Biologically active phytochemicals such as alkaloids, terpenes, polyphenols and saponins can be isolated from plants and formulated as drugs or used as crude materials for development of (semi)synthetic drugs. Generally, phytochemicals are complex organic molecules, characterized by a large molecular weight, chemical instability and low water solubility, causing poor absorption, low bioaivailability and therefore limited clinical use. Incorporation of phytochemicals into biodegradable and biocompatible nanosystems can improve their pharmacokinetic and pharmacodynamic properties and thus significantly enhance the therapeutic outcome. Among the numerous investigated nanocarriers, liposomes have been demonstrated to be particularly suitable due to the proven ability to: achieve accumulation of the phytochemicals in the diseased tissues or intracellularly, potentiate biological effects and bioaivailability, enhance stability of the incorporated plant material, promote safety profile of the formulation and decrease undesirable side effects or potential citotoxicity. This work presents an overview of the selected ex vivo, in vivo and clinical investigations, systematized according to the chemical features of the incorporated phytoconstituent.