Mitochondria-specific nanocarriers for improving the proapoptotic activity of small molecules

The efficiency and efficacy of drug action depends largely on how well an unaided drug molecule is able to reach its intracellular target or even its target inside organelles such as mitochondria. Subsequently, the specific delivery of a drug to its site of action inside cells will dramatically improve its action. Mitochondria play a key role in apoptosis, and several clinically used, as well as experimental, drugs are known to trigger apoptosis by interacting directly with the target site at or inside mitochondria. During the past decade, a variety of mitochondria-specific pharmaceutical nanocarriers have been developed for the purpose of delivering therapeutic DNA or low-molecular weight compounds to mitochondria inside living mammalian cells. Here, the preparation of drug-containing, mitochondria-targeted nanocarriers is described and protocols for their in vitro and in vivo assessment are given.