Essentials oils from citrus have anti-inflammatory and antioxidant activity. Furthermore, terpenes are their main phytochemicals, namely limonene is the most important one. As terpenes are permeation promoters, they have been used to improve transdermal delivery of drugs. In addition, a proper oil source is a key factor to obtain desired phytochemicals. Recently, polymeric nanoparticles, solid lipid nanoparticles, nanostructured lipid carriers, nanoemulsions, liposomes and elastic liposomes as carriers of citrus essential oils or citrus terpenes have been developed to achieve more effective formulations. In this chapter, the most recent publications on nanocarriers containing citrus oils or citrus terpenes were addressed. In that regard, citrus oil or terpenes loaded in nanotechnological systems improve drugs skin permeation. Besides, terpenes loaded in nanoparticles also increase transdermal delivery of drugs. As essential oils and their respective terpenes are volatile compound and prone to oxidation, its encapsulations reduce oxidation and volatility. Hence, an improved antioxidant activity can be obtained. Therefore, nanoformulations of citrus oils or citrus terpenes are potential approaches to skin topical and transdermal delivery.