HERBAL COSMETICS UNIT 2, PCG SEM 2.pptx

HERBAL COSMETICS
M PHARM - PHARMACOGNOSY Sem 2 UNIT 2
S. PRITHIVIRAJAN., M. Pharm
Dept. of Pharmacognosy, COP,
Madurai Medical College,
Madurai-20

CONTENTS
• Commonly used herbal cosmetics
• Raw materials
Oils, Humectants, Colors, Preservatives, Surfactants, and some
functional herbs
• Preformulation studies,
• Compatibility studies,
• Possible interactions between chemicals and herbs,
• Design of herbal cosmetic formulation.

Commonly used herbal cosmetics
• The herbal cosmetics are the preparations containing phytochemical
from a variety of botanical sources, which influences the functions of skin
and provide nutrients necessary for the healthy skin or hair.
• The natural herbs and their products when used for their aromatic value in
cosmetic preparation are termed as herbal cosmetics.
• There is common belief that chemical based cosmetics are harmful to the
skin and an increased awareness among consumers for herbal products
triggered the demand for natural products and natural extracts in cosmetics
preperations.
• The increased demand for the natural product has created new avenues in
cosmeceutical market.

Cleansing agent: Which remove the dust, dead cells, dirt that chokes the pores
on the skin and for skin care, especially in teenager (acne, pimples and
sustaining). Some of the common cleansers include vegetable oils like coconut,
sesame and palm oil.
Toners: The toners help to tighten the skin and keep it from being exposed to
many of the toxins that are floating in the air or other environmental pollutants.
Some of the herbs used as toners are witch hazel, geranium, sage, lemon,
burdock and essential oils.
Moisturizing agent: The moisturizing helps the skin to become soft and supple.
Moisturizing shows a healthy glow and is less prone to aging. Some of the
herbal moisturizers include vegetable glycerin, sorbitol, rose water, jojoba oil,
aloe Vera and iris.
Hair care: The most common cosmetic for hair care include Hair oil, Shampoo,
Hair conditioners, Hair gel, Herbal hair dye.

Miscellaneous: Other miscellaneous cosmetics like Tulsi, Roseroot, Carrot
having Anti aging properties. Shikakai, Chamomile, Wild cherry bark, Henna has
good properties for hair care.
i. Oat: It is a species of cereal grain grown for its seed, Oat oil is rich in
antioxidants, essential fatty acids and natural emollients used in many
lotions, creams, facial oils, and balms.
ii. Ghritkumari: It is a most ingenious mixture of an antibiotic, an astringent
coagulating agent, a pain inhibitor and a growth stimulator used for sunburn,
scratch and a cleansing purge for the body or skin.
iii. Multani Mitti: It is one of the earliest substances to be used to remove
pimple marks, treating sunburn, helps unclog pores, to cleanse the skin of
flakes and dirt.
iv. Haldi: it was used as a face pack along with vertiver and also as an
antiseptic.

v. Chandan & Vertiver. It was teed as scrubs and face packs that were applied
on face and whole body to remove dead cells, regenerate growth of new
cells and give a young look
vi. Tulsi: Tulsi is used as powerful anti- oxidative herb in cosmetics.
vii. Carrot: It is its richness in Vitamin A along with other essentialvitamins,
Carrot seed oil is used as anti-aging, revitalizing and rejuvenating agent.
Rawmaterials used in formulation of herbal cosmetics
There are several raw materials for producing cosmetics ingredients, such
as functional and structural ingredients. Functional ingredients ensure the basic
functionality of the products. These include oils, surfactants, waxes,
preservatives, etc. Some of the imporetant rawmaterials are,

1. Oils:
Oils are derived from vegetable and mineral sources, and are used in
cosmetics. Examples of vegetable oils are almond oil, arachis oil, castor oil,
olive oil and coconut oil. Examples of mineral oils are light and heavy
paraffin.
(i) Almond Oil:
It is a fixed oil obtained by expressing the seeds of Prunus amygdalus,
Family Rosaceae. The oil is pale yellow in colour, with a characteristic odour.
The active principles are mainly the mixture of glycoside with oleic
acid, linoleic acid, myristic and palmitic acid. It has an emollient action, so it
is used in the preparation of creams and lotions.

(ii) Arachis Oil: (Groundnut)
This is also a fixed oil obtained from the seeds of the Arachis hypogea
belonging to the family Leguminoseae. The oil is pale yellow in colour, with a
faint nutty odour. Refined groundnut oil is colourless, with active principles like
oleic, linoleic acid and a small amount of other acids. At 3°C, it is cloudy, at a
lower temperature, it solidifies. It is used in the preparation of hair oils and
brilliantines.
(iii) Castor Oil:
Oil is obtained from the seeds of Ricinus communis belonging to the
family, Euphorbiaceae. It has a slight odour; the oil is either yellow in colour or
colourless. It consists of a mixture of glycosides, in which 80% of ricinoleic
acid is the major constituent. At 0°C it forms a clear liquid. It is used as an
emollient, in the preparation of lipsticks, hair oils, creams and lotions.

