PREPARATION AND APPLICATIONS OF
PHYTOSOMES:-
ASSOCIATE PROFESSOR
DEPARTMENT OF PHARMACEUTICS
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PHYTOSOMES:-
•The term “phyto” means plant while “some” means cell like. The
phytosome process produces a little cell, whereby valuable
components of the herbal extract are protected from destruction
by digestive secretions and gut bacteria.
•The phytosome are newly introduced structures, which contain the
active ingredients of herb surrounded and bound by phospholipids.
The phospholipid molecular structure included a water-soluble heads
and two fat soluble tails, because of their dual solubility, phospholipid
acts as an effective emulsifier.
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liposomes phytosomes
Liposomes are used In the phytosome the
primarily to deliver water- phosphatidylcholine and
individual plant component
soluble substances. actually form a 1:1 or 2:1
Liposome is formed by complex depending on the
mixing a water-soluble substance. Thus in
substance with phytosome process the
phosphatidylcholine, no active constituent of herbal
chemical bond is formed, extract is an integral part
of the membrane, being
the phosphatidylcholine the molecules anchored
molecules collectively through chemical bonds to
surround the water the polar head of
soluble substance. phospholipid
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The difference between phytosome and liposome. The molecular
organization of phytosome (lower segment) and liposome (upper
segment)
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ADVANTAGES OF PHYTOSOMES:-
a. There is an impressive improvement of the bioavailability of herbal
essence because of their organization with phospholipid and
enhanced assimilation in the intestinal tract.
b. They allow the non-lipophilic herbal essence to permit better
absorption from the intestinal lumen.
c. The conceptualization of Phytosome is secure and the ingredients
have all been permitted for pharmaceutical and cosmetic use.
d. They have been utilized to convey liver protecting flavonoids, as they
are made of phytosomes which have high bioavailability. Apart from this,
Phosphatidylcholine is hepatoprotective in nature.
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e. This technology provides economical delivery of phytoconstituents
and they also provide synergistic advantages in protecting the skin
against exogenous or endogenous hazards in stressful environmental
conditions when used in cosmetic.
f. They can be also utilized to improve the diffusion of drug through
the skin in transdermal and dermal drug delivery.
g. These are employed for the delivery of huge and an assorted
group of drugs (peptides, protein).
DISADVANTAGES OF PHYTOSOME:-
Phytoconstituent is quickly eradicated from phytosome.
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PROPERTIES OF PHYTOSOMES:-
physicochemical properties:-
1. Phytosome is made by reaction of the stoichiometric quantity of
phospholipid with the standardized herb essence as substrate. The
spectroscopic information discloses that the phospholipid substrate
interplay is because of the generation of hydrogen bond in between
the polar head (i.e., phosphate and ammonium group) and the polar
functionalities of the substrate.
2. The magnitude of Phytosome changes from 50 nm to a few
hundred μm.
3. Phytosome, when reacted with water, gets converted into a micellar
shape resembling liposome and photon correlation spectroscopy
(PCS) disclose this liposomal organization acquired by phytosome
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4. The H1NMR and C13 NMR data concluded that the fatty chain
responsible for unchanged signals both in free phospholipid and in the
complex, which shows that long aliphatic chains are clothed around the
active principle generating lipophilic envelope.
5. The complexes are generally freely soluble in aprotic solvents,
moderately soluble in fats, insoluble in water and comparatively unstable
in alcohol. But the phytosomes of certain lipophilic phytoconstituents like
curcumin has proved maximum water solubility upon complexation with
phospholipid.
biological properties:-
Phytosome is innovative complexes which show improved absorption;
hence they reduce bioavailability problem and shows excellent
outcomes than traditional formulation, which has been proved by
pharmacokinetic studies or else by pharmacodynamic tests in
experimental animals in addition to human subjects.
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PREPARATION OF PHYTOSOMES:-
Step-1 • Phospholipid dissolve in organic solvent.
