Formulation Challenges of herbal cosmetics

1. CHALLENGES IN
HERBAL COSMETICS
Foram Machhar
Mpharm Sem-2
Roll no. 05
Department of Pharmaceutics

2. Introduction
• Cosmeceutical products are those poised
on the gap between cosmetic products that
simply cleanse and beautify and
pharmaceuticals that cure and heal.

3. Cosmeceuticals includes:
(i) beauty supplements like dietary supplements
(capsules, tinctures);
(ii) active cosmetics, which contain “active”
ingredients;
(iii) bioactive cosmetics, which contain “bioactive”
ingredients;
(iv) Performance cosmetics cosmetics;

4. (v) phytocosmetics, which are made with natural
ingredients from plants;
(vi) functional cosmetics, which perform a function
beyond the cosmetic;
(vii) dermaceuticals;
(viii) skinceuticals;
(ix) cosmetic drugs; and
(x) therapeutic cosmetics.

5. • Herbs have been used to maintain and enhance
human beauty because they have a lot of
functional properties.
• Herbal products are well researched and tested
for mildness, efficacy, biodegradability, low
toxicity, cleansing ability, emulsification,
moisturization, skin appearance, feel, fragrance,
and lubrication.

6. Application of herbs in cosmetic
product
Botanical extracts are multifunctional in nature because
they possess various properties :
 photoprotection,
 antiaging,
 moisturizing,
 antioxidant,
 astringent,
 Antiirritant
 antimicrobial activity,
which are
correlated
with each other.

7. Exposure of skin to sunlight and other atmospheric
conditions causes production of reactive oxygen
species, which can react with DNA, proteins, and
fatty acids, causing oxidative damage and
impairment of antioxidant system. Such injuries
damage regulation pathways of skin and lead to
photoaging and skin cancer development

8. The effects of aging include wrinkles, roughness,
appearance of fine lines, lack of elasticity, and de-
or hyperpigmentation marks. Herbal extracts act
on these areas and produce healing, softening,
rejuvenating, and sunscreen effects
• As an active ingredient in herbal cosmetics, there
are some phytoconstituents and herbal extracts
can be used.

9. The activeingredientof the herbal formulations maybe availablein the crudepowder form or
phytoconstituent.The crude drug powders can be water soluble,water insoluble,fibrousor poorly
wettable,the phytoconstituentsmay be inthe form o f concentrated extract,resinous,solublepowder or
liquid extract.There are variouschallengesto be addressedfor the phytoconstituentsdue to some
propertiesit possess.
Crude drug Powder or Mixture of
powder
Water insoluble
Water soluble
Fibrous
Poorly wettable
Granular
Phytoconstituent
Concentrated extract
Resinous (maybe alcohol)
Soluble powder (water)
Liquid extract
Herbal (active constituent)

10. • Various drawbacks are identified based on the properties of
phytoconstituents and thus combat against it, novel herbal drug
delivery system is developed.
• Several polyphenols have been formulated into that could solubilize,
stabilize or increase their bioavailability.
• Examples include the following: self-emulsifying delivery systems,
lipid nanocapsules, nanoemulsion or liposomes. All formulations
appear to improve the solubility of the various polyphenols e.g.,
resveratrol, quercetin, curcumin, and epigallocatechin gallate.
• Essential oil is blend of variety of volatile molecules terpenoids,
phenol-derived aromatic components and aliphatic component.
Thus they are highly volatile and face the challenge of unstability.
Nanocapsulation can be done for their capability of decreasing
volatility, improving stability, water solubility and efficacy of essential
oil-based formulations. Several other phytoconstituents and their
novel herbal delivery is shown in the following tables.

11. Phytoconstituents used:
Category of
Phytoconstituents
Examples of
phytoconstituents
Nature
Phytosterols Campsterol, stigmasterol,
betasitosterol, soyasterols
Lipophilic
Volatile oils Jojoba oil, citronella oil,
thyme oil, lavender oil
Liphophilic
Carbohydrates Gums, sugar esters Hydrophilic
Glycosides Glycyrrhizin, aloe vera
(anthraquinone glycosides)
Lipophilic
Tannins Hamamelitin Lipophilic
Lipids Castor oil Lipohilic
Polyphenols Epicatechins Hydrophilic
Vitamins Retinoids Hydrophilic
Alpha tocopherol
Ascorbic acid
Hydrophilic
Lipophilic
Hydrophilic