(iv) Olive Oil:
This oil is obtained from the fruit of the Olea europea, belonging to the
family, Oleaceae. The oil is either pale yellow or greenish yellow in colour, it
has a slight odour.
It consists of the glycerides of oleic acid, palmitic, linoleic, stearic and
myristic acids. At a lower temperature, it is solid or partly solid. It has
emollient, soothing properties. It is used in the manufacturing of creams, lotions
and bath oils.
(v) Coconut Oil:
This oil is obtained from the dried solid part of the endosperm of the
coconut – Cocos nucifera, family Palmea. It is a white or pearl-white unctuous
mass in winter and colourless in summer.

(vi) Liquid Paraffin: There are two types of Liquid paraffin classified
by its viscosity & weight namely Light, Heavy Liquid paraffin. Viscosity
and weight per ml (0.83-0.87g) are both low in Light Liquid paraffin. Both
having same properties and applications.
It consists of a mixture of hydrocarbons in the form of an oily liquid
which has no colour or odour. It is used in the manufacture of bath oils, hair
oils, brilliantines, lotions and creams, due to its better spreadibility.

2. Waxes: (Humactants)
Waxes are the esters resulting from the condensation of high molecular
straight chain fatty acids with high molecular straight chain monohydric alcohol
of the methanol series. They are used in cosmetics as a base, along with oils and
fats. Commonly used waxes are,
(i) Beeswax:
It is a purified wax separated from the honeycomb of bees, Apis mellifera
which belong to the Family, Apidae. Beeswax is composed of 70% ester myricyl
palmitate. It is yellowish brown in colour, solid, with a honey-like odour.
Under cold conditions it becomes brittle; when bleached, it becomes
yellowish-white solid with a faint characteristic odour. The melting point of
beeswax is 62°C-65°C. Beeswax helps in the incorporation of water to form an
emulsion.

(ii) Carnauba Wax:
This is obtained from the leaves of the Brazilian wax palm, Copernica
cerifera, which belongs to the Palmae family. Carnauba wax is available in
various grades. The highest grade is light-brown to pale-yellow in colour.
It is in the form of moderately coarse powder or flakes, with a
characteristic bland odour. The melting range of this wax is 81°C –86°C. It is a
hard wax and is used in the manufacture of candles, wax varnishes, leather and
furniture polishes.
(iii) Paraffin Wax:
It is derived by the distillation of petroleum. It is a mixture of solid
hydrocarbons consisting mainly of n-paraffins and, to some extent, their isomers.
So, it also called hard paraffin wax. Physically, the paraffin wax is colourless,
odourless or a white, translucent, wax-like solid, which is slightly greasy to
touch. Paraffin wax melts at 50°C-57°C.

3. Colours:
Colours have been used in cosmetics, since time immemorial, by
human beings. Basically, the desire to buy a cosmetic product is controlled by
three senses, namely, sight, touch and smell. So colour is one of the most
important ingredients of cosmetic formulations.
Colour is a visual sensation which can be caused by a definite
wavelength or a group of wavelengths by an object through one or more of
the following phenomena – emission, refection, refraction or transmission.
(i) Cochineal:
Cochineal is a red dyestuff derived from the dried female insect, Dactilopius
coccus, which belongs to the Coccidae family. Carminic acid is the main
colouring constituent in cochineal. On crystallization, carminic acid forms red
needles and at 130°C, the needles darken and also carbonize at 250°C.

For the preparation of caramine, the cochineal is extracted with water.
Alum is added to this solution to precipitate the red aluminium salt called
carmine lake.
(ii) Saffron:
It consists of the stigmas and tops of the styles of the plant, Crocus
sativa, which belongs to the Iridaceae family. It is a perennial plant grown in
Jammu and Kashmir in India. Saffron powder is yellowish and is easily soluble
in water, so it is used as a flavouring and colouring agent in food preparations.
Saffron contains a number of carotenoids – crocin is an important
natural saffron carotenoid. Picrocrocin is a colorless bitter glycoside
responsible for saffron’s characteristic odour.
(iii) Chlorophyll:
It is the natural green pigment, found abundantly in nature. It is the
component that is responsible for photosynthesis.

(iv) Alkanet
Alkanna Tinctoria Root Extract is a herb and belongs to the Borage family.
The Alkanet roots give you darker shades like dark red pigment. It is
hydrophobic, and the major chemical pigment is Alkannin.
(v) Beetroot
Beta vulgaris or extract is another excellent coloring agent which is
hydrophilic in terms of solubility. The major chemical pigment used in the
colorant is Betanin and it is high in red color. This is a popular colorant used in
water-based cosmetics. Betanin degrades while exposed to light, oxygen, and
heat.
(vi) β-Carotene
This is a yellow-to-orange dye you obtain from the fungus called
Blakeslea Trispora. It also beholds high stability with acid, heat, light, and alkali.

