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1. Introduction

1.1 General

With an advent of evolution, man is dependent on plants for a variety of his needs,

namely sources of food materials, fuel, building materials, fibers, bulk chemicals,

cosmetics and also as medicines.

The medicinal plants play key role in the maintenance of world health as these are

commonly available in abundant. These plants offer mankind immediate access to safe

and effective products for use in treatment of various diseases. Medicinal plants are

valuable to modern medicine in four basic ways1.

They are used as sources of direct therapeutic agents.

They serve as raw base for elaboration of more complex semisynthetic

compounds.

The chemical structures derived from the plant sources can be used as model for

new semi-synthetic compounds.

The plants can be used as taxonomical markers for discovery of new compounds.

1.2 Herbal dosage form

Herbs have been used in a wide variety of dosage forms, since they were first discovered

to have medicinal qualities. These include the fresh or dried herb plant parts, including

the leaves, stems, roots, flower, seeds or fruits. Many herbalists promote use of the fresh

plant materials.

Herbal medicine suppliers offer plant part to be produced in form of several types of

dosage form:

Herbal products can be given as pastes obtained from mashed herbs.

Can be given as juices squeezed from herbs.

Infusion or teas, where the herb is steeped into hot water.

Decoction or extracts of herbs made by boiling the herb in water to form a

concentrate.

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Cold teas can be made where the herb is simply steeped in cold water.

Herbs pulverized into a powder and used as such or compressed into a tablet or

filled into capsules.

Herbal wines produced by fermenting the herbs with water and sugar.

Various tinctures made by extracting the herb with alcohol, glycerin or vinegar.

Liniments made with alcohol and vegetable oils used externally.

Herbal ointment (salves) made with the herb, mixed and dissolved in wax,

petroleum jelly.

Various syrups made with the herb or extract mixed into sugar, honey or glycerin

vehicles.

Poultices where the herb is moistened (cold or hot) and applied directly to a bruise

or wound and held in place with gauze.

Herbal oils usually formulated with a base oil (e.g. olive oil, sesame oil, almond

oil), the herb is placed in any of these oils allowed to stand for several days,

strained and bottled.

Several polyherbal formulations, can be obtained, which containing powder or

extracts of more than one plant drug in combination to provide a multi component

system.

Although a large number of such formulations, containing the plants with known and

proven medicinal activity, in different dosage forms are available for different

disorders. With the advances of pharmaceutical technology, more convenient dosage

forms have evolved.

At present, herbal dosage forms can be classified into two categories. The first

category contains traditional dosage forms like pills, powder, semi fluid extracts,

pellets, gelatin, tinctures, syrups, lozenges, medicated teas, wines and solutions. The

second category consists of new dosage forms developed from modern technological

processes and TCM and western medicine principles. These forms include tablets,

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capsules, soluble granules, suppositories and intravenous and intra muscular

injections.

Modern herbal dosage forms offer small dosage size, and relatively good absorption

in the human body. The modern forms are more user friendly, because they are not

cumbersome to carry and can be worked into a busy schedule. Modern herbal dosage

forms have played a tremendous role in clinical treatment and have resolved problems

such as the inconvenience of preparation and administration of decoctions.

Swallowing capsule or tablets is often easier for people who cannot drink large

volumes of liquid or who do not like the bitter taste of decoctions2.

Modern herbal forms are still showing certain limitations, so the scientific and

systemic investigations are required to authenticate the medicinal value of herbal

drug.

So a scientific research plan is necessary for the improvement in the performance of

the modern herbal dosage forms, which is known to be caused due to the following

restrictions:

Poor bioavailability of herbal extracts.

Large doses of herbal extract.

Degradation of herbal extract in G.I.T.

Lack of uniformity in herbal dosage form.

Absence of localized delivery to target organ of such herbal medication.

These restrictions can be overcome by approaches to improve the therapeutic

performance of the established herbal drugs by formulating them as new drug delivery

system rather than going for cumbersome and costly research for a new entity3.

