In this review we present an updated survey of the main synthesis methods of gold nanoparticles (AuNPs) in order to obtain various tailored nanosystems for biomedical imaging. The synthesis approach significantly impacts on the AuNPs properties such as surface chemistry, biocompatibility and cytotoxicity. In recent years, nanomedicine emphasized the development of functionalized AuNPs for biomedical imaging. AuNPs are a good option for used as delivery photosensitizer agents for PDT of cancer. For example, the complex formed from AuNPs functionalized with PEGylate porphyrins presents several advantages in the medical field such as a better use in photodynamic therapy because of high triplet states and singlet oxygen quantum yield efficiency of porphyrin molecules.