12. Formulation challenges for Antioxidants and
photoprotective
Herbal ingredients Challenge Approaches
Vitamin C and E Non polar
Prone to oxidation and
therefore unstable
Microemulsions
Polyphenols
curcumin,
silymarin, resveratrol,,
genistein, pomegranate
fruit
extract
High enough drug
concentration for system
Low poor solubility, poor
absorption, rapid
metabolism thus, low oral
bioavailability
Emulsion,SEDDS,
transferosome gels.
Lipid nanocapsules
ultrasound technology.
Phytosome
Solid lipid nanoparticles,
Liposphere
ginkgo Poor permeation phytosome
• Counteracts the harmful effects of reactive oxygen species and
other free radicals
• Reduces erythema, sunburn cells, and immunosuppression
caused by sunlight and DNA adduct formation

13. Formulation challenges for Antaging cosmetics
Herbal ingredients Challenges Approach
tetrahydrocurcuminoids Poor water and plasma
solubiliy
Liposomes, phytosomes,
nanoemulsion
Alpha Lipoic acid Chemically labile,
degraded easily and thus
unpleasant odour
Encapsulated into solid
lipid nanoparticles
Oleanolic extract Waxy, viscous Transferosomes,
microemulsion
Centella Poorly absorbed ( large
molecular size), Poor
lipid solubility, poor
membrane permeation,
reduced bioavailability.
Nanoemulsions,
Phytosomes,
Transferosome
• Stimulates normal skin growth and cellular growth and repair
• Repairs the loss in tone and elasticity of the skin
• Reverses the chemical changes that occur in collagen with aging
and normalizes the immune system

14. Formulation challenges for Moisturizer
Herbal ingredients Challenges Approaches
Retinoids Unstable, non polar, poor
permeation
Microemulsion,
Aloe vera Waxy, Poorly
absorbed ( large
molecular size),
Poor lipid solubility,
poor membrane
permeation,
reduced bioavailability.
Transferosome gel,
Nanoemulsions,
Phytosomes,
• Causes excretion of cytokinins, which induces edema,
vasodilation, and frank inflammation
• Makes stratum corneum softer
• Fills spaces between the layers and reduces fine lines

15. Formulation challenges for Anti irritant and Anti-
inflammatory
Herbal Ingredients Challenges Approaches
Corriander seed oil Highly volatile,
unstable.
Nanocapsulation
Solid Lipid Nanoparticles
Bisabolol Highly viscous Phytosomes,
transfersomes.
Inhibits the release of histamine and relieves irritation

16. Formulation challenges for Anti irritant and Anti-
inflammatory
Herbal Ingredients Challenges Approaches
Cucumber Volatile Emulsion, transfersome
• Cools, refreshes, and tightens the pores of skin
• Controls oily skin and lowers the pH of the face after cleansing

17. Marketed Products
Product name Effect Active ingredients
Liposome Whitening 2% Citrus extracts
Phytosome Antioxidant Silybin extracts
Liposphere Antioxidant Sunflower, vitamin E and
A, agar white
Nanoparticle Antiacne Vitamin E
Nanocapsule Sunscreens Vitamins
Pearlescent beads Moisturizing Mineral oil, aloe vera,
gelatin, red
Nanosomes Antiaging, Ginseng, alpha bisabolol
vitamin A and E

18. Other challenges faced :
Natural:
There are different types of natural; natural,
natural identical, semi natural, naturally derived.
Thus consumers want it, but no technical
understanding.

19. Technical Challenges (Raw materials)
•Shorter shelf life
• Different sensorial performance
• Natural is not always safe (for example Aloin in aloe vera)
• Quality, freshness, storage conditions are king (oxidation, batch
to batch variations, microbial content..)
• Essential oils adulterations with synthetics and even naturals!
• Price!
• Availability, especially for organic raw materials

20. Technical Challenges (Finished product)
• Oil based products: massage oils, face oils, balms (100%
organic claim)
• Shampoos and bath products: green surfactants available
but viscosity and performance can be tricky (many brands
use semi naturals)
• SPF: without nanotechnology it is impossible at the
moment.

21. Marketing challenge:
• Consumers find difficult to spot the “fake” natural from the
original one (ie purely based on natural key ingredients
rather than the whole product)
• Efficacy claims can be limited because of ingredients
restriction linked to certifications
• There can be a conflict between looking premium and
being truly green

22. Reference:
1. Novel approaches in herbal cosmetics, D Chanchal & S
Swarnlata 2008 Blackwell Publishing, Journal of Cosmetic
Dermatology
2. Naik SR, Pilgaonkar VW, Panda VS. Evaluation of
antioxidant activity of Ginkgo biloba phytosomes in rat
brain. Phytother Res 2006; 11: 1013–6.
3. Kuno N, Matsumoto M. Skin beautifying agent, antiaging
agent for the skin, whitening agent and external agent for
the skin, US Patent 6682763, 2004.
4.The challenges of developing Natural and Organic
Cosmetics by Dr Barbara Olioso, organatural.co.uk