- A new generation of liposome.pdf

Herbasome® - A new generation of

LiposomesJulian Smits and Dr. Bernd Albrecht

Introduction

Lecithin = natural mixture of various phospholipids (plus other…)- mainly being Phosphatidylcholine- main source is soybean (rapeseed, sunflower, eggyolk…)

Use as emulsifier

Provide lamellar structures (e.g. SLM)

Introduction

Lecithin (especially Phosphatidylcholine) spontaneously forms lipidbilayers of spherical (liposomes) or lamellar structures.

Liposomes being an elegant way to encapsulate:- Hydrophilic (H), amphiphilic (A) and (in part) lipophilic (L) actives- or just water to increase their penetration.

H A

L

Introduction

“Liposomes are closed vesicles of polar lipid bilayers or

lamellae with enclosed aqueous layers and cores, which are

able to encapsulate hydrophobic, ambiphilic and hydrophilic

substances into their structure.”

F. Gunstone, Phospholipid Technology and Applications, 2008, The Oily Press Lipid Library Volume 22

Introduction

Liposomes exist per definition only in water….

Due to their high water content liposomal systems need to be preserved.

Preservation of Liposomes

Conventional preservatives:

• Benzoic acid and its sodium salt

• Other salts of benzoic acid

• Phenoxyethanol

• Parabens

• Sorbates

• Sulfits

• etc.

Listed in the Regulation (EU) No 1223/2009 of the European Parliament and of the Council of 30 November2009 on cosmetic products, Annex V, list of preservatives allowed in cosmetic products”.


Self preserving solvent systems:

• Water / Ethanol

• Propanediol (PG) / Water

• Glycerol / Water


Natipide II® = based on Water / Ethanol

INCI: Water (Aqua) / Lecithin / Ethanol

=> proliposomal system

Freeze fracture of Natipide II®


PhytoSolve® = based on Glycerol / Water

INCI: Glycerin / Water (Aqua) / Lecithin / Lipophilic product(s)

=> an innovative technology to stabilize lipophilic actives or lipids

Phospholipids

Polyolsor

Carbohydrates Lipids or

Lipophilic Actives

PhytoSolve®Cryo fixation of PhytoSolve®

Glycerol-based Liposomes

Glycerol is the second most used raw material in

the cosmetic industry:

• shows excellent solubility in polar solvents

• has numerous skin care benefits, e.g.:• moisturizing activity• improves skin feel and softness• is part of the natural moisturizing factor (NMF)

• is very safe to use (GRAS status)


Step 1: A mixture of lecithins and high-grade glycerol, free of water lead to liposome-like structures

LIPOID Liposome HGGINCI: Glycerin, Lecithin, Tocopherol

LIPOID Liposome HGGwith multilamellar vesicular structures

Step 2: Pear water was added and high-pressure homogenization wasapplied to create smaller particle sizes


Cryo fixation of Pear Water Herbasome®

INCI: Glycerin, Pyrus Communis (Pear) Water, Lecithin, Tocopherol

Repetitive Microbial Challenge Test

Periodic inoculation of test items(once a week over six weeks).

=> Glycerol-based liposomes passed the challenge test since there was nomicrobial growth after six inoculations.



First generation: Plant-water Herbasomes®


- Lecithin in pure Glycerol forms «Liposome-like structures»

- Addition of plant-derived water and high-pressurehomogenization lead to Herbasomes®

- Herbasomes® are preservative-free and self-preserving

Proven Skin Hydration:

- In vivo study (corneometry)- Over 7 days, twice daily- 24h after last application

=> 1.5x stronger skin hydration as Glycerol


20.9

28.6

0

5

10

15

20

25

30

4% Glycerol 5% Herbasome®

Skin

moi

stur

e [%

]


Incorporation of Herbasome® in formulations:

- Pear water Herbasome® (20% each, respectively)