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1.3 Novel drug delivery systems

The success of Novel Drug delivery Systems (NDDS) for a number of agents has

provided unprecedented impetus for this dosage form. The traditional prosthetic role of

polymeric materials in medicinal devices is being supplemented by novel applications in

the pharmacological and pharmaceutical areas. With ever improving techniques and

methodologies and increasing pressure to find new and clinically viable dosage forms for

new and old drugs. NDDS are being developed rapidly so as to overcome the limitations

of conventional drug delivery4. Conventional drug delivery involves the formulation of

the drug into a suitable form, such as compressed tablet for oral administration or a

solution for intravenous administration. These dosage forms have been found to have

serious limitations in terms of higher doses required lower effectiveness, toxicity and

adverse effects. NDDS offer added value with a number of therapeutic benefits over

conventional dosage forms5.

Therapeutic benefits of novel drug delivery systems6

Increased efficacy of the drug.

Site specific delivery.

Decreased toxicity/side effects.

Increased convenience.

Shorter hospitalization.

Viable treatments for previously incurable diseases.

Potential for prophylactic applications.

Lower health care costs both short and long term.

Better patient compliance

Translation of the advances of various scientific disciplines in to clinical therapy will

occur only if parallel progress is made in devising new concepts to achieve delivery of

drug to the desired site of action. Fortunately, this priority has been recognized and

research on NDDS is now a major focus of attention in both academic and industrial

research laboratories. Many NDDS have been successfully developed and

commercialized and have often demonstrated better acceptance by the health system and

higher market share than the conventional delivery systems. A few NDDS available in

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the global market are; Transdermal patches, Implants, Nasal systems, Microcapsules,

Osmotic systems, Ion exchange resin systems, Pellets in capsules7.

Table 1: Novel Drug Delivery Systems8, 9, 10

System Basic Concept

Transdermal Partial rate control via polymer membrane (matrix type,

reservoir type)

Ionotophoric system External control and pulsative delivery. (Anodic and

Cathodic)

Vesicles Targeting and slow release of lipophilic and hydrophilic

drugs (liposomes and nanoparticles)

Antibody drug

conjugates

Homing potential to antigen sites (monoclonal antibody)

Osmotic pump Zero order release determined by drug/salt/osmotic agent

(for oral and rectal delivery)

Complex emulsion Slow release potential.

Implants Release over days and year possible

Responsive feedback

system

Biological control over days and year possible.

Microsphere Targeting and slow release

Phytosome Targeting and faster absorption

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1.3.1 The interest

There are number of reasons for intense interest in NDDS:

The recognition of the possibility of repatenting successful drugs by applying

concepts and techniques of controlled release drug delivery systems, coupled with

the increasing expense in bringing new drug entities to market has encouraged the

development of NDDS11

.

NDDS are needed to deliver the novel, genetically engineered pharmaceuticals

i.e. peptides and proteins to their sites of action without incurring significant

immunogenicity or biological inactivation12

.

Treating enzyme deficient diseases and cancer therapies can be improved by

better drug targeting13

.

Therapeutics and safety of drug administered by conventional route can be

improved by more precise spatial and temporal placement within the body14

.

1.3.2 The technology

Ideally the delivery system should provide therapeutics in response to physiological

requirements. It should have the capacity to sense changes and alter the drug release

process recordingly. An analytically prepared release profile is essential. Such responsive

controlled drug delivery systems, although still in its early stages, focus on two

fundamental approaches:

Externally regulated systems utilizing triggers such as magnetism, ultrasound,

temperature and electricity15

.

Self regulated systems (utilizing pH sensitive polymers, enzyme substrate

reactions). These systems release the drug to its site of action in the body in

response to patient’s therapeutic needs, rather than merely releasing quantities of

the drug at desired rates. For example, artificial pancreas system is used for

automatic administration of insulin16

.

