Phytosome®s overview

For good bioavailability, natural products must have a good balance between hydrophilicity (for dissolving into the gastro-intestinal fluids) and lipophilicity (to cross lipidic biomembranes). Many phytoconstituents like polyphenolics have good water solubility, but are, nevertheless, poorly absorbed⁽¹⁾ because of their large size, incompatible with a process of passive diffusion and/or their poor miscibility with oils and other lipids.
As a result, the ability of flavonoids to cross the lipid-rich outer membrane of small intestine enterocytes is severely limited. Water-soluble phytoconstituents (mainly polyphenolics) can be converted into a lipid-compatible molecular complex known as Phytosome^®s. A Phytosome^® is generally more bioavailable than a simple herbal extract due to its enhanced capacity to cross the lipid-rich biomembranes and reach circulation^(2-5). Phospholipids are small lipid molecules where glycerol is bonded to two fatty acids, while the third hydroxyl, normally one of the two primary methylenes, bears a phosphate group bound to a biogenic amino or to an amino acid⁽⁶⁾thus making Phytosome^®s different from liposomes. Phospholipids from soy, mainly phosphatidylcholine, are lipophilic agents, and readily complex polyphenolics. In this context, phosphatidylcholine, the major molecular building block of cell membranes and a compound miscible in both water and in oil/lipid environments, is well absorbed orally, and has the potential to act as a chaperon for polyphenolics, shuttling them through biological membranes⁽⁷⁾.
Based on this technology, a line of products has been developed and commercialized by Indena (table 1).

Trade name	Phytochemical	Indication
18ß-glycyrrhetinic acid Phytosome^®	18ß-glycyrrhetinic acid from licorice rhizome	Soothing
Centella Phytosome^®	Triterpenes from Centella asiatica leaf	Cicatrizing, trophodermic
Crataegus Phytosome^®	Vitexin-2″-O-rhamnoside from Hawthorn flower	Antioxidant
Escin ß-sitosterol Phytosome^®	Escin ß-sitosterol from horse chestnut fruit	Anti-oedema
Ginkgoselect^® Phytosome^®	Ginkgoflavonglucosides, ginkgolides, bilobalide from Ginkgo biloba leaf	Vasokinetic
Ginselect^® Phytosome^®	Ginsenosides from Panax ginseng rhizome	Skin elasticity improver, adaptogenic
Ginkgo biloba Terpenes Phytosome^®	Ginkgolides and bilobalide from Ginkgo biloba leaf	Soothing
Ginkgo biloba Dimeric Flavonoids Phytosome^®	Dimeric flavonoids from Ginkgo biloba leaf	Lipolytic, vasokinetic
Greenselect^® Phytosome^®	Polyphenols from green tea leaf	Prevention of free radical-mediated tissue damages and weight management
Leucoselect^® Phytosome^®	Polyphenols from grape seed	Antioxidant, capillarotropic
Meriva^®	Curcuminoids from turmeric rhizome
PA₂ Phytosome^®	Proanthocyanidin A₂ from horse chestnut bark	Anti-wrinkles, UV protectant
Sericoside Phytosome^®	Sericoside from Terminalia sericea bark root	Anti-wrinkles
Siliphos^®	Silybin from milk thistle seed	Hepatocyte protection
Silymarin Phytosome^®	Silymarin from milk thistle seed	Antihepatotoxic
Virtiva^®	Ginkgoflavonglucosides, ginkgolides, bilobalide from Ginkgo biloba leaf	Vasokinetic
Visnadex^®	Visnadin from Amni visnaga umbel	Vasokinetic

Table 1. Commercially available Phytosome^®s and their trademarks

1. Manach C, Scalbert A, Morand C, Rémésy C, Jiménez L. Polyphenols: food sources and bioavailability. Am J Clin Nutr 2004;79:727–47.
2. Bombardelli E, Curri SB, Della Loggia R, Del Negro P, Tubaro A, Gariboldi P. Complex between phospholipids and vegetal derivatives of biological interest. Fitoterapia 1989;60:1–9 [Suppl. to issue N.1].
3. Mauri PL, Simonetti P, Gardana C, Minoggio M, Morazzoni P, Bombardelli E, et al. Liquid chromatography/atmospheric pressure chemical ionization mass spectrometry of terpene lactones in plasma of volunteers dosed with Ginkgo biloba L. extracts. Rapid CommunMass Spectrom 2001;15:929–34.
4. Kidd PM, Head K. A review of the bioavailability and clinical efficacy ofmilk thistle phytosome: a silybin–phosphatidylcholine complex (Siliphos^®). Altern Med Rev 2005;10:193–203.
5. Rossi R, Basilico F, Rossoni G, Riva A, Morazzoni P, Mauri PL. Liquid chromatography/atmospheric pressure chemical ionization ion trap mass spectrometry of bilobalide in plasma and brain of rats after oral administration of its phospholipidic complex. J Pharm Biomed Anal 2009;50:224–7.
6. Citernesi U, Sciacchitano M. Phospholipid/active ingredient complexes. Cosmet Toilet 1995;110:57–68.
7. Kidd PM. Phosphatidylcholine: a superior protectant against liver damage. Altern Med Rev 1996;1:258–74.


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