Phytopharmaceuticals are the newly termed herbal medicine, which includes standardized extract, bioactive fraction, and phytoconstituent. They have been practiced to cure, treat, and mitigate diseases. Phytopharmaceuticals have many health benefits, but their therapeutic efficacy is limited due to poor absorption, low bioavailability, and early elimination profile. A novel phospholipid complex is a newly introduced patented technology developed to incorporate the standardized plant extracts/fractions or water-soluble phytoconstituents into phospholipids to produce lipid compatible molecular complex, called phytosome, which improves their absorption and bioavailability. In herbal formulations, phytosome is the most advanced dosage form that has an upgraded absorption rate and enhanced pharmacokinetics compared with conventional products. The phospholipid complex results from hydrogen bonding between phospholipids and phytoconstituents, offering the maximum incorporation of herbal active ingredients into the lipidic layer and core. The increased therapeutic efficacy is due to the formation of amphiphilic phospholipid-complex of herbal medicine. This review highlights the role of phospholipids on delivery of herbal bioactives and natural extracts with particular emphasis on phytosomes. Moreover, the status of bioavailabilities, commercial products, patents, and clinical trials of phytosomal systems of phytopharmaceuticals were addressed.