Based on the science and technology of drug delivery, these technical

advancements can be categorized as follows:

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I. Controlled drug delivery diffusion process17

A. Polymer membrane permeation controlled:

(Drug reservoir in a rate controlling polymer matrix) 18- 20

Table 2: Marketed brands of polymer membrane permeation controlled dosage

form

NDDS Drug Therapeutic uses

Progestasert(I.U.D.) Progesterone To achieve contraception (one

year)

Occusert Pilocarpine For management of glaucoma

(One week)

Transderm Nitro Nitroglycerin For treatment of anginal attacks

(One day)

Estraderm Estradiol For treatment of post menopausal

(Three to four days)

Transderm-scop Scopolamine For prevention of motion sickness

(72 hrs.)

Catapress TTS Clonidine For treatment of hypertension (One

Week)

B. Polymer matrix diffusion controlled21, 22

Table 3: Marketed brands of Polymer matrix diffusion controlled dosage

form

NDDS Drug Therapeutic uses

Frandol tape Isosorbide dinitrate For treatment of anginal attacks

(One day)

Nitro-Dur Nitroglycerin For treatment of anginal attacks

(One day)

Compudose

Implant

Estradiol For treatment of post menopausal

syndrome. (One year)

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C. Micro reservoir dissolution controlled system20, 22

Table 4: Marketed brands of Micro reservoir dissolution controlled dosage

form

NDDS Drug Therapeutic uses

Syncro-Mate-

C-Implant

Norgestomet For control and synchronization of

estrus cycle livestock. (20 days)

Nitro-Disc Nitroglycerine For treatment of angina attacks.

(One day)

II. Controlled drug delivery by modulation process

A. Osmotically modulated

Table 5: Marketed brands of Osmotically modulated dosage form23, 24

NDDS Drug Therapeutic uses

Alzet osmotic

pump

Insulin For management of diabetes

(Several months)

Acutrim tablet Phenyl propanolamine Appetite suppression.(One

day)

Indomethacin

tablet

Indomethacin For treatment of pain

B. Hydro dynamically modulated:

Imbibation and swelling of the annular openings and thus release through the

opening e.g. for continuous delivery of insulin in treatment of diabetes25

.

C. Vapour pressure modulated:

Vapour pressure blows drug out e.g. for constant infusion of heparin in

anticoagulation treatment, for administration of insulin in antidiabetic medication,

for administration of morphine for treatment of pain in cancer26

.

D. Mechanically modulated:

Externally controlled mechanically operated systems like metered dose nebulizer

for intranasal administration of buserelin (LHRH) and insulin27

.

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E. Magnetically modulated:

Electromagnetic triggering for delivery of bovine serum albumin at controlled

rate28

.

F. Ultrasonically modulated:

Ultrasonic waves energize the drug release29

.

G. pH modulated:

pH dependent release mechanism for controlled oral aspirin30

.

H. Ion Modulated (Pennkinetic system):

Ion exchange resin and drug complex for sustained release of drugs orally31

.

I. Iontophoresis:

Drugs involved are electrochemically gradient e.g. Phoresor32

.

J. Swelling modulated:

Release is controlled by hydration induced swelling of polymeric matrix33

.

Table 6: Marketed brands of swelling modulated dosage form

NDDS Drug Therapeutic uses

Syncro-Mate-B

implants

Norgestomet For control and synchronization of

esters cycle livestock.

(Sixteen days)

Val release

tablets

Diazepam For management of anxiety and

insomnia.

K. Hydrolysis modulated:

For parenteral controlled release of naltrexone in treatment of narcotic addicts for

about three months. Drug is incorporated with biodegradable or bioerodable

polymers.34

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L. Enzymatically modulated:

Enzymatic hydrolysis of biopolymers by a specific enzyme in the target tissue.

Albumin microspheres for the controlled release of 5-fluorouracil with the aid of

protease activator in cancer treatment35

.

1.4 Carrier based delivery system

The use of carriers to target drugs to various organs is based on the fact that the

properties of the carrier determine the destination and fate of the drug entrapped in the

carrier provided that the drug leaches from the system at a suitable controlled rate.