4. Surfactants
Surfactants are materials that lower the surface tension (or interfacial
tension) between two liquids or between a liquid and a solid. These are
classified based on the charge of the polar head of the surfactant which can
have a positive charge (cationic), a negative charge (anionic), or no charge
(non-inonic). Amphoteric surfactants have both a cationic and anionic part
attached to the same molecule.
Anionic – Anionic surfactants are the most commonly used surfactants because
they tend to provide the best cleaning power and the most foam. the most
commonly used anionic surfactants is SLS (Sodium lauryl sulfate or Sodium
Laureth Sulfate).
Nonionic – They don’t ionize in water or aqueous solutions. Nonionic
surfactants are gentler when cleaning. Because they don’t carry a charge, they
are the most compatible with other types of surfactants.

Cationic – Cationic surfactants not give foaming like the other types of
surfactants. They are often used in hair care products (mainly conditioners
and anti-static products because they don’t provide the foaming for use in
shampoos) because their positive charge is attracted to the negative charge
in hair. This makes it difficult to completely wash them from hair, so some
stays behind to help reduce friction between hairs which, in turn, reduces
the amount of electrostatic charge in hair. This helps make hair more
manageable and helps prevent damage.
Amphoteric – Amphoteric surfactants can carry either a positive or negative
charge depending on the pH of your product. Despite that, they are still
compatible with all of the other types of surfactants. These tend to be very
mild surfactants which is why they are usually combined with other
surfactants.

In the preparation of cosmetics, there are mainly five uses for which
surfactants are used.
- Detergency - Wetting - Foaming - Solubilization
A natural surfactant has to have both the head and tail groups to
come from truly natural sources. Natural surfactants can be derived from many
types of plants. Common sources are coconut or palm, but they can also be
derived from other types of fruits and vegetables. 5 plant-derived non-ionic
surfactants are as follows:
1. Disodium Laureth Sulfosuccinate: Disodium laureth sulfosuccinate is a
gentle anionic surfactant. Its larger molecules are unable to penetrate and irritate
the skin, making it the preferred choice for use in products formulated for
sensitive skin

2. Coco Glucoside: Coco glucoside is a non-ionic natural surfactant with an
alkaline pH around 12. It is a gentle foamy cleanser derived from coconut oil
and fruit sugars and is completely biodegradable.
3. Decyl Glucoside: Decyl glucoside is also obtained from coconut oil and
glucose and is completely biodegradable. It is similar to Coco Glucoside except
that it has a shorter chain length and creates less foam. The foam that is created
is less stable.
4. Lauryl Glucoside: Lauryl glucoside is similar to Coco glucoside and Decyl
glucoside but with a longer chain. It is also more viscous. Lauryl Glucoside
takes the longest to foam but the form that is created is also the most stable.
5. Coco Betaine: Coco betaine is a mild, coconut-based amphoteric surfactant
with a pH around 6-8. It is completely biodegradable and increases the form and
viscosity of products to which it is added.

5. Preservatives:
These are the agents which are used to prevent spoilage of cosmetic
products. They are products of the oxidation of oils and fats and also the growth
of microorganisms. Most cosmetic preparations, especially those containing
water are likely to deteriorate if preservatives are not added.
Broad-spectrum preservatives:
Phenoxyethanol + Caprylyl Glycol and Phenoxyethanol + Ethylhexylglycerine
are broad-spectrum preservatives based on the mixture of an active
ingredient fungicidal, piroctone olamine, Phenoxyethanol, and natural emollient,
which improves the active ingredient's antimicrobial activity through its
connection to the cell membrane of the microorganisms, which prevents
bacterial and fungal growth in a high degree.

 Preservatives are essential components of cosmetic formulations that
provide numerous benefits, ensuring the quality, safety, and efficacy of
personal care products.
 Essential oils are volatile aromatic compounds derived from plants. Many
essential oils possess antimicrobial properties that can inhibit the growth of
microorganisms. Examples of essential oils commonly used as natural
preservatives in skincare include tea tree oil, rosemary oil, lavender oil, and
thyme oil.
 Plant extracts, derived from various parts of plants such as leaves, stems,
and flowers, can also offer preservation benefits. Some plant extracts contain
natural antimicrobial compounds that help inhibit the growth of
microorganisms. Common examples include grapefruit seed extract, rosemary
extract, and neem extract.

Grapefruit Seed Extract
Also labeled as GSE, this natural preservative has been around for
decades. High in healthy antioxidants like vitamins E and C, grapefruit
seed supports healthy, glowing skin.
Tocopherol
A vegetable-derived compound of vitamin E, tocopherol is a great natural
preservative for cosmetics because as an antioxidant, it helps to repair and
fortify the skin against environmental damage.
Rosemary
This fragrant antioxidant adds aromatherapy benefits to products, while also
helping to keep them bacteria-free. It is a natural antibacterial known to calm
the skin and effectively fight breakouts.

