The mitochondria have long since been known to be of great importance to life. They have roles in heme biosynthesis, energy production, and initiation of apoptosis among many other things. Due to their complex role in everyday life, their dysfunction has been associated with a variety of different diseases such as cancer, diabetes, aging, obesity and several neurodegenerative diseases. Although leaps and bounds have been made towards therapy, many of the general public still lose the battle with these diseases every year. There are several drugs that currently act on restoring mitochondrial function. However, there still needs to be improvement in that many of the drugs cannot cross the complex structures of the mitochondria. Nanocarriers have recently become more popular for the delivery of therapeutics to specific cells. They have the ability to deliver high amounts of payloads with high effiency without altering the structure of the drug itself. Specific cellular targets, such as target organelles, have not been fully explored. This dissertation will focus on improving the ability for mitochondrial acting therapeutics to reach their desired location through the use of small molecule prodrugs and nano-carriers. In vitro and in vivo results will be shown for a variety of different diseases.