1.4.1 Liposomes

These are artificial microscopic bilayer vesicles made of phospholipids, enclosed in

aqueous compartment. Drugs incorporated in liposomes can be delivered to the desired

site in desired concentrations without being toxic. Disease categories for liposomal drug

delivery are disease related to immune system, cancer chemotherapy, arthritis,

haemophilia, diabetes and infectious diseases. Several products undergoing clinical trials

are Doxorubicin amphotericin-B, gentamycin, vaccine for AIDS, Vincristine, and etc36.

1.4.2 Monoclonal antibodies

These are artificially produced proteins, which exhibit specificity for one single antigen.

The major application for which monoclonal antibodies are being studied for therapeutic

use is in cancer37

.

1.4.3 Nanoparticles

These are colloidal particulate systems in the sub-micron size range acting as carrier for

drug molecules. Medical applications using nanoparticles are in the treatment of

infections of reticulo-endothelial system, enzyme replacement therapy in the liver,

treatment of cancer etc38

.

1.4.4 Microspheres

These are small solid particulate carriers containing dispersed drug particles either in

solution or crystalline form. Microspheres are used as carriers for drugs and other

therapeutic agents. Some drugs under investigation for microsphere system are

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mitomycin, 5-fluorouracil, progestrone, adriamycin, cisplatin, etc. Novel development is

magnetic microspheres, which have great potential in the localized tumor treatment39

.

1.4.5 Phytosome

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. An emulsifier is a material that can combine

two liquids that normally will not mix well together. By combining the emulsifying

action of the phospholipid, with the standardized botanical extracts, the phytosome

provides dramatically enhanced bioavailability and deliver faster and improved

absorption in the intestinal tract and, because not all botanical properties are as

bioavailable as others, joining them to phospholipids produces an effective medium for

increased absorption of the active constituents of herb40

.

The flavonoids and terpenoids component of these herbal extracts lend themselves

quite well for the direct binding to phosphatidylcholine. Specially, the choline head of the

phosphatidylcholine molecules binds to these compounds, while the fat soluble

phosphatidyl portion comprising the body and tail, then enveloped the choline bound

materials. Thus, as a result a little microspheres, or cell or vesicles is produced. The term

"phyto" means plant while "some" means cell like. The phytosome process produced a

little cell, whereby valuable components of the herbal extract are protected from

destruction by digestive secretions and gut bacteria40

.

Thus the phytosome is another breakthrough technology for the development in

herbal technology. The phytosome process intensifies herbal compounds by improving

absorption, increasing bioavailability and enhancing delivery to the tissue. Some herbal

compounds are not very bioavailable, however binding them to phosphatidylcholine

produces a highly bioavailable form of the herbal compound. Several studies have shown

that the body uses phytosome molecules more effectively that non phytosome molecules.

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1.4.5.1 How does "Phytosome" differ from a "Liposome"

Liposomes are used primarily to deliver water-soluble substances.

Liposome is formed by mixing a water-soluble substance with phosphatidylcholine, no

chemical bond is formed, the phosphatidylcholine molecules collectively surround the

water soluble substance. In contrast, with the phytosome process, the phosphatidylcholine

and individual plant component actually form a 1:1 or 2:1 complex depending on the

substance. Thus in phytosome process the active constituent of herbal extract is an

integral part of the membrane, being the molecules anchored through chemical bonds to

the polar head of phospholipid. The main difference between liposome and phytosome

are shown in fig. no 1.

Fig. 1: Main difference between liposome and Phytosome40

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1.4.5.2 Advantages of phytosome

Phytosomes offer several advantages which are as follows:

Phytosome is much better absorbed than liposome because drug is in complex form

with lipid.

Entrapment efficiency is high and more ever predetermined because drug itself in

conjugation with lipid is forming vesicle.

Unlike liposome, there is no need of following the tedious, time consuming step for

removing the free, untrapped drug from the formulation.

Leakage of drug during storage does not occur in phytosome, because drug is bonded

with lipid, however loss may occur due to some chemical degradation i.e. hydrolysis.

