Phytosomes are one of the novel drug delivery system containing hydrophilic bioactive phyto-constituents of herbs surrounded and bounded by phospolipids.

1. Phytosomes
Under guidence of
Dr. Beny Baby
Associate professor
Dept. of Pharmaceutics
Karnataka College of Pharmacy
Presented by
Sujit Shrestha
M. Pharm (II semester)
Pharmaceutics

2. Content
• Introduction
• Definition
• Structure
• Advantages
• Properties
• Method of preparation
• Characterization
• Evaluation
• Application

3. Introduction
• The word phytosomes is derived from term “phyto”
which means plant while “some” means cell like.
• Phytosome is a patented technology developed by a
leading manufacturer of drugs and neutraceuticals, to
incorporate standardized plant extracts or water
soluble phyto-constituents into phospholipids to
produce lipid compatible molecular complexes, called
as phytosomes and this vastly improve their
absorption and bioavailability.

4. Definition
• Phytosomes are one of the novel drug delivery system
containing hydrophilic bioactive phyto-constituents
of herbs surrounded and bounded by phospolipids.
• The phytosome technology produces a little
microsphere or little cell, which protects the plant
extract or its active constituent from destruction by
gastric secretion and gut bacteria due to the gastro-
protective property of Phosphatidylcholine.

5. • The phytosome process has also been applied to
many popular herbal extracts including Ginkgo
biloba, grape seed, hawthorn, milk thistle, green tea,
and ginseng.

6. Structure
• Phytosome structure contain the active ingredients of the
herb surrounded by the phospolipids.
• The presence of the surfactant i.e the phospolipid in the
molecule which are shielded from water triggered
degradation while at the same time, allows obtaining a
higher adhesion of the product itself to the surface it
comes into contact with and a better interaction of various
molecules with cell structure.
• The size of phytosomes varies from 50 nm to a few
hundred µm.

8. S.No Features Phytosome Liposome
1 Arrangement of
molecules
In Phytosomes, phospolipid and an
individual phyto constituent are present in
1:1 or 1:2 ratio depending on the
substance.
Hundreds or perhaps thousands of
phospolipids molecules surround the
water soluble molecule.
2 Layer of
membrane
It is an integral part of the membrane being
the molecule anchored through chemical
bond to the polar head of the phospolipids.
The active principle is dissolved witin
medium contained within the cavity or
within the layers of the membrane
3 Content of
phospolipids
Less Higher Much Higher
4 Absorbance
profile
Better absorbed Good Absorbed
5 Bonding It is a unit of few molecules bonded
together.
It is an aggregrate of many phsopolipid
molecule that encloses other phyto
active molecules without specifically
bonding to them.

9. Advantages
• Marked enhancement of bioavailability
• Valuable components of the herbal extract are protected from
destruction by digestive secretions and gut bacteria.
• Assured delivery to the tissues.
• Dose requirement is reduced due to the absorption of chief
constituent.
• Phytosomes shows better stability profile because chemical bonds
are formed between phospolipid molecule and phytoconstituent.
• Phospolipid used in the phytosome process beside acting as a
carrier also nourishes the skin because it is essential part of the
cell membrane.

10. • Phospatidylcholine used in the preparation of phytosomes,
beside acting as a carrier also act as a hepatoprotective, hence
giving the synergistic effect when hepatoprotective substance
are employed.
• Phytosomes are widely used in cosmetics due to there more
skin penetration and have lipid profile.
• By enhancing the solubility of the bile to herbal constituent,
phytosomes facilitates the liver targeting.
• Phytosomes are better able to transition from a hydrophilic
environment into the lipid friendly environment of the
enterocyte cell membrane and from there into the cell, and thus
can be used for systemic targeting.

11. Properties of Phytosomes
1. Chemical Properties
 Phytosomes is a complex between a natural product and
natural phospolipids.
 The phytosomes complex is obtained by reaction of suitable
amount of phospolipid and the substrate in an appropriate
solvent such as glycerol.
 The main phospolipid substrate interaction is due to the
formation of hydrogen bond between the polar head of
phospolipid and polar functionalities of the substrate.
 When treated with water, Phytosomes assumes a micellar
shape forming liposomal like structure.

