Cell‐penetrating peptides (CPPs) are short peptides with significant potential in the field of drug delivery as they can enhance the cellular uptake of their attached cargo. Meanwhile, lipid nanoparticles (LNPs) are important nanocarriers for various drugs as they provide stability to drug molecules and their surface can be modified with different ligands for targeted delivery. Consequently, modification of different LNPs with CPPs is an important approach to improve intracellular drug delivery and targeting. In this chapter, we briefly introduce CPPs, their types, and the mechanisms of their uptake. We also introduce LNPs and discuss their applications in drug delivery. We then focus on the modification of different LNPs with CPPs and the potential applications of these promising nanocarriers in intracellular delivery as well as in tumor and liver targeting. We finally discuss some strategies …