For a long time, platinum has been used in the design and manufacture of a range of medical implants and in clinically used platinum drugs with a central platinum(II) atom. After losing the respective leaving group and subsequent substitution with water, the positively charged molecules are nucleophilically targeted by the free electrons of the N7 atom of purines to form intrastrand and interstrand adducts. The established mechanisms of action of platinum drugs comprise platination of genomic and mitochondrial DNA. This leads to a hindrance of DNA-based functions (e.g., transcription, replication, etc.). Such cellular dysfunction eventually causes apoptosis, especially when DNA lesions cannot be repaired. Platinum-based anticancer drugs play a central role in cancer therapy. However, their applicability and efficacy are limited by drug resistance and adverse effects. Nanocarrier-based platinum drug delivery systems are promising alternatives to circumvent the disadvantages of bare platinum drugs.