No problem of drug incorporation.

The entrapment efficiency of drug molecule in liposome depends upon encaptured

volume and drug bilayer interaction; however it is irrelevant in phytosome.

The lipid composition in liposome decides its membrane fluidity, which in turn

influences the rate of drug release and physical stability of the system. However in

phytosome membrane fluidity depends upon the phase transition temperature of the

drug-lipid complex, but it does not affect release rate since the drug is bound. The

drug is released from phytosome by hydrolysis (including enzymatic).

The physiochemical stability of phytosome depends upon the physicochemical

properties of drug-lipid complex.

In phytosome, phospholipid transfer/exchange is reduced and solubilization by HDL

(high density lipid) is low.

Due to amphiphilic behavior, phytosome system allows, after medication, a multiple

transfer through lipophillic membrane system or tissue, through cellular walls,

piggyback endocytosis and exocytosis.

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Following absorption, their degradation velocity into active drug molecules depends

to a great extent on the size and functional groups of drug molecule, the chain length

of the lipids and the spacer. These can be varied relatively precisely for optimized in

vivo pharmacokinetics.

1.4.5.3 Method of preparation of phytosome

According to the invention, the novel complexes are prepared by reacting

equimole of natural or synthetic phospholipid, which can be phosphatidylcholine,

phosphatidylethanolamine or phosphatidylserine, with an equimole of active constituent

of herbal extract, in aprotic organic solvents such as dioxane or acetone, from which the

complex can be isolated by precipitation with non solvents such as aliphatic hydrocarbon

or by lyophilization or by freeze drying. The complex obtained after precipitation are

dried under vacuum and dissolved in organic solvent i.e. chloroform etc. and then

introduced into 250 ml round bottom flask with round glass neck. The flask is attached to

rotatory evaporator and rotated at 60 rpm. The organic solvent is evaporated under

reduced pressure, when the organic solvent is completely evaporated, the casted film is

dispersed in aqueous medium, i.e. phosphate buffer saline solution. Upon hydration the

lipid swells and peeled off from the wall of the round bottom flask and vesiculate

forming vesicles41

.

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Fig. 2: Preparation of Phytosomes

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Fig. 3: Schematic Representation of Preparation of Phytosome

Active constituent

of herbal extract Phospholipid

Mixed in aprotic solvent for complex

formation with constant stirring

Complex in dry form

Complex dissolves in

organic solvent

Thin film is formed

Phytosome Suspension

Complex is isolated with

addition of nonsolvent

Drying

Hydration

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Table 7: Different Additives Employed in Formulation of Phytosomes41-47

Class Example Uses Reference

Phospholipid

Soya phosphatidyl choline

Egg phosphatidyl choline

Dipalmityl phosphatidyl

choline

Distearyl phosphatidyl

choline

Vesicles forming

component

Fuzzati et al.

Maffei et al.

Aprotic

solvent

dioxane, acetone,

methylene chloride

As a solvent Gabetta et al

Non solvent n-hexane and non solvent

i.e. aliphatic hydrocarbon

Complex

precipitating

solvent

Gabetta et al.

Alcohol

Ethanol

Methanol

As a solvent Morazzoni et al.

El-Maghraby et al.

Vanden Berge et al.

Dye

Rhodamine-123

Rhodamine-DHPE

Fluorescein-DHPE

Nile-Red

6 Carboxy fluorescence

For CSLM study Fuzzati et al.

Maffei et al.

Conti et al

Buffering

agent

Saline phosphate buffer

(pH 6.5)

7 % v/v Ethanol

Tris buffer ((pH 6.5)

As a hydrating

medium

Fuzzati et al

Conti et al.

El-Maghraby et al

Vanden Berge et al.

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Table 8: Methods for the Characterization of Phytosomes48-51

Parameter Method References

Vesicle shape

(morphology)

Transmission electron microscopy Sutarjadi et al.

Entrapment efficiency Mini column centrifugation

method

Unger

Vedavathy

Vesicle size and size

distribution

Dynamic light scattering method El-Maghraby et al.