12. 2. Biological properties
 Phytosomes are advances form of herbal products that are
better absorbed, utilized and as a result produce better then
conventional herbal extracts.
 Phytosomes are lipophilic substance with definite melting
point, freely soluble in non polar solvent, and moderately
soluble in fats.
 Phytosomes can accommodate the active principle that is
anchored to the polar bed of the phospolipids, which finally
becomes an integral part of the membrane.
 The increased bioavailability of the phytosome over the non
complexed botanical derivatives has been demonstrate by
pharmacokinetics studies or by pharmacodynamic test in
experimental animals and in human subjects.

13. Schematic represenatation of preparation of phytosome
complex isolated with addition of non solvent
drying
hydration
Active constituent of herbal
extract
Phospolipid
Mixed in aprotic solvent for
complex formulation with
constant stirring
Complex in dry form
Complex dissolves in
organic solvent
Thin film is formed
Phytosomes suspension

14. Different Additives used in formulation of
Phytosomes
 Phospolipids
Eg: Soya Phosphatidyl choline, Egg Phosphatidyl choline,
Dipalmityl Phosphatidyl choline, Distearyl Phosphatidyl choline.
 Aprotic Solvent
Eg: Dioxane, Acetone, Methylene Chloride
 Non Solvent
Eg: n-hexane and other aliphatic hydrocarbon
 Alcohal
Eg: Ethanol, Methanol

16. Method of Preparation
1. Solvent evaporation method
2. Rotary evaporation technique
3. Anti solvent precipitation technique

17. 1. Solvent Evaporation Method
• Particular quantity of drug polymer and phospolipid can
be taken into spherical bottom flask and reflux with
specific solvent at a temperature 50-60ºC for 2 hrs.
• The mixture may be concentrated to 5-10 ml to get the
precipitate whch can be filtered and collected.
• The dried precipitate phytosome loaded can be placed in
amber colored glass bottle and store at room temperature.

18. 2. Rotary Evaporation Technique
• The particular quantity of drug polymer and phospolipid can
be dissolved in specific solvent in a rotary spherical bottom
flask followed by stirring for 3 hours at temperature not
exceeding 40ºC.
• Thin film of the sample can be obtained to which n-hexane is
added continuously stirred using a magnetic stirrir,
• The precipitate phytosome loaded obtained can be placed in
amber colored glass bottle and stored at room temperature.

19. 3. Anti solvent Precipitation Technique
• The particular quantity of drug, phospolipid and polymer may
be taken into a spherical bottom flask and reflux with specific
solvent at a temperature not exceeding 60ºC tor 2 hours.
• The mixture can concentrated to 5-10ml.
• n-hexane can be added carefully with continuously stirring to
get the precipitate which has filtered and collected and stored
in vaccum desiccator overnight.
• The dried precipitate is crushed in mortar and sieve through
#100 meshes.
• The dried precipitate phytosome loaded can ne placed in
amber colored glass bottle and stored at room temperature.

20. Evaluation of phytosomes
Particle size
Entrapment Efficiency
FTIR Spectrographic Analysis
Differential Scanning Calorimetry (DSC)
Drug content
Scanning Electron Microscopy
Stability study

21. Particle Size
• The average diameter and zeta potential of the phytosome
loaded may be each measured employing a Zetasizer ZEN
3600 at a fixed scattering angle of 90º at 25ºC.

