Photodynamic therapy (PDT) is a low-invasive method for cancer treatment or other skin diseases. Important advantages of PDT over other therapies include the ability to deliver a precisely targeted treatment through selective illumination, the potential for repeated application at the same site if needed. However, the biodistribution of photosensitizers is unfavorable and phototoxicity to the skin, mainly caused by an agent’ hydrophobicity and non-selectivity, is a considerable limitation of their use. In this article, the potential of photosensitizer-loaded nanocarrier, including the enhancement of PDT efficacy and the reduction of the side effects of PDT, was discussed.