Skin permeation

potential

Confocal laser scanning

microscopy

Fluorescence microscopy

Transmission electron microscopy

Thin layer chromatography

Simonetti et al.

Vanden Berge et al.

Surface charge and

charge density

Zeta meter Foster

Turbidity Nephlometer Sutarjadi et al.

Simonetti et al.

In vitro drug release

study

Side by side diffusion cell with

artificial or biological membrane,

Dialysis bag diffusion

Vanden Berge et al.

Gabetta et al.

Effect on the skin

structure

Histological studies

Transmission electron microscopy

Zoha et al.

Bomberdelli et al.

Stability study Dynamic light scattering method

Transmission electron microscopy

Frankel et al.

1.4.5.4 Applications of phytosome

The novel form of herbal products phytosomes are better absorbed than conventional

herbal extracts. This was observed in SILIPHOSTM

(Silybin phytosome). Silybin is

chief component of silymarin, valued for its ability to protect and restore liver.41

Phytosomes serve as a delivery system consisting of microscopic vesicles that

improve the potential bioavailability, as can be observed in skin care or nutritional

products. The phytosomes of Gingko biloba flavones, glycyrrhetinic acid, terpenes

exhibit enhanced percutaneous bioavailability40

.

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Herbal products in form of phytosomes lead to reduction in dose size. In case of

Grape seed phytosome, one 50 mg of capsule of Grape seed phytosome, in terms of

absorption only is equivalent to 50 mg of regular grape seed extract. But in terms of

biological activity, it is estimated that one 50 mg capsule of grape seed phytosome

may be as effective as 150 mg of unbound grape seed extract40

.

Phytosome as a carrier system may be employed in targeting of the herbal product at

desired site55

.

Table 9: Phytosome Preparation with their Uses

Flavonoid-Rich

Extract

Daily

dosage

Indication

Grape Seed Phytosome

50 to 100

mg

Systemic antioxidant, specific. Best

choice for most people under age of fifty.

Also specific for the eyes, lungs,

diabetes, varicose veins, and protection

against heart disease.

Green Tea Phytosome

50 to 100

mg

Systemic antioxidant. Best choice for

protection against cancer. Also protects

against damage to cholesterol.

Ginkgo Biloba

Phytosome

120 mg

Best choice for most people over the age

of 50. Protects brain and vascular lining;

SILIPHOS™

120 mg

Best choice if the liver or skin needs

additional antioxidant protection.

Milk Thistle Phytosome

150 mg

Good choice when the liver or skin only

needs minor support.

Hawthorn Phytosome

100 mg

Best choice in heart disease or high

blood pressure

Leucoselect Phytosome 50-100 mg Best choice for antioxidant support,

cardiovascular system.

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1.5 Plant profile of Emblica officinalis gaertn

Plate 1. Emblica officinalis plant in natural habitat

1.5.1Biological source

Amalaki consists of fresh fruit pulp of Emblica officinalis Gaertn. (Fam. Euphorbiaceae);

a small or medium sized tree, found in mixed deciduous forests, ascending to 1300 m on

hills and cultivated in gardens and home yards56

.

1.5.2 Geographical Source

It is planted through the deciduous of tropical India and on the hill slopes up to

2000 meter. It is commercially cultivated in the state of Uttar Pradesh in India. It is also

grown in Tamil Nadu, Rajasthan and Madhya Pradesh also.

