Herbasome - A new generation of

Liposomes
Julian 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 lipid
bilayers of spherical (liposomes) or lamellar structures.

A
L

Liposomes being an elegant way to encapsulate:

- Hydrophilic (H), amphiphilic (A) and (in part) lipophilic (L) actives
- or just water
to increase their penetration.

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 November
2009 on cosmetic products, Annex V, list of preservatives allowed in cosmetic products.

Preservation of Liposomes

Self preserving solvent systems:

Water / Ethanol
Propanediol (PG) / Water
Glycerol / Water

Preservation of Liposomes

Natipide II = based on Water / Ethanol

INCI: Water (Aqua) / Lecithin / Ethanol
=> proliposomal system

Freeze fracture of Natipide II

Preservation of Liposomes

PhytoSolve = based on Glycerol / Water

INCI: Glycerin / Water (Aqua) / Lecithin / Lipophilic product(s)
=> an innovative technology to stabilize lipophilic actives or lipids

Phospholipids
Polyols
or
Carbohydrates

Lipids
or
Lipophilic Actives

Cryo fixation of PhytoSolve

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)

Glycerol-based Liposomes
Step 1:

A mixture of lecithins and high-grade glycerol, free of water

lead to liposome-like structures

LIPOID Liposome HGG

INCI: Glycerin, Lecithin, Tocopherol

LIPOID Liposome HGG

with multilamellar vesicular structures

Glycerol-based Liposomes
Step 2:

Pear water was added and high-pressure homogenization was

applied to create smaller particle sizes

Cryo fixation of Pear Water Herbasome

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

Glycerol-based Liposomes
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 no
microbial growth after six inoculations.

Glycerol-based Liposomes

First generation: Plant-water Herbasomes

Glycerol-based Liposomes

Lecithin in pure Glycerol forms Liposome-like structures

Addition of plant-derived water and high-pressure

homogenization lead to Herbasomes

Herbasomes are preservative-free and self-preserving

Glycerol-based Liposomes
30

28.6

Proven Skin Hydration:

25

In vivo study (corneometry)

Over 7 days, twice daily
24h after last application

Skin moisture [%]

20.9
20

15

10

4% Glycerol

=> 1.5x stronger skin hydration as Glycerol

5% Herbasome

Glycerol-based Liposomes

Incorporation of Herbasome in formulations:

-

Pear water Herbasome (20% each, respectively)

2 different cream formulations

analyzed by cryo fixation electronmicroscopy

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

Ingredient

INCI

Deionised Water

Aqua/Water

48.80

Sodium Hydroxide 10%

Aqua/Water, Sodium Hydroxide

1.30

Keltrol CG-SFT

Xanthan Gum

0.60

Sympatens GMS

Glyceryl Stearate

2.00

Crodafos CES

Cetearyl Alcohol, Dicetyl Phosphate, Ceteth-10

Phosphate

6.50

Akorex L

Canola Oil, Citric Acid

Grape Seed Oil

Vitis Vinifera (Grape) Seed Oil

5.00

Shea Butter Organic

Butyrospermum Parkii (Shea) Butter

5.00

Euxyl PE 9010

Phenoxyethanol, Ethylhexylglycerin

0.80

Pear Water Herbasome

Glycerin, Aqua/Water, Lecithin, Tocopherol

10.00

20.00

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

Crodafos blank formulation

Crodafos formulation with

20 % Herbasome

Glycerol-based Liposomes
Formulation 2: o/w cream based on SLM 2015

Ingredient

INCI

Water

Aqua/Water

28.50

Glycerol

Glycerin

5.00

Phospholipon 80H

Hydrogenated Lecithin

0.50

Keltrol CG-SFT

Xanthan Gum

0.20

SLM 2015

Aqua/Water, Caprylic/Capric Triglyceride,

Butylene Glycol, Hydrogenated
Phosphatidylcholine

20.00

Myritol 318

Caprylic/Capric Triglyceride

15.00

Grape Seed Oil

Vitis Vinifera (Grape) Seed Oil

10.00

Euxyl PE 9010

Phenoxyethanol, Ethylhexylglycerin

Pear Water Herbasome

Glycerin, Aqua/Water, Lecithin, Tocopherol

0.80
20.00

Glycerol-based Liposomes
Formulation 2: o/w cream based on SLM 2015

SLM 2015 blank formulation

SLM 2015 formulation with

20 % Herbasome

Glycerol-based Liposomes

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

Prospects: Actives in Glycerol-based liposomes

F
LIPOID Liposome HGG

Description

INCI

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

Identification

Prospects: Actives in Glycerol-based liposomes

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