- 2 different cream formulations

- analyzed by cryo fixation electronmicroscopy

Formulation 1: o/w cream containing phosphate based emulsifier Crodafos

Ingredient INCI %A Deionised Water Aqua/Water 48.80

Sodium Hydroxide 10% Aqua/Water, Sodium Hydroxide 1.30Keltrol CG-SFT Xanthan Gum 0.60

B Sympatens GMS Glyceryl Stearate 2.00

Crodafos CESCetearyl Alcohol, Dicetyl Phosphate, Ceteth-10 Phosphate 6.50

Akorex L Canola Oil, Citric Acid 10.00Grape Seed Oil Vitis Vinifera (Grape) Seed Oil 5.00Shea Butter Organic Butyrospermum Parkii (Shea) Butter 5.00Euxyl PE 9010 Phenoxyethanol, Ethylhexylglycerin 0.80

C Pear Water Herbasome® Glycerin, Aqua/Water, Lecithin, Tocopherol 20.00


Formulation 1: o/w cream containing phosphate based emulsifier Crodafos

Crodafos blank formulation Crodafos formulation with 20 % Herbasome®


Formulation 2: o/w cream based on SLM 2015

Ingredient INCI %A Water Aqua/Water 28.50

Glycerol Glycerin 5.00Phospholipon 80H Hydrogenated Lecithin 0.50Keltrol CG-SFT Xanthan Gum 0.20

B SLM 2015 Aqua/Water, Caprylic/Capric Triglyceride,

Butylene Glycol, Hydrogenated

Phosphatidylcholine

20.00

C Myritol 318 Caprylic/Capric Triglyceride 15.00Grape Seed Oil Vitis Vinifera (Grape) Seed Oil 10.00Euxyl PE 9010 Phenoxyethanol, Ethylhexylglycerin 0.80

D Pear Water Herbasome® Glycerin, Aqua/Water, Lecithin, Tocopherol 20.00


Formulation 2: o/w cream based on SLM 2015

SLM 2015 blank formulation SLM 2015 formulation with 20 % Herbasome®



Summary

• Lecithin forms liposome-like structures in a glycerol matrix

=> Glycerol can overtake the role of water in liposomal systems

• Glycerol-based liposomal preparations (e.g. Herbasome®) do not need further

preservation (preservative-free systems)

• Herbasome® show a skin hydration effect that is 1.5x stronger than Glycerol

• Herbasome® can be incorporated in creams and lotions

Prospects: Actives in Glycerol-based liposomes

- Citrolumine 8® (launched in 2010) based on Glycerol / Water

- “Brightens Skin Tone, Fades Age Spots, Increase Skin Radiance”

INCI: Glycerin, Water, Lecithin, Citrus Paradisi (Grapefruit) Fruit Extract, Citrus Aurantium Amara (Bitter Orange) Fruit Extract, Sodium Ascorbate, Tocopherol, Helianthus Annuus (Sunflower) Seed Oil)

=> Remarkable stability


FIdentification Description INCI

LIPOID Liposome HGG Lecithin in high-grade glycerol Glycerin, Lecithin, Tocopherol

LIPOID Liposome 0090 Lecithin in a glycerol/water matrix Glycerin, Water (Aqua), Lecithin, Tocopherol

Pear Water Herbasome® Lecithin in a glycerol/water matrix plus pear water condensate

Glycerin, Pyrus Communis (Pear) Water, Lecithin, Tocopherol

LIPOID Liposome 0616 Lecithin in a glycerol/water matrix plus collagen hydrolysate

Glycerin, Water (Aqua), Lecithin, Hydrolyzed Collagen, Tocopherol

LIPOID Liposome 0809 Lecithin in a glycerol/water matrix plus dihydroxyacetone

Glycerin, Water (Aqua), Phosphatidylcholine, Dihydroxyacetone, Tocopherol


• Glycerol-based liposomal preparations can be considered as a new

generation of preservative-free liposomes

e.g:

• for plant-derived waters (no «Aqua» in INCI)

• for all kinds of actives (limitation: solubility in glycerol)

• for water-sensitive (but not glycerol-sensitive) actives

Documents

- A new generation of liposome.pdf