This document discusses phytosomes, a novel drug delivery system for herbal extracts. Phytosomes improve the bioavailability of plant extracts by combining phytoconstituents with phospholipids. This allows poorly soluble botanical extracts to be better absorbed in the intestinal tract and cross membranes. The document describes the preparation, characterization, formulation and commercial uses of phytosomes. Some benefits are improved stability and absorption compared to simple herbal extracts. Commonly used phospholipids are phosphatidylcholine, phosphatidylethanolamine and phosphatidylserine.

1. SHIV KUMAR
M.PHARM(2ND
SEM)
DEPARTMENT OF PHARMACEUTICAL
SCIENCES AND TECHNOLOGY
MRSPTU,BHATINDA

2. 1. INTRODUCTION
2. WHAT IS PHYTOSOMES?
3. MERITS OF PHYTOSOMES COMPLEX USES
4. DIFFERENCE BETWEEN PHYTOSOMES AND LIPOSOMES
5. METHOD OF PREPARATION
6. CHARACTERIZATION OF PHYTOSOMES
7. FORMULATION OF PHYTOSOMES
8. COMMERCIALLY AVAILABLE PHYTOSOMES
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3.  Polyphenolics and terpenes are ubiquitous in plants, but their poor
solubility in water and organic solvents make the bioavailability of several
botanical extracts erratic and poor.
 The limited solubility , both in water and in lipophilic phases, as well as
hydrolytical instability at physiological pH values make several botanical
extracts containing polyphenolics and terpenes very poorly absorbed both
orally and topically.
 Bioavailability can be improved by using new delivery systems which can
enhance the rate and the extent of solubilization into aqueous intestinal fluids
and the capacity to cross biomembranes.
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4.  Polyphenolics exhibit a marked affinity for phospholipids via hydrogen
bondings and dipolar interactions with the charged phosphates groups of
phospholipids.
 By complexing the polyphenolic phytoconstituents in a definite ratio with
phosphatidylcholine,
 Indena has developed a delivery system named “Phytosome®”.
 First phytosomal preparation-Flavonognan Silybin(silymarin)obtained from
Milk thistle fruit having properties of antioxidant,liver detoxification,anti-
inflamatory.
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5.  Phytosomes are novel drug delivery system containing hydrophilic
bioactive phytoconstituents of herbs surround and bound by
phospholipids.
 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.
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6.  Phospholipid:
a) Phosphotidylcholine
b) Phosphotidylethanolamine
c) Phosphotidylserine
 Phospholipid : drug(2:1 or 1:1)
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7.  There is a dramatic enhancement of the bioavailability of botanical extract
due to their complexation with phospholipid and improved absorption in
the intestinal tract.
 They permit the non-lipophilic botanical extract to allow better absorption
from the intestinal lumen, which is otherwise not possible.
 Phytosome process produces a little cell whereby the valuable component of
the herbal extracts are protected from destruction by digestive secretions
and gut bacteria.
 The formulation of phytosomes is safe and the components have all been
approved for pharmaceuticals and cosmetic use.
 Phytosomes shows better stability profile because chemical bond are
formed between phosphotidylcholine molecules and phytoconstituents.
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8.  They have been used to deliver liver protecting flavonoids because
they can be made easily bioavailable by phytosomes.
 Entrapment efficiency is high and more over predetermined because
drug itself in conjugation with lipids is forming vesicles.
 Phosphotidylcholine used in the phytosomes process besides acting as a
carrier also nourishes the skin because it is a essential part of cell
membrane.
 They can be also used for enhanced permeation of drug through skin
for transdermal and dermal delivery.
 Their low solubility in the aqueous media allows the formation of
stable emulsions or creams.
 Phytosomes are also superior to liposomes in the skin care products.
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9. PHYTOSOMES LIPOSOMES
Active chemical
constituents(phytoconstituents)
are anchored through
chemical bonds to the polar
head of the phospholipids.
Active chemical constituents is
dissolved in the medium of the
cavity or in the layer of the
membrane.
No chemical bonds are
formed.
Ratio of phosphatidylcholine
to phytoconstituents is 1:1
or 2:1 , depending on the
phytoconstituents.
Thousand of
phosphatidylcholine
molecules surrounds the water
soluble molecules.
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10.  The most significant dietary source of the essential nutrient choline, is an
orthomolecule ubiquitous in known life form.
 Besides being an important emulsifier in the lungs,gastrointestinal tract,bile.
 PC is the principal molecular building block for circulating lipoproteins and
for cell membrane. They are making up the matrix into which fit a large
variety of proteins that are enzymes, transport proteins, receptors and
other biological energy converters.
