Herbal excipients

Herbal excipients

Contents

•       Herbal excipients

•       Diluents

•       Colors

•       Oils

•       Waxes

•       Gums

•       Preservatives

•       Antioxidants

•       Perfumes

Objective

At the end of the session, student will be able to

•       Explain the various excipients used for formulating cosmetics

•       Identify suitable colors for preparing herbal cosmetics

•       Explain the various natural colors available for formulating cosmetics

•       Identify suitable raw materials for preparing herbal cosmetics

•       Explain the various oils available for formulating herbal cosmetics

•       Explain the various waxes available for formulating herbal cosmetics

•       Explain the various gums available for formulating herbal cosmetics

•       Explain the various preservatives available for formulating herbal cosmetics

•       Explain the various antioxidants available for formulating herbal cosmetics

•       Explain the various perfumes available for formulating herbal cosmetics

Herbal excipients

•       Excipients are defined as ‘the substance used as a medium for giving a medicament

•       Pharmaceutical excipients can be defined as non-active ingredients that are mixed with therapeutically active compound(s) to form medicines.

•       The ingredient which is not an active compound is regarded as an excipients. Excipients affect the behavior and effectiveness of the drug product more and more functionality and significantly.

•       Plant derived polymers

•       Synthetic polymers                      

Plant derived polymers

Advantages

•       renewable

•        can be cultivated or harvested in sustainable manner

•       can supply constant availability of raw material

Disadvantages

•       synthesized in small quantities

•       In mixtures that are structurally complex, which may differ according to the location of the plants as well as other variables such as the season

•       Result in a slow and expensive isolation and purification process.

Classification of Herbal Excipients

Excipients are commonly classified according to their application and function in the drug products:

•       Binders, Diluents

•       Lubricants, Glidants, Disintegrants

•       Polishing Film formers and coatings agents

•       Plasticizers, Colorings

•       Suspending agents Preservatives, antioxidants

Raw materials – colors

•       Nature –various colors – ancient man

•       Later – used as cosmetics –dying the hairs, painting lips and faces, coloring food, pharmaceutical and textile products

•       Colorant : Substances added to cosmetics products to colour the product and /or to impart color to the skin and /or its appendages

•       Colour – an dye, pigment or other substance that can impart colour toa food, drug or cosmetics or to the human body

•       Colored compounds – chromogen or bear chromophores  - absorbs light in near UV region

•       Pigments or colors – present – cell sap – anthocyanin (bright red/ blue color), flavonoids, anthroquinone, napthoquinone, carotenoids, indigoids, benzopyrone derivatives and diaryl heptanoids

•       Synthetic dyes – toxic

•       Natural dyes – food colorants – approved as food and medicinal dyes

Annatto – carotenoids

•       Biological source: Dried seeds – Bixa orellana

•       Family: Bixaceae

•       Physical properties: Yellow orange in color

•       Soluble in alcohol, ether, insoluble in water

•       Chemical constituents: oleo resin – Bixin (yellow colored carotenoid) – 2.5%

Uses: coloring agent – cosmetics, food, beverages 

Chlorophyll

Biological source: Green leaves of higher plants and green algae (PRESENT IN CHLOROPLAST)

•       Mixture of 4 pigments – Chlorophyll a (blue black)

                                                                          Chlorophyll b (Green black)

                                                                        Carotene (Orange red)

                                                                        Xanthophyll (Yellow)

Physical properties: Soluble in organic solvent, Slightly soluble in water

Uses: Coloring agents – soaps, oils and cosmetics

Cochineal

Biological source: Dried female insects Dactilopius coccus

Family : Coccidae

Production: Bugs –collected – autumn –protected winter

•       Killed –immersion in hot water or exposure to hot sun

•       Natural exposure  - sun – good quality and variety of dye

•       Heating  - sun –color changes to purplish black color – black grains

•       Burning – sulphur and charcoal fumes –develop purple grey color – black grains

•       Tubular glands  - surface – wax

Chemical constituents: 10 % anthroquinone dye – Carminic acid , 10% fat, 2% wax                                          

•       Uses: Coloring agent – cosmetics, drug, liquid and solid food preparations

Henna (Lawsonia)

Biological source: Dried leaves – Lawsonia inermis

Family : Lythraceae

Chemical constituents: Lawsone – 2,5 – diOH-1,4-naphthoquinone (orange dye)

Uses: Hair dye

          Along with dihydroxy acetone –sunscreen agent

Curcumin - Turmeric

Biological source: Bright yellow coloring material obtained from the rhizomes of Curcuma longa