Step-2
• Solution of phospholipid in solution containing Organic solvent +
Herbal extract
Step-3 • Drying
Step-4
• Thin Film Formation
Step-5
• Hydration of thin film
Step-6
• Formation of phytosome complex (suspension)
Step-7
• Isolation by precipitation with non solvent (such as aliphatic
hydrocarbons)
Step-8 • Drying (By lyophilization or spray drying)
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CHARACTERIZATION OF PHYTOSOME:-
There are numerous issues, for instance, the physical size, membrane
permeability, percentage of entrapped solutes, chemical composition of
the preparing materials which perform a dynamic character in
influencing the performance of phytosomes in physical in addition to
biological systems.
The following are the characterization methods utilized for phytosomes
in characterizing the aforementioned physical attributes:-
transition temperature: The transition temperature of the vesicular
lipid system can be settled via differential scanning calorimetry.
entrapment efficiency: The entrapment efficiency of a phytosomal
preparation can be determined by exposing the preparation to
ultracentrifugation method.
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vesicle size and zeta potential: The particle size and zeta potential
of phytosomes can be confirmed by dynamic light scattering, which
usages a computerized examination system and photon correlation
spectroscopy.
surface tension activity measurement: The surface tension activity
of the drug in aqueous solution can be determined by the Du Nouy ring
tensiometer.
visualization: Visualization of phytosomes can be accomplished
using Scanning Electron Microscopy (SEM) and by Transmission
Electron Microscopy (TEM).
vesicle stability: The steadiness of vesicles can be measured by
calculating the size and structure of the vesicles over time. The mean
size is calculated by DLS and structural changes are monitored by TEM
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APPLICATIONS OF PHYTOSOMES:-
1. Enhancing Bioavailability:
Evodiamine, a quinoline alkaloid, (Evodia rutaecarpa) possess a
multitude of pharmacological activities, such as anti-tumor, anti-
inflammatory, anti-nociceptive, anti-obesity, and thermoregulatory
effects. Evodiamine has anti-tumor potential in a wide variety of tumor
cells by inhibiting proliferation, inducing apoptosis and reducing
invasion and metastasis. Phytosomes of Evodiamine proved to have
higher in vitro dissolution rate, better absorption, longer action time
and higher bioavailability.
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2. Antioxidant properties:-
A physically stable phytosomal formulation of Quercetin was prepared
with higher encapsulation efficiency and physical stability to improve its
efficacy in intestinal absorption and its preservation from oxidation in
foodstuffs.
3. Hepato-Protective:
The leaf extracts of Ginkgo biloba (Family: Ginkgoaceae) have been
found to possess cardioprotective, anti-asthmatic, anti-diabetic, anti-
oxidant, hepatoprotective and potent CNS activities. The study
demonstrated that phytosomes of G. biloba (200 mg/kg) significantly
alleviated isoproterenol-induced myocardial necrosis.
Histopathological examination of the myocardium further confirmed
the cardioprotective effects of phytosomes.
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4. Cancer treatment:
Research on methanolic extract of Terminalia arjuna bark and its
phytosome to investigate its antiproliferative activity on human breast
cancer cell line MCF-7 by MTT assay by comparing its activities with
Quercetin and its phytosomes. The phytosome exerted more
antiproliferative effect as compared to free drug.
5. Transdermal application
The phytosomal complex of saponins and plant extracts (Panax ginseng
M.) proved to be more active in vasal protection, capillary permeability,
protection against UV radiation.
6. Wound healing
The leaves of Wrightia arborea when taken its ethanolic extract and
formulated into phytosomes exhibited more penetration and enhanced
wound healing properties.
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REFERENCE:-
1. International Journal of Research in Pharmacy and Chemistry.
2. International Journal of Pharmaceutical Sciences and Drug
Research.
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QUESTIONS:-
• Explain briefly about phytosomes and its applications. 5M x 2
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