 Manage the vast majority of life processes.
 As a carrier for both fat-miscible and water-miscible nutrient.
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11.  Phytosomes are prepared by reacting natural or synthetic phospholipids with active
components like bioflavonoid, flavolignan and polyphenolic constituents.
 Solvent Evaporation method is the most common technique used for the
preparation of phytosomes.(Refluxed at 50-60C for 2hr). Phytosomes of
ginsenoside, puerarin and kushenin are prepared in this manner.
 Mechanical Dispersion method is used for the preparation of marsupsin-
phospholipid complexes.
 Phospholipids is dissolved in a suitable solvent and active ingredient is added drop
by drop while sonicating the solution .Phospholipid complex is sometimes prepared
under reflux and stirring conditions to effect complete interaction.
 Prepared complex called phytosome can be isolated by precipitation with
nonsolvent,lyophilization,spray drying or vacuum drying.
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12.  Visualization of particle size
 Transmission electron microscopy(TEM)
 Scanning electron microscopy(SEM)
 Spectroscopic evaluation
 1
H-NMR
 13
C-NMR
 FTIR(Chemical stability)
 Entrapment efficiency(Ultracentifugation)
 Spreadibility
 Percentage yield
 DSC
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13.  Can be formulated :
(a)Orally
(b)Topically
 The formulation tips here shown is indicated by the Indena for
(a) Soft gelatin capsules
(b) Hard gelatin capsules
(c) Tablets
(d) Topical dosage form
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14. Ingredients Quantity
Ginkgoselect ®
Phytosome®
180 mg
Soy bean oil 250 mg
Soy lecithin q.S
Glycerylmonostearate q.S
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15. Ingredients Quantity
Ginkgoselect ®
Phytosome®
180 mg
Dicalcium phosphate dihydrate 196 mg
Silicified microcrystalline cellulose 47 mg
Croscarmellose sodium 23 mg
Talc 2 mg
Magnesium stearate 2 mg
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16. Ingredients Quantity
Leucoselect ®
Phytosome®
100 mg
Soy polysaccharides 138 mg
Corn starch 100 mg
Silicon dioxide 6 mg
Talc 3 mg
Magnesium stearate 3 mg
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17. Phytosome Herbal drug Indication
Ginkgoselect ®
ginkgobiloba Improve memory,
Brain function,
Anti inflammatory agent
Silybin®
Silybum marianum Anti oxidant,
Anti aging,
Hepatoprotective
Hawthore®
Crataegus oxyacantha Help to strengthen heart
and cardiovascular
system
Ginselect®
Panax ginseng Promote adaptogenic
functions and resistance
to stress
Curcumin Curcuma longa Chemoprotective agent
Grapseed Grapseed Natural antioxidant
protectantDepartment of pharmacognosy/LMCP/Mrugesh
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18. Phytosome Herbal drug Indication
Greenselect®
Camellia sinensis Antioxidant,
Cardioprotective,
Food product
Mirtoselect®
Vaccinium myrtillus Antioxidant
Leucoselect®
Vitis vinifera Cardiovascular protectant,
Anti-inflammatory,
Antioxidant
Sabalselect®
Serenoa repens Non-cancerous prostate
enlargement
Lymphaselect®
Melilotus officinalis Effective in hemorrhoids,
thrombophlebitis, post-
surgical edema formation,
lymphedema
OleaselectTM
Olea europaea Antioxidant, inhibit harmful
oxidation of LDL
PolinaceaTM
Echinacea angostifolia Enhance immune function
in response to toxic
challenge
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19. 1. Shalini Sharma,"Phytosomes : AN EMERGING TECHNOLOGY”,
JPRD/2010/PUB/ARTI/VOV-2/ISSUE-5/JULY/2014,ISSN 0974 – 9446.
2. Sanjat Saha,Phytomes:a brief overview,2013:2(1):12-20.
3. Asit R Sahu, Formulation and Evaluation of Phytosome Drug Delivery
System of Boswellia Serrata Extract, Int J Res Med. 2015; 4(2);94-99.
4. Sushila Rathee, Optimization and development of Antidiabetic phytosomes
by box-benhken design, ISSN: 0898-2104 (Print) 1532-2394.
5. http://ijpsr.com/bft-article/phytosomes-a-novel-drug-delivery-for-herbal-
extracts/?view=fulltext
6. https://www.pharmatutor.org/articles/phytosomes-is-a-novel-drug-delivery-
system-based-herbal-formulation-an-review
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