Neem oil
Neem oil is a natural, bioactive plant extract obtained primarily from
neem seeds. It has excellent antimicrobial, antioxidant, pesticidal and
insecticidal properties rendering it an attractive alternative to synthetic
chemicals in application of food preservation, packaging and storage.
Properties of Preservatives:
An ideal preservative must possess the following attributes,
1. It should be compatible with the formulation.
2. Soluble to the extent needed to achieve an effective concentration.
3. Stable enough to provide a sustained antimicrobial effect.
4. Colourless and odourless or nearly so.
5. Non-irritant and non-allergic in the concentrations used.

Classification of Preservatives
• Organic Acids – Benzoic acid, Formic acid.
• Alcohols – Ethyl alcohol, Isopropyl alcohol.
• Aldehydes – Formaldehyde, Cinnamic aldehyde.
• Phenolics – Cresol, Phenol.
• Esters – Methyl p-hydroxy benzoate, Ethyl p-hydroxy benzoate.
• Mercury – Thiomersol, Nitromersol.
• Surface Active Agents – Benzalkonium chloride, Cetyl pyridinium chloride.
• Miscellaneous Compounds – Ethyl Vanillin and Vanillin.

Functional Herbs
Functional herbs have been used as flavor, colour, aroma, enhancing
agents and for preservation of foods. There has been increasing studies on the
role of herbs as natural preservatives and for medicinal purposes.
1.Lavender
Lavender belongs to a class of herbs called nervines, which support a
healthy nervous system and a sense of balance in the body. Lavender is one of
the best-studied herbs for creating a sense of calm.
2. Rosemary
Rosemary supports memory and cognitive function; it’s a nootropic,
meaning it boosts brain function. It’s most widely known for that purposes. In
herbalism, it’s also considered a carminative, or digestive tonic, and it’s said to
support healthy circulation, too.

3. Lemon balm
Lemon balm is a nervine and a member of the mint family. It has a
somewhat citrusy flavor, which comes from the terpene limonene. Limonene,
as a compound, is popular for supporting a sunny mood. And while lemon balm
does not have sedative properties, it’s great before bed because of its calming
properties.
4. Oregano
Robinett keeps oregano oil with her to use when her immune system
needs a boost—it’s naturally antibacterial, antifungal, and antiviral. Most often,
she takes it orally when she’s traveling or applies it topically to cuts and
scrapes. Plus, once it flowers, oregano tends to attract and support bees and
other insect pollinators.

5. Peppermint
Peppermint is great after a meal while your settles. It has cooling
properties to brush teeth with peppermint toothpaste or apply peppermint oil to
skin. Because it’s cooling, people may find it soothing for conditions with hot
qualities, like acid reflux or certain kinds of headaches. Some people use it
when they get hiccups, too.
LAVENDER ROSEMARY LEMONBALM OREGANO PEPPERMINT

Preformulation studies involved in herbal formulations
Preformulation is a group of studies that focus on the physicochemical
properties of a new drug candidate that could affect the drug performance and the
development of a dosage form.
This could provide important information for formulation design or
support the need for molecular modification. Every drug has intrinsic chemical
and physical properties which has been consider before development of
pharmaceutical formulation.
Preformulation study is done to develop the elegant, stable, effective and
safe dosage form by establishing kinetic rate profile, compatibility with the other
ingredients and establish Physicochemical parameter of new drug substances.
The major principles involved in preformulation studies are,

Organoleptic Characters
Color: If the color is undesirable or variable, incorporation of a dye in the final
product is recommended
Taste: If taste is considered to be unpalatable, a less soluble form of the drug
(salt or prodrug) ought to be considered.
Odor: The substance may exhibit an inherent odor characteristic of major
functional groups present. Odor greatly affects the flavor of a preparation or food
stuff.
Physical Description & Bulk Characterization
Drugs can be used therapeutically as solids, liquids and gases. Solid
materials are preferred in formulation work because of their ease of preparation.
The majority of drug substances in use occur as solid materials.

