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PHYTOSOMES
M PHARM
Pharmaceutics
PESCP
Phytosome www.DuloMix.com 2
▪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 surrounded 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.
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▪Phytosomes are complex of natural active ingredients
and phospholipids which increase absorption of herbal
extracts or isolated active ingredients when applied
topically or orally.
▪ In general, they are considered as natural digestive aid
and carriers for both polar and non-polar active
substances.
▪ Most of phospholipids possess nutritional properties,
like phosphatidylserine which acts as a brain cell
nutrient, phosphatidylcholine which is important in liver
cell regeneration.
Difference between Liposome
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and phytosome
Phytosome Liposome
In phytosome, the phosphatidyl-choline A liposome is formed by mixing a water
and the plant components actually form soluble substance with
a 1:1 or a 2:1 molecular complex phosphatidylcholine in definite ratio
depending on the substance(s) under specific conditions.
complexes.
Phytosome involves chemical bonds. Here, no chemical bond is formed; the
phosphatidylcholine molecules
surround the water soluble substance
Phytosome are much better absorbed Bioavailability of liposomes is less than
showing better bioavailability. phytosomes.
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Advantages of phytosome
▪Phytosomes show better stability as chemical bond is
formed between phospholipid molecule and
phytoconstituents.
▪Dose of phytoconstituents is reduced due to more
bioavailability of the phytoconstituents in the complex
form.
▪Duration of action is increased.
▪Phytoconstituents complex with phospholipids are
more stable in gastric sections and resist the action of
gut bacteria.
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▪Enhanced permeability of phytoconstituents across the
biological membranes.
▪Absorption of lipid insoluble polar phytoconstituents
through different routes shows better absorption, hence
shows significantly higher therapeutic effects.
▪Phosphatidylcholine used in the formation of
phytosomes, besides acting as a carrier also possess
several therapeutic properties, hence gives the
synergistic effect when particular substance is given.
▪Drug entrapment is not a problem with phytosome as
the complex is biodegradable.
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▪ Phosphatidylcholine (or phosphatidylserine) is a
bifunctional compound. The phosphatidyl moiety is
lipophilic and the choline (serine) moiety is hydrophilic in
nature. This dual solubility of the phospholipid makes it
an effective emulsifier.
▪ The choline head of the phosphatidylcholine molecule
binds to these compounds while the lipid soluble
phosphatidyl portion comprising the body and tail which
then surrounds the choline bound material.
▪Hence, the phytoconstituents produce a lipid compatible
molecular complex with phospholipids.
Preparation of Phytosome
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Phytosomes are prepared by
reacting 3-2 moles or
preferably 1 mole of
phosphatidylcholine with 1
mole of active
phytoconstituents(flavonoids
and the terpenoids) in an
aprotic solvent such as
dioxane/ acetone from which
complex can be isolated by
precipitation with non solvent
as aliphatic hydrocarbons or
by lyophilization or by spray
drying.
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Antisolvent precipitation technique
• Drug + soya lecithin
• Reflux with 20ml dichloromethane at 60℃ for 2 hours
• Concentrate mixture to 5-10 ml.
• Add hexane 20ml.
• Filter the ppt, dry, crush and pass through #100 seive.
Rotary evaporation technwwiwq.DulouMix.ceom 10
• Drug+ soya lecithin
• Dissolve in 30ml of tetrahydrofuran
• Stirring for 3hrs at temp not exceeding 40℃
• Thin film is formed
• Add n-hexane with stirring
• Ppt obtained
• Dry and pass through mesh.
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• Drug and soya lecithin
• Reflux with 20ml of acetone at a temperature 50-60℃ for 2hrs.
• Concentrate the mixture to 5-10ml
• Formation of thin film and drying
• Hydration and formation of ppt
• Filter and collect formed Phytosomes.
Application of Phytosomes
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➢Silymarin Phytosome:
▪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.
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➢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.
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➢Phytosome of green tea:
▪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.
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➢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
▪ phytosome).png
▪ phytosome.png
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References
▪Saraf S. Applications of novel drug delivery system
for herbal formulations. Fitoterapia. 2010 Oct
1;81(7):680-9.
▪Singh, A., Saharan, V., Singh, M., Bhandari, A.
Phytosome: Drug Delivery System for Polyphenolic
Phytoconstituents. Iranian Journal of Pharmaceutical
Sciences, 2011; 7(4): 209-219.
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