Cell‐specific drug delivery remains a major unmet challenge for cancer nanomedicines. Here, light‐triggered, cell‐specific delivery of liposome‐encapsulated doxorubicin to xenograft human cancer cells in live zebrafish embryos is demonstrated. This method relies on light‐triggered dePEGylation of liposome surfaces to reveal underlying targeting functionality. To demonstrate general applicability of this method, light‐triggered, MDA‐MB‐231 breast cancer cell specific targeting in vivo (embryonic zebrafish) is shown using both clinically relevant, folate‐liposomes, as well as an experimental liposome‐cell fusion system. In the case of liposome‐cell fusion, the delivery of liposomal doxorubicin direct to the cytosol of target cancer cells results in enhanced cytotoxicity, compared to doxorubicin delivery via either folate‐liposomes or free doxorubicin, as well as a significant reduction in xenograft cancer cell burden within the embryonic fish.