Most of them are pure chemical compounds of either,
• Amorphous (higher solubility)
• Crystalline in nature (higher stability)
• Polymorphism
Amorphous drugs have randomly arranged atoms or molecules. Amorphous
forms are typically prepared by precipitation, lyophilization, or rapid cooling
method.
Crystalline Drugs are characterized by repetitious spacing of constituent atoms or
molecules in a 3-D array. Amorphous Crystalline forms of drugs may be used
because of greater stability than the corresponding amorphous form.
Polymorphism is the ability of a compound to crystallize as more than one
distinct crystalline species with different internal lattices or crystal packing
arrangement even they are chemically identical depending on the variation in
Temperature, Solvent, Time

Hygroscopicity
Many drugs, particularly water-soluble salts, have a tendency to adsorb
atmospheric moisture. Changes in moisture level can greatly influence many
parameters such as, chemical stability, flowability, and compatibility.
Adsorption and equilibrium of moisture content can depend upon
atmospheric humidity, temp, surface area, exposure, and the mechanism for
moisture uptake, Analytic methods for monitoring the moisture level are
Gravimetric Method, Karl Fischer titration, Gas chromatography
Fine Particle Characterization
Size, shape & surface morphology of drug particles affect the flow
property. dissolution & chemical reactivity of drugs. The effect is not only on
the physical properties of solid drugs but also, in some instances, on their
biopharmaceutical behavior.

Particle size of drugs may affect formulation and product efficacy.
Certain physical and chemical properties of drug substances are affected by
the particle size distribution including:
Drug Dissolution Rate, Content Uniformity, Texture, Stability, Flow
Characteristics, & Sedimentation Rates.
Thermal Effects
Differential scanning calorimetry and Differential thermal analysis
[DSC & DTA] Measure the heat loss or gain resulting from physical or
chemical changes within a sample as function of temperature.
Thermo gravimetric analysis (TGA) - Measure changes in sample weight as a
function of time (isothermal) or function of time (isothermal) or temperature.
De-solvation and decomposition processes are frequently monitored by TGA.
Also to investigate Purity, polymorphism, solvation, degradation, and
excipient compatibility and predict any physicochemical interactions between
components in formulations

Powder Flow Properties
Flow properties are significantly affected by Changes in particle size,
density, shape, and adsorbed moisture, which may arise from processing or
formulation.
The powder flow properties can be characterized by the following methods:-
1.Angle of Repose 2.Compressibility
Angle of repose - It is the maximum angle between the surface of a pile of
powder and horizontal plane.
Tan = h/r
The rougher and more irregular the surface of the particles, the higher
will be the angle of repose. Lower values indicate better flow characteristics.
Compressibility - It is characterized by Carr's compressibility index.
Carr's compressibility = Tapped density-bulk density × 100
indexcarr's index(%) Tapped density

Solubility analysis
The solubility of drug is an important physicochemical property because
it affects the bioavailability of the drug, the rate of drug release into the
dissolution medium, and consequently, the therapeutic efficacy of the
pharmaceutical product.
The solubility of a material is usually determined by the equilibrium
solubility method, which employs a saturated solution of the material, obtained
by stirring an excess of material in the solvent for a prolonged period until
equilibrium is achieved.
General rules - Polar solutes dissolve in polar solvents
Non-polar solutes dissolve in non-polar solvents

lonization constant
For a compound containing basic or acidic functional groups, solubility at
a given pH is influenced by the compound's ionization characteristics.
The solubility of a compound in aqueous media is greater in the ionized
state than in the neutral state. Thus, solubility of ionizable compounds is
dependent on the pH of the solution.
Considerations for an ionizable compound include the impact of
ionization on stability and permeability. The Henderson-Hasselbalch equation
provides an estimate of the ionized and un-ionized drug concentration at a
particular pH.

pH Solubility profile
It is a set of solubility values at specified pH values. The values given in
a pH profile refer to solubility as a function of pH for all species of
thecompound (ionizable and neutral) in solution.
Partition coefficient
Measure of a drug's lipophilicity and an indication of its ability to cross
cell membranes. Defined as the ratio of un-ionized drug distributed between
the organic and aqueous phases at equilibrium,
Po/w = (Coil/C water) equilibrium
P>1 - Lipophilic drug P<1 - Hydrophilic drug.
For drug delivery, the lipophilic/hydrophilic balance has been shown to
be a contributing factor for the rate and extent of drug absorption.

It provides a means of characterizing the lipophilic/hydrophilic nature of
the drug. Commonly determined using an oil phase of octanol or chloroform
and water.
Dissolution
Dissolution rate data, when combined with the solubility, partition
coefficient. and pka results, provide some insight into the potential in-vivo
absorption characteristics of drug entity.The dissolution rate of drug substances
may be affected by Chemical form, pH, and different salt forms may give
significant differences.

Stability analysis
Development of a drug substance into a suitable dosage form requires the
Preformulation stability studies of drug under the following categories,
Stability study in toxicology formulation
Stability study in solution state
Stability study in solid state
Stability study in toxicology formulation
Solid state stability - Identification of stable storage conditions for drug in the
solid state and identification of compatible excipients for a formulation.
Drug-excipient stability profile - Hypothetical dosage forms are prepared with
various excipients and are exposed to various conditions to study the
interactions of drug and excipients.