1.5.3 Synonyms

Sanskrit: Amalaka, Amrtaphala, Dhatriphala

Assamese: Amlaku, Amlakhi, Amlakhu

Bengali: Amla, Dhatri

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English: Emblic Myrobalan

Gujrati: Ambala, Amala

Hindi: Amla, Aonla

Kannada: Nellikayi

Kashmiri: Embali, Amli

Malayalam: Nellikka

Marathi: Anvala, Avalkathi

Oriya: Anala, Ainla

Punjabi: Aula, Amla

Tamil: Nellikkai, Nelli

Telugu: Usirika

Urdu: Amla, Amlaj

1.5.4 Description

(a) Macroscopic57

Fruit, globose, 2.5-3.5 cm in diameter, fleshy, smooth with six prominant lines; greenish

when tender, changing to light yellowish or pinkish colour when mature, with a few dark

specks: taste, sour and astringent followed by delicately sweet taste.

b) Microscopic58

The epicarpic cells are rectangular in shape and their outer and radial walls are highly

cuticularized. In surface view the epicarpic cells appear polygonal in outline with thick

walls. Anomoytic type of stomata are found to be present, but rare. Collateral fibro

vascular bundles are scattered throughout the inner mesocarp. Pitted and helical tracheids

with tapering ends are seen. At places in the phloem, large cavities filled with crystal

mass are present.

1.5.5 Chemistry of Emblica officinalis 59, 60, 61

This herb has many substances, including apigenin, gallic acid, ellagic acid, chebulinic

acid, quercetin), chebulagic acid, corilagin, isostrictiniin, methyl gallate, and luteolin.

Tannins in amla include Phyllaemblicin B, emblicanin A (37%), emblicanin B (33%),

punigluconin (12%) and pedunculagin.

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O HO

O H O H

O H

Fig4: 3,4,5 Trihydroxy benzoic acid (Gallic acid)

Amla is highly nutritious and is an important dietary source of Vitamin C, minerals and

amino acids. The edible fruit tissue contains protein concentration 3-fold and ascorbic

acid concentration 160-fold compared to that of the apple. The fruit also contains

considerably higher concentration of most minerals and amino acids than apples.

Glutamic acid, proline, aspartic acid, alanine, and lysine are 29.6%, 14.6%, 8.1%, 5.4%

and 5.3% respectively of the total amino acids.

The pulpy portion of fruit, dried and freed from the nuts contains: gallic acid 1.32%,

tannin, gum 13.75%; albumin 13.08%; crude cellulose 17.08%; mineral matter 4.12%

and moisture 3.83%. Amla fruit ash contains chromium, 2.5 ppm; zinc 4 ppm; and

copper, 3 ppm.

The following products in a crystalline form from the fruit were identified as geraniin

(1), quercetin 3-b-D-glucopyranoside (2), kaempferol 3-b-Dglucopyranoside (3),

isocorilagin (4), quercetin (5) and kaempferol.

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Fig 5: Chemical structures of phenolic compounds from Emblica officinalis fruit

1.5.6 Uses

Traditionally, the fruit is useful as astringent, cardiac tonic, diuretic, laxative, livertonic,

refrigerant, stomachic, restorative, alterative, antipyretic, anti-inflammatory, hair tonic,

and digestive medicine. It is used for a variety of ailments such as anemia, hyperacidity,

diarrhea, eye inflammation, anomalies of urine, leucorrhea, jaundice, nervine debility,

liver complaints, and cough. It is reported to be effective in the treatment of peptic ulcer

and dyspepsia. It is also reported to have hepatoprotective, antioxidant, antimutagenic,

cyto protective, antitumor, antifungal, antimicrobial, hypolipidemic, and anti

atherosclerotic effects57

.

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1.5.9 Important Formulation

The plant is used in many forms. One of the most popular is as a decoction and infusion

of leaves and seeds. However, it is also used as a liquor, a fixed and an essential oil; in

confection; as a powder and also in paste and pickles. It makes an astringent extract equal

to catechu, which is prepared from the root by decoction and evapouration. The fresh

juice of the round, acidulous fruit is used in combination with that of other Myrobalans –

chebulic (Terminalia chebula) and Beleric (Terminalia belerica) in the form of a

decoction known as Triphala (three fruits). It is used as a cooling and refrigerant sherbet,

and as an astringent medicine in diarrhoea, haemoptysis (spitting blood), haematemesis

(vomiting blood) and other similar conditions58

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1.6 Plant profile of Eucalyptus globulus Labill

\

Plate 2. Eucalyptus globulus plant in natural habitat

1.6.1Biological source:

Tailapar¸ah consists of mature leaf of Eucalyptus globulus Labill. (Fam. Myrtaceae) a

large tree attaining a height of 90 m or more. .