Family : Zingiberaceae

Solubility: soluble – ethanol, acetic acid

Insoluble – water, ether

Uses: Food colouring agent

Carthamine

Biological source: Carthamin is a natural red pigment derived from safflower, Carthamus tinctorius

Family : Asteraceae

Uses: It is used as a dye and a food coloring. As a food additive, it is known as Natural Red 26.
Carthamin was used as a dye in ancient Egypt. It was used extensively in the past for dyeing wool for the carpet industry in European countries

Crocin  (Saffron)

Biological source: Golden yellow – orange carotenoid pigment obtained from the dried stigmas and upper parts of styles of Crocus sativus

Family : Iridaceae

Solubility: Soluble in hot water and insoluble in absolute alcohol

Uses : Food colourant

Capsanthin (Paprika)

Biological source: Red colour carotenoid pigment obtained from the fruit of Capsicum annum

Family : Solanaceae

Constituents: Carotenoid - Capsanthin

Uses: Coloring agent for food, pharmaceutical, cosmetics and beverages

Lutein (Tagetus)

Biological source: Yellow orange colour carotenoid pigment obtained from the flower of Tagetus erecta

Family : Compositae

Uses: Coloring agent for food, pharmaceutical

Used as additive of chicken feed to give colour to egg yolks

Betanin (Beet root)

Biological source: Red glycoside obtained from the beet root, Beta vulgaris

Family :

Uses: Coloring agent for ice cream, powdered soft drink beverages, soups, in some sugar confectionery

Raw materials - Oils

•       Various fixed oils and volatile oils – base – various creams, lotions, hair conditioners, hair tonics

•       Certain oils –therapeutic properties – tooth paste, mouth washes, gargles

•       Oils  - vegetable origin and mineral origin – cosmetics

•       Mineral origin – Light and heavy liquid paraffin

CASTOR OIL

Biological source: Fixed oil – cold compression – seeds –Ricinus communis

Family : Euphorbiaceae

Physical properties: Pale yellow /colorless, transparent viscous liquid

Mild odour and bland, slightly acrid taste

Chemical constituents: Trigycerides of Ricinoleic acid (87%), Oleic acid 7%, linoleic acid 3%, palmetic acid

Uses: Cosmetics – emollient – lipsticks, hair oil and fixes, eye cream, rouge, stick eye shadow

                                   Topical creams and ointments – 5-12.5%

Almond oil

Biological source: Fixed oil –expression – seeds – Prunus amygdalus

Family : Rosaceae

Chemical constituents: Glycerides of oleic acid (77%), linoleic acid, palmitic acid and myristic acid

Uses: Mild emollient – ingredient – cleansing cream, cold cream and eye cream

Wheat germ oil

Biological source: Fixed oil – wheat germ – Triticum aestivum

Family : Graminae

Chemical constituents: 44 % - linoleic acid, 10 % linolic acid, 30 % oleic acid , 4.7% unsaponifiable matter

Uses: Source of natural vitamin E

Arachis oil

Biological source: Fixed oil – expressed – seeds –cultivated varities – Arachis  hypogaea

Family : Leguminosae

Chemical constituents: Fixed oil

Uses: Preparation – ointments, soaps, emollient, creams and baby oil

Neem oil

Biological source: Fixed oil – fully matures seeds – Azadirachta indica

Family : Meliaceae

Chemical constituents: Glycerides of saturated and unsaturated fatty acids – oleic acid and stearic acid

Uses: Medicated soaps  - skin diseases

 

Raw materials – Waxes

•       Bases – cosmetics – mixture of oils, fats and waxes

•       Unctuous, fusible, viscous solid substances – waxy luster

•       Esters – fatty acids – high molecular weight monohydric alcohol – cetyl alcohol and cholesterol

Commonly used waxes

•       Carnauba wax

•       Pisang wax

•       Castor wax

•       Candelilla wax

•       Bees wax

•       Spermaceti wax

•       Paraffin wax

Carnauba wax

Biological source: Exudates – pores –brazilian wax palm tree- Copernicia prunifera

Family : Palmae

Chemical constituents: Hydroxylated fatty acids – carnuabic acid and cerotic acid

Uses: Hard wax – deodorant sticks and other cosmetics

Bees wax – Oldest forms of wax

Biological source: Wax obtained from the honey comb of bees Apis melifera

Family : Apidae

Chemical constituents: Myricin, melissic acid

Uses: Used in oinments, lipsticks and face creams

Spermaceti

Biological source: Waxy substance obtained from the head of sperm whale Physeter macrocephalus

Family : Physeteridae

Chemical constituents: Acetyl palmitate, free acetyl alcohol, esters of lauric, myristic and stearic acids