COMPATABLITY STUDIES
Drug substances are usually combined with excipients which serve
different and specialized purpose. Although excipients are pharmacologically
inert, they can undergo chemical reactions and physical interactions with drug
substances under favorable environmental conditions.
These interactions can lead to instability resulting in the formation of
new entities with different physicochemical properties and pharmacological
effects. Active ingredient- excipient compatibility studies have been used to
obtain rapid stability assessment of drug and excipients, drug stability are
investigated under the stress conditions
There are mainly three types of incompatibility found.
(I) Physical Incompatibility (II) Chemical Incompatibility
(III) Physiological Incompatibility

(1) Physical Incompatibility
Physical interactions may result in changes in dosage uniformity, color,
odor, flow properties, solubility, sedimentation rate, dissolution rate ete
Incompatibilities are assessed by physically observing the test samples.
(2) Chemical Incompatibility
This involves the interaction of drug substance and excipient through
chemical degradation pathway. Chemical interactions can be in the form of
hydrolysis, oxidation, racemization, polymerization, Maillard reactions,
photolysis etc.
(3) Physiological Incompatibility
Those interactions occur after the drug product has been administered
to the patient. The interaction is between the medicine drug substance and
excipients and the body fluids.

Analytical Methods to Check Incompatibility,
(a) Thermal methods of analysis
- Differential Scanning Calorimetry (DSC)
- Differential Thermal Analysis (DTA)
(b) Accelerated Stability Study
(c) Diffuse Reflectance Spectroscopy (DRS)
(d) Chromatography
- Self Interactive Chromatography (SIC)
- Thin Layer Chromatography (TLC)
- High Pressure Liquid Chromatography (HPLC)

Differential Scanning Calorimetry (DSC)
DSC is widely used to investigate and predict any physicochemical
interaction between drug and excipients involving thermal changes. The pre-
formulation screening of drug-excipient interaction requires (1: 1) Drug:
excipient ratio, to maximize the like hood of observing an interaction. Mixture
should be examined under N2 to eliminate oxidative and pyrrolytic effects at
heating rate (2, 5 or 100 c/min) on DSC apparatus.
Differential Thermal Analysis (DTA)
Thermal Analysis is useful in the investigation of solid state interactions.
It is also useful in the detection of eutectics. Thermo-grams are generated for
pure components and their physical mixtures with other components. In the
absence of any interaction, the thermo- grams of mixtures show patterns
corresponding to those of the individual components.

Accelerated stability study
Different formulations of the same drug are prepared. Samples are kept at
40°C/75% RH. Chemical stability is assessed by analyzing the drug content at
regular interval. Amount of drug degraded is calculated. For this, & Drug
decomposed VS time (month) is plotted

Diffuse Reflectance Spectroscopy (DRS)
Principle of DRS is based on the "Penetration of a portion of incident
radiation flux into the interior of the solid sample, return of some portion of
radiation to the surface of sample following partial absorption and multiple
scattering at boundary of individual sample partides DKS detect the
decomposed products, along with physical and chemical adsorption of
excipients on to AP1 and vice versa.

Chromatography
(1) Self Interactive Chromatography (SIC)
SIC is useful for proteinous drug and excipients. It is a modified type of
affinity chromatography, Here, drug is made immobilized as the stationary
phase & solution to be tested (excipient soln.) acts as mobile phase Measure Rt
(Retention time) & compare with non-retained marker.
For different mobile phases (i.e. different excipients) the injected drug
have different interactions (may be repulsive or attractive) with the stationary
phase of drug leads to shift in retention time (Rt).
A. When interaction is repulsive, a sharper peak is
obtained at a shorter retention time.
B. When no net interaction between the
immobilized drug, Rt-dead volume of column.
C. When attractive interactions, it will have longer
retention time & wider peak.

Thin Layer Chromatography (TLC)
TLC is generally used as confirmative test of compatibility after
performing DSC. Stationary phase (SP) consist of powder (Silica, Alumina.
Polyamide, Cellulose & lon exchange resin) adhered onto glass, plastic or metal
plate. Solution of Drug-Excipient mixture are prepared & spotted on the same
baseline at the end of plate.
The plate is then placed upright in a closed chamber containing the
solvent which constitutes the mobile phase (M.P.)
Any change in the chromatograph such as the appearance of a new spot
or a change in the Rf varies of the components is indicative of an interaction.
The technique may be quantitated if deemed necessary. If significant interaction
is noticed at elevated temperatures, corroborative evidence must be obtained by
examining mixtures stored at lower temperatures for longer durations.

High Pressure Liquid Chromatography (HPLC)
• High-performance liquid chromatography is the most recent technique. The
stationary phase may be a solid or liquid on a solid support. The mechanisms
responsible for distribution between phases include surface absorption, ion
exchange, relative solubilities, and steric effects.
• This method was used for alkaloid metabolite extraction and analysis. A simple
reversed phase liquid chromatographic method has been developed for the
simultaneous quantitation of four anticancerous alkaloids, vincristine,
vinblastine, and their precursor's catharanthine and vindoline, using a specific
HPLC column.
• The active pharmaceutical ingredients (APIs) and model compounds of
diversified chemical structure are studied.

