When used at a high dose, many anticancer drugs produce undesirable side effects including hepatotoxicity. Transdermal delivery bypasses first-pass metabolism, allowing the use of a lower dose of drug while decreasing systemic toxicity. In this review, we summarize various advanced technologies for improving anticancer drug delivery via the skin. This technology is discussed in the context of three anticancer drugs, 5-fluorouracil (5-FU), methotrexate (MTX) and 5-aminolevulinic acid (5-ALA). The use of a erbium:YAG (Er:YAG) laser for transdermal delivery of anticancer drugs is specifically highlighted in this review.