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Herbal medicine and phytochemicals have always been great therapeutic options to treat various diseases due to their compatibility, safety, easy production, low cost and side effects. However, low absorption rate ,and poor bioavailability are notable challenges that have limited the use of most phytoconstituents. To address these challenges, different drug delivery methods have been proposed for generating operative carrier systems for phytochemicals. Among them, transdermal drug delivery (TDD) using nanophytosome has been introduced as a promising candidate for the delivery of insoluble phytoconstituents. Phytosomes can overcome skin barriers, and are therefore effective carriers for herbal medicines. They are generally produced by combining phytoconstituent agents in medicinal plant extracts with phospholipid molecules. They have improved the clinical applications of phytoconstituents such as polyphenols by enhancing their bioavailability and uptake. In this review, main benefits of transdermal delivery systems, advantages of nanophytosome over other lipid nanoparticles in TDD of phytochemicals, and methods of phytosome preparation and characterization are briefly reviewed.