Possible interactions between chemicals and herbs
Herb–drug interactions are important issue for clinical therapeutic efficacy
of medicine treatment. Herb–drug interactions affect either
the pharmacokinetic activities or pharmacodynamics activities of drugs, leading
to therapeutic failure or toxicities.
Pharmacokinetic Mechanism of Interaction
Such interaction involve in the alteration of pharmacokinetic parameters
of herbs under the influence of chemicals This kind of interaction is associated
with absorption, distribution, metabolism and excretion of the herbal
formulation. These changes are basically modifications in the concentration of
the drugs.
• Alterations of absorption (I e. slippery elm reduces absorption of thymine
(helps to regulatemetabolism) & lithium (a mood stabilizer)

• Changes in the gastrointestinal pH (le changing the stomachs acid
environment which can affect howmuch of a medicine is absorbed).
• Adsorption, chelation and other complex's (Le. two products combining
and affecting the solubility or absorption).
• Changes in Gastro intestinal motility (how quickly a drug passes through
the system).
• Protein binding can affect how much of a drug is available for absorption.
• Horse chestnut binds with plasma and tissue proteins and competes
against warfarin, a medicine used to prevent blood clots
• Changes in metabolism and elimination resulting in either increasing or
decreasing the amount of drug available to have an effect.

• The interaction may involve a herb causing either an increase or decrease in the
amount of drug in the blood stream.
• A decrease in drug dosage by virtue of an interaction could make the drug
ineffective.
• An increase in drug dosage could make it reach levels that produce side effects.
(II) Pharmacodynamic Mechanism of Interaction
Alterations in the way a drug affects a tissue or organ system. These
interactions result in either enhancing or antagonizing effects. Change in first
pass metabolism (the way the liver processes a drug)
 Grapefruit juice inhibits a transport protein that acts as a pump to move drugs
across the cell wall, which can lead to higher levels of many drugs
 Digoxin (controls heart rate), some preparations with laxative effect (aloe,
liquorice) decrease potassium and increase digoxin toxicity.

 Theophylline (eases breathing), any preparation that has stimulant effects i.e.
caffeine (including guarana) may have additive central nervous system effects
and increase theophylline levels.
 Herbal products with a diuretic affect (including caffeine products) a problem
for patients on lithium which helps to stabilize mood.
 Warfarin (prevents blood clots), increased risk of bleeding with products that
have a coumarin component (black cohosh, chamomile) or antiplatelet effects
(bilberry leaf, fish oil, vitamin E and ginger, garlic), cranberry.
 St John's Wort and certain antidepressants, can cause 'serotonin syndrome' a
serious condition marked by confusion, incoordination, and cardiovascular
irregularities.
 Garlic & Warfarin increases inhibtion of platelet aggregation leading to
increased bleeding, bruising (Garlic for high cholesterol and blood pressure).

DESIGN OF HERBAL COSMETIC FORMULATION
Various marketed herbal cosmetic products are available for skin, hairs,
lips, eyes etc. Herbal cosmetics are more beneficial in the cosmetic and
therapeutic application than other synthetic cosmetics.
The herbal cosmetics are defined as which are having various herbal
ingredients and herbal extracts. The best thing about the herbal cosmetics is
that it is purely made by the herbs and shrubs.
Some common beautifying agents incorporate creams, face packs and
scrubs, hair oils, hair hues, shampoos, hair conditioners, lipsticks, bash on or
rouge as it is at times known, eyeliners, mascaras, foundations and eye shadow,
perfumes and scent & cleansers.

The natural-Ingredients are isolated from a plant and chemically
purified, Ingredients are naturally derived but require significant chemical
synthesis to produce. Also, the ingredient is not normally used, The majority of
natural products on the market would be considered green washed.
Natural additives are the substances added directly to cosmetic product
during processing, as for preservation, colouring and stabilization. OR Natural
additives lend their own special qualities by adding nature's own nutrients and
providing a unique look, colour, texture and aroma.
Herbal cosmetics formulation can be designed as Powders, Lotions,
Emulsions, Solutions, Suspensions, Creams, Pastes, Gels, Sticks

(a) Face Packs
Face packs are the preparations, which are applied topically to facial
areas having high affinity to keratin and they remain on skin surface. It is used
for the purpose of achieving tightening sensation and a cleaning effect in the
area of application.
• Face packs contain colloidal clay, kaolin or other suitable solids dispersed in
a liquid vehicle. It also contain humectants (ie. Glycerol) to prevent a
complete-dehydration of pack film in order to maintain plasticity of film
sulfonated oils are used which also enhances cleaning efficiency.
• There are other materials used in packs, for example, Alumina, Fuller's
earth, Bone carcall and Kieselghur for its Cleaning activity by adsorptive
efficiency. Soluble colors are used to tint preparations & Zinc Oxide, Titanic
Dioxide and other materials like filtered honey crushed almond and
preservatives.

