Phytosomes : Preparation and Application

1. Phytosomes : Preparation
& Application
Presented By: Hemant Saini
D50217008
M.Pharm. IInd Sem
PDM University

2. Contents
• Definition
• Method of Preparation
• Difference Between Liposome and Phytosome
• Advantages of Phytosomes
• Properties of Phytosomes
• Applications of Phytosomes

3. Phytosome
• The term “phyto” means plant while “some” means cell-like.
Phytosomes are little cell like structure. This is advanced forms
of herbal formulations which contains the bioactive
phytoconsituents of herb extract surrounds and bound by a
lipid. Most of the bioactive constituents of phytomedicines are
water-soluble compounds like flavonoids, glycosides.
• Because of water soluble herbal extract and lipophilic outer
layer phytosomes shows better absorption and as a result
produce better bioavailability and actions than the conventional
herbal extracts containing dosage form.

4. Preparation of Phytosome
• Phytosomes are prepared by reacting 3-2 moles or preferably 1 mole of
phosphatidylcholine with 1 mole of active phytoconstituents mostly
the flavonoids and the terpenoids in an aprotic solvent such as dioxane
or acetone from which complex can be isolated by precipitation with
non solvent such as aliphatic hydrocarbons or by lyophilization or by
spray drying. In the phyto-phospholipid complex formation the ratio
between these two components is in the range of 0.5-2 moles. The
most preferable ratio of phospholipid to phytoconstituents is 1:1.
• Spectroscopic techniques reveal’s that the molecules of the
phytoconstituents are bonded to phospholipid moiety by means of a
chemical bond.

5. Difference between Liposome and
phytosome
Phytosome
• In phytosome, the phosphatidyl-
choline and the plant components
actually form a 1:1 or a 2:1 molecular
complex depending on the
substance(s) complexes.
• Phytosome involves chemical bonds.
• Phytosome are much better absorbed
than liposomes showing better
bioavailability.
Liposome
• A liposome is formed by mixing
a water soluble substance with
phosphatidylcholine in definite
ratio under specific conditions.
• Here, no chemical bond is
formed; the phosphatidylcholine
molecules surround the water
soluble substance.
• Bioavailability of liposomes is
less than phytosomes.

6. Structure difference between Liposome and Phytosome

7. Advantages of Phytosomes
• It enhances the absorption of lipid insoluble polar phytoconstituents
through oral as well as topical route showing better bioavailability,
hence significantly greater therapeutic benefit.
• As the absorption of active constituent(s) is improved, its dose
requirement is also reduced.
• Phosphatidylcholine used in preparation of phytosomes, besides
acting as a carrier also acts as a hepatoprotective, hence giving the
synergistic effect when hepatoprotective substances are employed.
• Chemical bonds are formed between phosphatidylcholine molecule
and phytoconstituent, so the phytosomes show better stability profile.
• Added nutritional benefit of phospholipids.

8. Advantages of Phytosomes (contd.)
• It assures proper delivery of drug to the respective tissues.
• The nutrient safety of the herbal extracts need not be
compromised by conveying the herbal drug as means of
phytosomes.
• Entrapment efficiency is high and more over predetermined
because drug itself is in conjugation with lipids in forming vesicles.
• There is no problem in drug entrapment while formulating
phytosomes.
• Phytosomes are also superior to liposomes in skin care products.

9. Properties of Phytosomes
1. Chemical Properties
• Phytosomes is a complex between a natural product and natural
phospholipids.
• The phytosome complex is obtained by reaction of suitable amounts
of phospholipid and the substrate in an appropriate solvent such as
glycerol.
• The main phospholipid-substrate interaction is due to the formation
of hydrogen bonds between the polar head of phospholipids (i.e.
phosphate and ammonium groups) and the polar functionalities of
the substrate.
• When treated with water, phytosomes assumes a micellar shape
forming liposomial-like structures.

10. Biological Properties
• Phytosome are advanced forms of herbal products that are better
absorbed, utilized and as a result produce better results than
conventional herbal extracts.
• Phytosomes are lipophilic substances with definite melting point, freely
soluble in non-polar solvents, and moderately soluble in fats.
• Phytosomes can accommodate the active principle that is anchored to
the polar head of the phospholipids, which finally becomes an integral
part of the membrane.
• The increased bioavailability of the phytosome over the non
complexed botanical derivatives has been demonstrated by
pharmacokinetics studies or by pharmacodynamic tests in experimental
animals and in human subjects.

11. Application of Phytosomes
• Most of the phytosomes are focused to Silybum marianum which contains
premier liver-protectant flavonoids.
• The fruit of the milk thistle plant (S. marianum, Family Steraceae) contains
flavonoids known for hepato-protective effects.
• Silymarin has been shown to have positive effects in treating liver diseases of
various kinds, including hepatitis, cirrhosis, fatty infiltration of the liver
(chemical and alcohol induced fatty liver) and inflammation of the bile duct.
Silymarin Phytosome
Phytosomes of grape seed
• Grape seed phytosome is composed of oligomeric polyphenols of
varying molecular size complexed with phospholipids.
• The main properties of procyanidin flavonoids of grape seed are an increase
in total antioxidant capacity and stimulation of physiological defenses of
plasma.

12. Application of Phytosomes (contd.)
• Green tea leaves (Theasinensis) is characterized by presence of a polyphenolic
compound epigallocatechin 3-O-gallate as the key component.
• These compounds are potent modulators of several biochemical process
linked to the breakdown of homeostasis in major chronic-degenerative
diseases such as cancer and atherosclerosis.
• Green tea also furnishes us with a number of beneficial activities such as
antioxidant, anticarcinogenic, antimutagenic, hypocholesterolemic,
cardioprotective effects.
Phytosome of green tea
Phytosomes of curcumin
• Maiti et al. developed the phytosomes of curcumin (flavonoid from
turmeric, Curcuma longa linn) and naringenin (flavonoid from grape, Vitis
vinifera).
• Phytosome of naringenin produced better antioxidant activity than the free
compound with a prolonged duration of action

13. References
1. INTERNATIONAL JOURNAL OF RESEARCH IN
PHARMACY AND CHEMISTRY (www.ijrpc.com)
2. International Journal of Pharmaceutical Sciences and
Drug Research (www.ijpsdr.com)