Uses : Used as emollient – ointments, cold creams

Carnauba Wax

Biological source: Exudate from the pores of leaves of Brazilian wax palm tree Copernicia prunifera

Family : Palmae

Chemical constituents: Esters of hydroxylated fatty acids – carnuabic, cerotic and melissyl cerotate

Uses: Used in deplitories and deodarant sticks

Myrica Wax

Biological source: Wax obtained from the peels of berry of Myrica cerifera

Family : Myricaceae

Chemical constituents: Palmitic, myristic and lauric acid esters

Uses: Reducess the stickiness of creams and emulsion, used in hair care preparations – excellent holding properties

Rice bran wax

Biological source: vegetable wax extracted from the bran oil of rice Oryza sativa

Family : Graminae

Chemical constituents: Aliphatic acids – palmitic acid, behenic acid and higher alcohol esters like ceryl alcohol, melissyl alcohol, squalene and phospholipids

Uses: Thickener, binding agent with strong emollient properties. Used in lipsticks, balms and sun screens

Raw materials - Gums

•       Hydrophobic or hydrophilic high molecular weight molecules – colloidal properties

•       Natural gums

•       Prepared gums

Natural gums

1. Sea weed gum – agar, algin, carrageenan, laminaran

2. Plant exudates – Acacia, tragacanth, karaya, ghatti
3. Seed gums – Guar gum, isabgol, tamarind, locust bean gum, quince seed gum

Carrageenan

Biological source: Sulphated polysaccharide extract – sea weed – carageen or Irish mass – Gigartina stellata

Family : Rodophyceae

Uses: Hard lotion – Gelling, emulsifying and stabilizing agent

Antitartar tooth paste

Hair setting lotion

Gum Tracaganth

Biological source: Dried gummy exudates – stem – Astragalus gummifer

Family : Leguminosae

Chemical constituents: Tragcanthin – 8-10%, Bassorin – 60 -70%

Uses: Suspending, thickening and emulsifying agent – tooth paste, mascara, skin lotions, non greasy hair cream, barrier cream

Gum Acacia

Biological source: Dried gummy exudate – stem and branches – Acacia senegal

Family : Leguminosae

Chemical constituents: Arabinose, galactose, rhamnose, glyceronic acid

Uses: Suspending, thickening and emulsifying agent – barrier cream, face mask

Locust bean gum

Biological source: Endosperm – seeds – Cerotina siliqua

Family : Leguminosae

Chemical constituents: D – galacto – D –Mannoglycan, 4% Pentan, oxidase and ceratoniase enzyme

Uses: Binder, thickening agent, stabilising agent - cosmetics

Pectin

Biological source: Purified carbohydrate – acid hydrolysis – inner portion – rind  - Citrus peels – Citrus limonii or Citrus auranticum

Family : Rutaceae

Uses: Emulsifying and gelling agent - cosmetics

Xanthan gum

Biological source: Fermentation – bacteria – Xanthomonas compestris on high molecular weight polysaccharides

Chemical constituents: D – glucose, D – glucouronic acid and D - mannose

Uses: Binder, thickening agent – cosmetics

Preparation of antitartar toothpaste and sunscreen preparation

Raw material - Preservatives

•       Preservative - “any substances which are exclusively or mainly intended to inhibit the development of microorganisms in the cosmetic product”.

•        Preservatives help to preserve the formula and ensure the durability of your cosmetic products.

•       They are essential for a formula containing water. Indeed, the presence of water in a formula creates a favorable environment for microorganisms development.

•       Used in cosmetics is essential to prevent alterations caused by microorganisms and contamination during formulation, shipment, storage or consumer use.

Synthetic Preservatives

Advantages
Using synthetic preservatives allows you to have a good understanding of the safety and toxicity profile of the ingredient. Low concentrations of synthetic preservatives effectively preserve the product.

•       Synthetic preservatives have a broad spectrum of activity against bacteria and fungi.

•       They are more affordable than natural preservatives.

Organohalogen compounds

Organohalogen compounds are a large class of natural and synthetic chemical that contain at least one following halogens: fluorine, chlorine, bromine, iodine.

•       Triclosan

•       Methylisothiazolinone

•       Methylchloroisothiazolinone

•       Chlorphenesin

•       Chloroxylenol

Aldehyde and Glycol ethers

•       Formaldehyde

•       Benzylhemiformal

•       Diazolidinyl urea

•       Imidazolidinyl urea

•       2-bromo-2-nitropropane-1,3-diol

•       DMDM hydantoin

•       MDM hydantoin

•       phenoxyethanol

•       2-butoxyethanol

•       2-(2-butoxyethoxy)-ethanol

•       2-(2-ethoxy)-ethanol

Parabens

•       Parabens are a series of parahydroxybenzoates or esters of parahydroxybenzoic acid. They are known as preservatives and used for their bactericidal and fungicidal properties.