(b) Cold Cream
These are used for cleaning, moisturizing, protective and also acts as
sun screen creams. Cold creams become harder and more lustrous, A smooth
consistency of cold creams can be achieved by reducing warm component or
adding lanolin or absorption base.
(c) Vanishing Creams
Vanishing creams are so termed because upon application and rubbing
them into the skin. -there remains little or no visible evidence of their former
presence.
The basic nature of vanishing cream is oil in water emulsions. There two
types of vanishing creams available in markets; one is light vanishing cream,
which has low binding capacity to powders and the other is heavy vanishing
cream, which has strong capacity to bind with powders. Heavy vanishing creams
as known as foundation creams, which are used as skincare products.

(d) Shampoo
Shampoo can be defined as a preparation of a surfactant in suitable form
of liquid, solid or powder, which when used under specified condition will
remove surface grease, dirt and skin debris from hair shaft and scalp.
The formulation of a Shampoo should have special capabilities like
minimizing eye sting, controlling dandruff or imparting appealing fragrance.
The major component of the shampoo is surfactant (soaps and synthetic
detergent) with other additions like conditioners,sequestering agents, rinsing
components (acids), foam builders, opacifying agents, clarifyingagents (EDTA)
anti-dandruff agent, thickening agent, preservatives, stability additives andother
cosmetic additives (perfumes and dyes).

(e) Hair Conditioners
Hair conditioners are the preparations, which maintain the condition of
hairs. The products containing proteins, such as collagen derived Pepticles,
(ie, casein albumin) which act optimum at pH 6.0 and are absorbed in to the
damaged hair shaft are to maintain conditions of hair.
The product-containing surface active agent, act as ceroplastic and
substantive to hair. It absorb by damaged hair to maintain its electrostatic
nature. eg, tetra alkyl substituted amine salt.
The oil and wax containing products labricate the hair shaft and
improve optical properties of hairs, eg. Frilliantine, cholesterol lanolin
silicone oil, etc.

(f) Talcum Powders
Talcum powders are the protective preparations again mechanical stress,
which act as skin lubricants and cooling agent. Minute particles of powder have
large surface are results in strong light dispersion, which usually covers the skin
underneath. The talcum powder consists of talc as main ingredient with
additives lie absorbent. adherent, covering agent, perfumes, heat conducive
agents, fragrance and antioxidants.
(g) Tooth Powders
Tooth powder is a preparation used for cleaning as well as therapeutic
dentifrices. Most commonly used formulations consist of calcium carbonate as
polishing agent, sodium soap like sodium lauryl sulfate as surface active agent,
mixture of insoluble metaphosphate and Tricalcium phosphate as an abrasive
Various tooth powders an available in the market, which are formulated
according to their active constituents

(h) Tooth Paste
Toothpastes are the preparation intended for use with tooth brush to the
purpose of cleaning the accessible surface of the bed. It enhance personal
appearance by maintaining cleaner wet bushing with it reduce tooth decay. The
general formulation of toothpaste contains various ingredients to their special
properties
• Abrasives - it removes debris, residual stains from teeth. Commonly used
agents are Calcium carbonate, Tricalcium phosphate,
• Surface-active agents –It use the surface tension to improve cleaning and also
for foaming characteristics eg sodium lauryl sulphate, sodium coconut
monoglyceride sulfanate, and sodium N-lauryl succinate etc
• Humectants - It is used to retain moisture or prevent hardening of pate when
it is exposed to air. Eg. glycerol, Sorbitol and propylene glycol, etc.

• Binders - These are used to prevent separation of liquid phase from solid,
particularly during savage. Eg. glycerite of starch, natural tree exudates,
seaweed colloids
• Flavors - These are used to impart the taste of paste. Most commonly flavors
used in pastes are spearmint, peppermint, winter green, cinnamon-mint.
(i) Lipsticks
Lipsticks is composed essentially of an oil-wax base, stilt enough to
form a stick with a staining dye dissolved or dispersed in the oil, and pigment
suspended there in suitably perfumed and flavored, molded and enclosed in a
case. Other ingredients which are used in lipstick formulation are
preservatives, fragrances, surfactant and stabiliren, emulsifiers and
antioxidants etc.

(j) Eye Liners
It is the oldest and most extensively used cosmetics for enhancing the
eyes. formulation of eyeliner consists of pigments or dyes, waxes, oils, gums,
esters, preservatives, Pearle scent and perfumes etc. The coloring agents
which are most commonly used are carbon black, iron and chromium oxide
pigments, carmine NF and cochineal etc.

HERBAL COSMETICS UNIT 2, PCG SEM 2.pptx

HERBAL COSMETICS UNIT 2, PCG SEM 2.pptx

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