Properties and biomedical relevance of phytosome encapsulated polyphenolics

Abstract

Polyphenols are secondary metabolites of plants, containing in their structure the aromatic ring with one or more phenolic groups. Such molecules have great antioxidant potential. They can modulate the activity of many enzymes and cell receptors and generate specific biological effects. Several polyphenols are already in use as active ingredients of pharmaceuticals or different cosmetic products. The large size of these polycyclic molecules and poor solubility in aqueous and/or lipid media may limit development of stable formulations and their passive diffusion into and through the biological membranes. The current strategy for enhancement of solubility and permeability of biomedically relevant polyphenols is based on formation of specific complexes with phospholipids which self associate in aqueous media and form specific unilamellar vesicles often described as phytosomes or herbosomes. There is an increasing number of scientific publications in this field during the last decade and different polyphenolics (e.g., curcuminoids, silybin, silymarin, ginkgoflavonglucosides, ginkgolides, bilobalide, and dimeric flavonoids from Ginkgo biloba leaf, sericoside, polyphenols from Camellia sinensis leaf (epigallocatechin, catechin, epicatechin-3-Ogallate, epigallo catechin-3-O-gallate), Vitis Vinifera (resveratrol, quercitin, catechin, procyanidins, epicatechin), are marketed as phytosomes obtained by the patented technology Phytosome® (Indena, Italy). The chapter reviews the significance of encapsulation of poliphenolic active ingredients, properties of commercially available phytosomes (physicochemical characteristics, stability, loading capacity, solubility, dispersibility) and phytosome relevance for development of pharmaceutical preparations and personal care products. The potential for enhancement of biological effects (cardiovascular, antiinflammatory, hepatoprotective, anticancer, hypoglycemic, weight loss, antiaging), of the currently investigated phytosomes is reviewed comprehensively.