Phytosomes
Neha Chopra
ITM University, Gwalior
[email protected]
Abstract
The term “Phyto” means plant and “some” means cell It is also mentioned as herbosomes this is a
new patented technology, where standardized plant extracts or water soluble phytoconstituents are
complexed with phospholipids to produce lipid compatible molecular complexes, there by greatly
increasing absorption and bioavailability. The recent development and conducted works of various
researchers have been studied thoroughly to establish the transdermal route as a potential way to
deliver phytoconstituents. Plant derived products or plant extracts are increasingly receiving attention
as dietary supplements for the homeostatic management of inflammation, toxicities, cancers, weight
loss and other chronic or acute degenerative disorders. But these products frequently face stability
and bioavailability problems. Plant products after their isolation become prone to instability and are
potentially unfit to cross the bio membrane as such. The phytosome technique reduces these tasks to
reasonable extents. The phytosome or Herbosome technique increases the hydrophilicity of highly
lipophilic drug there by making it suitable for drug delivery and increases the lipophilicity of
hydrophilic phytoconstituents adequately to cross biological membrane. The topical application of
phytosomes for cosmetic purpose has already been proven. This review also contains a comparative
account of liposomes and phytosomes along with recent advancements in the field of phytosome
technology with a special concern to transdermal drug delivery. The poor oral bioavailability of
polyphenolic compound can be enhanced through the incorporation of them into phospholipid based
self-assembled delivery system, i.e. popularly known as phytosome. There are number of products
available in the market that contains phytosomal drug delivery system such as Ginkgo biloba,
Silybum marianum, and Camellia sinensis.
Keywords- Phytosome; Plant; Phospholipid; Herbosomes; Bioavability; Product; technology etc.
Introduction
Most of the biologically active constituents of plants are polar or water soluble but due to the problem
in absorption, restricts the utilization of these type of compounds which ultimately decreases the
bioavailability. For improvement of bioavailability, herbal products must have proper homeostasis
between hydrophilic (for absorption into gastrointestinal tract fluid) and lipophilic (to cross lipid bio
membrane balance) [1]. Plant preparations are widely used in traditional as well as modern medicine
system. During the traditional time, various pharmacological studies have been carried out with many
plants extracts and their constituents to check their therapeutic application. Over the past year, great
advancement has been made for the development of novel drug delivery system (NDDS) for various
plant extracts and their active constituents. Novel drug delivery such as targeted drug delivery which
directly channels the active entity on the site of action and such delivery system could offer targeted
and sustained release of drug so that pharmacological effect could be achieved at lower dose. The
development in the area of herbal medicine started earlier to cure human diseases with lesser side
effects [2].
A number of chief constituents of herbal medicine are easily soluble in water (glycoside, flavonoid);
however, these constituents are bounded in their potency because they may be partially soluble or
hydrophobic in nature, so when applied topically shows less therapeutic efficacy . Numerous efforts
have been put forward to enhance the bioavailability of such drug by formulating them to target drug
delivery system such as phytosomes and liposomes are good options. The use of these techniques in
formulation development process may lead to good bioavailability of herbal drugs as compare to
conventional herbal extracts [3]. Phytosomes means herbal drug loaded in vesicles, which is available
in the Nano form. The phytosome provide an envelope,like coating around the active constituent of
drug and due to this the chief constituent of herbalextract remains safe from degradation by digestive
secretion and bacteria. Phytosome is effectively able to absorb from a water loving environment into
lipid loving environment of the cell membrane and finally reaching to blood circulation. The current
reviewhighlights the future scope and emerging technologies in the field ofNDDS for the benefit of
herbal and traditional medicines prepared from plant origins [4]. The term “Phyto” means plant and
“some” means cell like. It is also mentioned as herbosomes. This is a new patented technology, where
standardized plant extracts or water soluble phytoconstituents are complexed with phospholipids to
produce lipid compatible molecular complexes, there by greatly increasing absorption and
bioavailability. Phosphatidylcholine, phosphatidylserine, phosphatidylethanolamine,
phosphatidylinositol are the phospholipids used, but phosphatidylcholine are widely used because of
their certain therapeutic value in case of liver diseases, alcoholic steatosis, drug induced liver damage
and hepatitis. Phospholipids are also employed as natural digestive aids and as carriers for both fat
miscible and water miscible nutrients.
