nSEP. Additionally, from dose-response assays to assess the effects of lipid-soluble components on the proliferation of human hepatoma (HepG2) and breast (MCF-7) cancer cell lines, it was found that hexane extract of red ginseng (HER) in rSEP has higher efficacy than the hexane extract of red ginseng marc (HERM) obtained in nSEP. This strongly suggested that rSEP would be a more attractive industrial process in terms of the efficacy of lipid-soluble extract as well as the recovery yield.