•       Methylparaben

•       Ethylparaben

•       Propylparaben

•       Butylparaben

•       Isobutylparaben

Natural preservatives

•       List of the most common natural preservatives found in cosmetic products

•       Benzoic Acid

•       Sorbic Acid

•       Salicylic Acid

•       Alcohol

Antioxidant preservatives

•       An antioxidant is a substance that inhibits oxidation or reactions promoted by oxygen, peroxides or free radicals.

Synthetic antioxidant

•       Butylated hydroxytoluene (BHT)

•       Butylated hydroxyanisole (BHA)

Natural antioxidant

•       Tocopherol (Vitamin E)

•       Ascorbic Acid (Vitamin C)

•       Polyphenols

•       Flavonoids

Raw materials – Antioxidants

•       Cosmetics – prone to spoilage – oxidation of fats, fatty acids and other organic material by atmospheric oxygen

•       Antioxidants – keeps oils and fats from rancid

•       Concentration – 0.02% - 0.1%

Ideal characters

•       Stable

•       Effective over a wide PH range

•       Colorless and odorless

•       Non toxic

•       Compatible – other ingredients and packaging material

Phenolic antioxidants

1. Vitamin E

•       Natural antioxidant – topically applied –UV radiation

•       Shown to reduce – erythema, edema and sun burn

•       Increase SPF  - antiageing effect

2. Gallate – Methyl, ethyl, propyl, octyl gallate

3. BHA – Butyrated hydroxy anisole

4. BHT – Butyrated hydroxy toulene

BHA and BHT

•       Neutalise fee oxygen radicals

•       Prevent auto oxidation of organic materials – rancidity of fats and oils

•       Extend  - product shelf life

•       Effective with EDTA

•       Concentration – 0.01 – 0.1%

•       Preserve and stabilize – creams, lotions, shampoos, make ups and sunscreen lotions

Non - Phenolic antioxidants

1. Vitamin C/Ascorbic acid

•       Protects skin – oxidative damage – UV rays

•       Anti ageing property – avoids hyper pigmentation

•       Anti inflammatory

•       Effect is increased with Vitamin C and E

•       Concentration – 0.2 – 4 %

•       Used  - lotions, creams, sun protection products, shampoos and lipsticks

•        

2. Lecithin – Synergist – phenolic antioxidant

3. Coenzyme Q 10

•       Benzoquinone compound – plant and human tissues

•       Membranes of endoplasmic reticulum, lysosomes, vesicles, inner membrane of mitochondria

•       Because of ability to transfer electron – antioxidant

•       Concentration – 2-6%

•       Anti wrinkle property

4. Grape seed extract

•       Proanthocyanidins

5. Pine bark extract

•       Pyenogenol  -wine, cranberries, green and black tea, black currant onions

Raw materials – Perfumes

•       Per – through, Fumum – smoke

•       Early perfumes – pleasant smells – burning wood and grass

•       Component  -  impart fragrance – cosmetic products

•       Used  - products – bath salt to skin lotions, face creams, sprays, shampoos and aromatic substances

•       Level of fragrances – varies – product to product

•       Face creams – 0.01% fragrance/weight

•       Soap – 0.5% - 3%

Classified

•       Ottos – concentrated principle – natural flowers

•       Floral oils –Rose, jasmine, broom, gardenia, orchid

•       Essential oils – Eucalyptus, peppermint, mint, citrus, vetver oil, clove, lemon and coriander oil

•       Dipropylene glycol

•       Benzaldehyde

•       Benzophenone

•       Benzyl benzoate

 

Summary

•       Colorant : Substances added to cosmetics products to colour the product and /or to impart color to the skin and /or its appendages

•       Natural pigments

•       Various fixed oils and volatile oils – base – various creams, lotions, hair conditioners, hair tonics

•       Certain oils –therapeutic properties – tooth paste, mouth washes, gargles

•       Bases – cosmetics – mixture of oils, fats and waxes

•       Unctuous, fusible, viscous solid substances – waxy luster

•       Esters – fatty acids – high molecular weight monohydric alcohol – cetyl alcohol and cholesterol

•       Hydrophobic or hydrophilic high molecular weight molecules colloidal properties

•       Used in cosmetics is essential to prevent alterations caused by microorganisms and contamination during formulation, shipment, storage or consumer use.

•       Antioxidants – keeps oils and fats from rancid