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Background: The primary objective of any pharmacotherapeutics approach entirely lies with the effectiveness of the rationally designed delivery system to effectually deliver the suitable drug at the appropriate concentration at the proper site. Phytosomes are most effective carrier for the possible enhancement of bioavailability, reduction in the clearance rate, providing higher dissolution, and amplification of solubility by several folds of various natural products. Methods: The present review article focuses exclusively on the recent global advancements in the emerging novel drug delivery field of phytosomes from the year 1996 to present. Results: The article comprehensively highlights the reported phospholipid complexes of the active phytoconstituents (18β-Glycyrrhetinic acid, Andrographolide, Baicalein, Baicalin, Berberine, Catechin, Celastrol, Curcumin, Epigallocatechin-3-O-gallate, Evodiamine, Gingerol, Gymnemic acid, Icaritin, Kaempferol, L-carnosine, Luteolin, Mitomycin-C, Piperine, Quercetin, Resveratrol, Rutin, Salicin, Silibinin or Silybin or Silymarin, Sinigrin, and Umbelliferone) and herbal extracts (Aegle marmelos, Allium cepa, Allium sativum, Bacopa monnieri, Boswellia serrata, Butea monosperma, Calendula officinalis, Centella asiatica, Citrullus colocynthis, Ginkgo biloba, Glycine max, Lawsonia inermis, Mentha pulegium, Momordica balsamina, Momordica dioica, Phyllanthus amarus, Phyllanthus emblica, Tecomella undulate, and Woodfordia fruticosa) in treatment of various ailments along with the possible enhancement of pharmacodynamics and pharmacokinetic attributes. The review also exhaustively focuses on the clinical trials of several vesicular products and patents information. Conclusion: This article will be vital for the researchers of numerous fields who are working towards the development of novel drug delivery system for translating better therapeutic effects of herbal based components.