Photodynamic Therapy: Targeting Cancer Biomarkers for the Treatment of Cancers

SIMPLE SUMMARY: Photodynamic therapy (PDT) is a minimally invasive treatment option that can kill cancerous cells by subjecting them to light irradiation at a specific wavelength. The main problem related to most photosensitizers is the lack of tumor selectivity, which leads to undesired uptake in normal tissues resulting in side effects. Passive targeting and active targeting are the two strategies to improve uptake in tumor tissues. This review focused on active targeting and summarizes recent active targeting approaches in which highly potent photosensitizers are rendered tumor-specific by means of an appended targeting moiety that interacts with a protein unique to, or at least significantly more abundant on, tumor cell surfaces compared to normal cells. ABSTRACT: Photodynamic therapy (PDT) is a well-documented therapy that has emerged as an effective treatment modality of cancers. PDT utilizes harmless light to activate non- or minimally toxic photosensitizers to generate cytotoxic species for malignant cell eradication. Compared with conventional chemotherapy and radiotherapy, PDT is appealing by virtue of the minimal invasiveness, its safety, as well as its selectivity, and the fact that it can induce an immune response. Although local illumination of the cancer lesions renders intrinsic selectivity of PDT, most photosensitizers used in PDT do not display significant tumor tissue selectivity. There is a need for targeted delivery of photosensitizers. The molecular identification of cancer antigens has opened new possibilities for the development of effective targeted therapy for cancer patients. This review provides a brief overview of recent achievements of targeted delivery of photosensitizers to cancer cells by targeting well-established cancer biomarkers. Overall, targeted PDT offers enhanced intracellular accumulation of the photosensitizer, leading to improved PDT efficacy and reduced toxicity to normal tissues.