Fig.1. Structure of Phyotosome
Properties of phytosomes -
1. Physico-chemical properties
Phytosomes are prepared by reaction of stoichiometric amount of phospholipid with the
standardized plant extract as substrate. The spectroscopic data reveals that the phospholipid-
substrate interaction is due to the formation of hydrogen bond between the polar head (i.e.,
phosphate and ammonium group) and the polar functionalities of the substrate. The size of
phytosome varies from 50 nm to a few 100 µm. Phytosomes when treated with water, they
assume a micellar shape resembling liposome and Photon Correlation Spectroscopy (PCS)
reveals these liposomal structures acquired by Phytosomes. From the 1HNMR and 13CNMR
data, it can be deduced that the fatty chain gives unchanged signals both in free phospholipid and
in the complex, which indicates that long aliphatic chains are wrapped around the active
principle, producing lipophilic envelope. Regarding the solubility of phytosomes, the complexes
are often freely soluble in aprotic solvents, moderately soluble in fats, insoluble in water and
relatively unstable in alcohol. But the phytosomes of certain lipophilic phytoconstituents like
curcumin has shown increased water solubility upon complexation with phospholipids which has
been discussed later in this paper [7] [8].
2. Biological properties - Phytosomes are novel complexes which are better absorbed and
utilized, hence they produce more bioavailability and better result than the conventional herbal
extract or non-complexed extracts, which has been demonstrated by pharmacokinetic studies or
by pharmacodynamic tests in experimental animals and in human subjects. Phytosomes express
their behavior in physical or biological system because of their physical size, membrane
permeability, percentage entrapment, chemical composition, quantity and purity of the materials
used
Sr. Trade name Chief constituents Source Dose Use
No.
1 Centella Triterpine Centella asiatica - Cicatrizing, trophodermic
phytosomes
2 Ginselect Ginsenosides Gingko biloba 120 mg Adaptogenic
phytosomes
3 Greenselect Polyphenols Camellia sinensis - Free radical scavenging
phytosomes activity
4 Leucoselect Polyphenols Vitis vinifera 300 mg Antioxidant
5 Meriva Curcuminoids Curcuma longa 200-300 Anti-inflammatory
mg
6 Silymarin Silymarin Silybum marianum - Antihepatotoxic
7 Oleaselect Polyphenols of olive Olea europaea - Anti-inflammatory,
oil antioxidant
TM phytosome
8 Crataegus Vitexin-2’-O- Crataegus - Antioxidant
phytosomes rhamonoside Mexicana
9 Visnadine Visnadine Ammi visnaga - Circulation improver
10 Bilberry Triterpine Vaccinium - Potent antioxidant
myritillus
11 Ruscogenin Steroid saponin Ruscus aculeatus - Anti-inflammatory
phytosomes
12 PA2 phytosomes Proanthocynidin Horse chestnut bark - Antiwrinkles,
UV protectant
13 Zanthalene Zanthalene Zanthoxylum - Soothing, anti-itching
phytosomes bungeanum
14 Lymphaselect Triterpenes Melilotus officinalis - Indicated in insomnia
phytosomes
15 Sabalselect Fatty acid, sterols Serenoa repens - Beningn prostate
phytosome hyperplasia
16 Sericoside Sericosides Terminalia sericea - Skin improver
phytosome
17 Echinacea Echinacosides Echinacea - Immunomodulators,
phytosome angustifolia nutraceuticals
18 Rexatrol Resveratrol Polygonum - Antioxidant, antiaging
cuspidatum
Table 1. Commercially available Phytosomes
Conclusion
The phytotomies should not be confused with liposomes where hydrophilic drug molecules are entrapped within a
cavity or spaces between the membranes. The liposomes may involve several hundred phospholipid molecules for
this entrapment and are usually now being used for cosmetic purposes. Instead, the phytosomes involves interaction
of 1- 4 phospholipid molecules with the phytoconstituents which are chemically anchored to each other. Several
researches have shown the phytosomes to be a better alternative for liposomes in terms of membrane permeability
and stability. Phytosomes are a class of lipid based vesicular carriers, which can be used for encapsulation of plant
originated nutraceuticals such as polyphenols. Flavonoids are one of the main types of polyphenols and phyto-active
compounds, which have several nutritional and therapeutic benefits.
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