1.6.2 Geographical Source:

Native to Australia, but planted worldwide and introduced in Nilgiris, Anamalai and

Palni hills, Simla and Shillong at an altitude of 1500-2500 m

1.6.3 Synonyms56

Sanskrit : N¢laniry¡sa, Ekalipth, Sugandha Patrah

English : Blue gum, Eucalyptus

Hindi : Yukeliptas

Malayalam : Yukkaalimaram

Marathi : Nilgiri

Tamil : Yukkaalimaram

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1.6.4: Description

a) Macroscopic

Drug consists of mature leaves, more or less scimitar shaped, thick, leathery, greyish-

green, petiolate, up to 26 cm long and 4 cm broad; petioles 2.0 to 3.5 cm long and 0.5 to

1.5 mm thick, sometimes twisted; apex acute to acuminate, base obtuse; midrib

prominent, particularly on the lower surface; margin of leaf entire and somewhat

thickened, brittle and possess numerous brown to dark brown corky warts. In transmitted

light, numerous oil glands can be seen as translucent dots; upper surface smooth, lower

surface slightly rough due to the presence of projecting veins; venation – unicostate

reticulate; lateral veins near the margin forming a continuous line; odour strong and

characteristic.

b) Microscopic

Leaf - T.S. shows typical isobilateral structures with two or three rows of palisade cells

on both upper and lower sides, surfaces show thick cuticle; numerous sunken stomata 199

and large ovoid schizogenous oil cavities of 160 to 200 μ diam.; idioblasts present with

rosettes or prismatic calcium oxalate crystals; rosette crystals 25 to 35μ in size, prismatic

crystals 15 to 25μ in size; vascular bundle of midrib are crescent shaped with one

vascular strand present on each side, all having interrupted patches of sclerenchyma;

corky warts comprising of 10 or more layers of cells; laminary bundles enclosed in

bundle sheath, the cells of which extend to the epidermis on both sides; upper and lower

epidermal cells have straight walls; stomata anomocytic; stomatal index on both upper

and lower surface 5 to 10; the palisade ratio on upper surface 5 to 17 and lower surface 3

to 6.

Powder - Yellowish brown, free flowing, characterized by the presence of cluster and

prismatic crystals of calcium oxalate; epidermis straight walled with sunken stomata;

fibers present.

1.6.5 Chemistry of Eucalyptus Globulus

Essential oil containing terpenes such as 1,8 - cineole, camphene, sabinene, myrcene, p-

menthone, α-and γ-terpinene, fenchone, α- β- thujone, citral, verbenone. Fifteen

compounds were obtained and identified as beta-sitosterol (1), betulinic acid (2),

stigmasterol (3), euscaphic acid (4), 2a-Hydroxybetulinic acid (5), macrocarpal B (6),

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macrocarpal A (7), oleanolic acid (8), 3,4,3'-O-trimethylellagic acid (9), 3-O-

methylellagic acid 4'-O-(2"-O-acetyl )-alpha-L-rhamnopyranoside (10), camaldulenside

(cypellocarpin C, 11), 3-O-methylellagic acid 4'-O-alpha-L-rhamnopyranoside (12), 3-O-

methylellagic acid (13), ellagic acid (14), and gallic acid (15).

Fig 6: Chemical Structure of rutin

1.5.6 Uses

The Eucalyptus leaf water extract presented a remarkable capacity to scavenge all the

reactive species tested, with all the 50% inhibitory concentrations being found at the

mug/mL level. Phytochemical analysis showed the presence of polyphenols such as

flavonoids (rutin and quercetin) and phenolic acids (chlorogenic acid and ellagic acid),

which may be partially responsible for the observed antioxidant activity.

The Eucalyptus plants have antibacterial and antiviral activities, use in traditional

medicine such as in the treatment of airway inflammatory diseases.