22. Entrapment Efficiency
• Phytosome loaded can be diluted 1 fold with 10ml of solvent
and so centrifuged 18,000 rpm for ½ hour at -4ºC using
cooling centrifuge machine.
• The supernatent was isolated and the quantity of free drug may
be determines by UV/Visual spectrometry.
• To determine the entire quantity of drug 0.1ml of the
phytosome loaded suspension can be diluted in fuel, adusting
the volume to 10ml.
• The entrapment efficiency may be calculated according to the
subsequent formula.
Entrapment efficiency(%) = (total amount of drug) – (amount
of free drug)×100/(total amout of drug)

23. FTIR Spectrographic Analysis
• FTIR spectral data can be taken to determine the
structure and chemical stability of phytosome loaded,
phospolipids, polymer and drug sample. Samples can
be crushed with KBr to get pellets at 600kg/cm2
pressure. Spectral scanning may be done in the range
between 4000-400cm-1.

24. Differential Scanning Calorimetry (DSC)
• The drug sample, phospholipids, polymer, physical
mixture and phytosome loaded can be placed within
the aluminium crimp cell and heated at 10ºC/min
from 0 to 400ºC in the nitrogen atmosphere.
• Peak transition onset temperatures may be recorded
by means of the instrument.

25. Drug Content
• Drug content of phytosome loaded can be determined
by dissolving accurately weighed 100mg of
phytosome loaded in 10ml solvent.
• After appropriate dilution absorbance may be
determined by UV spectrophotometer.
• The drug content can be calculated by the subsequent
formula:
Drug content(%) = (total amount of drug) – (amount
of free drug) ×100/(total amount of drug)

26. Scanning Electron Microscopy (SEM)
• Scanning electron microscopy can be used to confirm
particle size distribution and surface morphology of the
phytosome loaded.
• Dry samples may be placed on an electron microscope
brass stub and coated with gold in an ion sputtet.
• Digital pictures of phytosome loaded may be taken by
random scanning of the stub at 1000, 5000, 10000 and
30000X magnifications.

27. In Vitro and In vivo Entrapment
• In vitro and in vivo evaluation can be done according
to therapeutic activity measuerment parameters of the
biologically active phytoconstituents present in the
phytosome loaded with the help of suitable animal
models.

28. Stability Study
• stability study of optimized phytosomoal formulation was
performed to investigate the physical appearance and leak
out of the drug from phytosomes during storage.
• Optimised phytosomal formulation of drug extract was
sealed in glass vials and stored at refrigeration
temperature (2-8ºC) and room temperature for a period of
3 month.
• Sample from optimised phytosomal formulation were
withdrawn at definite time intervals and observed.

29. Phytosomes uses

30. Phytosomes and its uses
S.No Phytosome Product Phytoconstituent complex
with phosphatidylcholine
Dose Indications
1 Silybin Phytosome Silybin from Silybum
marianum
120mg Hepatoprotective, antioxidant for liver
and skin
2 Ginko Biloba Phytosome 24% Ginkoflavanglycosides
from Ginko biloba
120mg Protect brain and vascular lining; Anti
skin ageing (best for over the age of
50)
3 Green tea Phytosome Epigallocatachin from Thea
sinensis
50-100
mg
Nutraceutical, systemic antioxidnt.
Best for protection against cancer and
damage to cholesterol.
4 Centella Phytosome Terpenes - Used to treat vein and skin Disorders
5 Curcumin Phytosome Polyphenol form Curcuma
longa
200-
300mg
Cancer chemo preventive agent
6 Ginseng Phytosome Ginsenosides from Panax
ginseng
150mg Immunomodulator

31. Conclusion
• Phytosomes forms a bridge between the conventional delivery
system and novel delivery system.
• Phytosomes are advances form of herbal extract that are better
absorbed which results better than conventional herbal extract.
• Phytosomes have improved pharmacokinetic and
pharmacological parameter, which in result can
advantantageously be used in various diseases.
• The nutraceutical product based on phytosome technology
become present a the site of action of liver, kidney, brain, heart
at similar or less dose as compared to conventional plant
extract.

32. Reference
• Recent trend of phytosomes for delivering Herbal
Extract with Improved Bioavailability; volume 1
issue 4; 2012
• Review Article: Phytosome loaded Novel Herbal
Drug Delivery system 21/06/2016
• Novel Apporach for herbal drug delivery 2017
• Review article: Phytosomes is a novel drug delivery
system based herbal formulation 2/22/2018