The arginine-rich cationic Tat peptides have been reported to enhance the intracellular delivery of macromolecules, including DNA, RNA, and proteins. In this work an arginine cationic peptide derived from the HIV-1 Tat protein was conjugated with noncovalent bonds to sulfonated aluminum phthalocyanine (AlPcS, a photosensitizer for the light-activated photodynamic cancer therapy), doxorubicin (DOX, a chemotherapeutic agent), or quantum dots (QDs, often used as carriers for the delivery of anticancer drugs). The fluorescence of intracellular conjugates of AlPcS-Tat, DOX-Tat, and QDs-Tat was studied by means of confocal laser scanning microscopy in the human nasopharyngeal carcinoma KB cells and cervical carcinoma Hela cells in vitro. The Tat peptide with noncovalent links can enhance at least a twofold of intracellular delivery of AlPcS, DOX, and QDs via an endocytotic pathway in the two tumor cell lines. This finding may suggest that the Tat peptide-mediated intracellular delivery of anticancer drugs may have the potential for improving efficacy of cancer therapy.