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What do we understand by nanodispersions?

 

Nanodispersions, in other words, liquids with particles in nano size meaning < 1 µm = < 1000 nm, are widely used in skin care preparations and in dermatological cosmetic applications.1,2,3,4,5,6 Optimal haptic properties can be achieved with nanodisperse lipids and oils. Thus the inconvenient oily and fattening components can be converted into aqueous lotions that rapidly penetrate into the skin. Water-soluble active agents and particularly such with high polarity are encapsulated into liposomes which also belong to the category of nanodispersions.

Regardless of their biodegradability and their structure, either lipophilic (oils, fats, waxes, organic active agents), hydrophilic (liposomes with aqueous interior) or inorganic, nanodispersions imply a high availability of active agents and accordingly allow using low concentrations of active agents in the formulations. Just to mention some examples: Liquid nanoparticles loaded with retinyl palmitate (vitamin A) sooner than conventional emulsions reach the irritation threshold that is critical for the formation of vitamin A acid. Liposomes with very low concentrations (≤ 1%) of sodium ascorbyl phosphate (vitamin C) inhibit the melanin formation.

In comparison to conventional formulations, nanodispersions with particles smaller than 1 µm allow a reduction or even elimination of cosmetic additives such as emulsifiers, spreading agents and penetration enhancers. Cosmetic additives often stress the skin and can even be counterproductive when facilitating washout effects or irritations. Moreover, the combination of nanodispersions with conventional formulations often fails due to the incompatibility with emulsifiers.7
Since the preservatives listed in the annex of the EU Cosmetic Directive imply the risk of sensitisations when permeating, nanodispersions are produced under sterile conditions and filled in ampoules, or alternatively produced without any preservatives whatsoever. The advantage, of course, is that physiological concepts are realized to a large extent.

An important criterion with topically applied nanoparticles is their biodegradability in the human body. The following nanoparticles are easily biodegraded:

  • Nanocrystals of difficultly soluble or high-melting organic substances such as boswellic acids (frankincense), phytosterines, flavonoids and their glycosides as for instance rutin, as well as ceramides.  
  • Liquid nanoparticles based on phosphatidylcholine – in this case not the particles are penetrating into the skin but the molecular individual components. They can contain fat-soluble active agents such as vitamins, coenzyme Q10, ceramides, herbal oils and essential fatty acids.
  • Liposomes with water-soluble vitamins, antioxidants, glycosides, moisturizers etc.

There are other nanoparticles with carrier substances and sometimes also active agents that are non-biodegradable, as for instance:

  • Lipid nanoparticles made of waxes, poly-alpha-olefins and other hydrocarbons. On the skin they combine into occlusive films from which lipophilic active agents such as coenzyme Q10 are released.
  • Polymer beads made of polyamides, polypeptides or polysaccharides with embedded, mostly pharmaceutical active agents.
  • Silica nanoparticles (silicic acid) that integrate and stabilize amorphous active agents and pigments in their pores.
  • Inorganic substances such as titanium dioxide, zinc oxide and carbon (carbon black) for sun screen purposes and decorative cosmetic products.
  • Elementary precious metals such as silver and gold. Gold forms red dispersions; silver has antibacterial and anti-inflammatory effects.

Aqueous nanodispersions with small particles look like aqueous solutions while particles larger than 400 nm show an opaque or even milky consistency. They can also be coloured, as for instance gold dispersions.  

In the field of dermatological cosmetics they are used for the supportive prevention and the adjuvant skin care in the case of skin irritations.8 For this purpose individual substances but also substance compounds and herbal extracts are used. The focus is on biodegradable nanodispersions that are compatible with the human physiology.

Nanoparticles with a size of 100 nm or smaller have to be labeled as nanomaterial according to the Regulation EC1223/2009 of the EU Cosmetic Directive, in force since 11.07.2013. They are subject to strict requirements. Exempt of the directive are nanoparticles with a particle size > 100 nm as well as liquid, biodegradable nanoparticles that already decompose into their individual components in the skin barrier.

Table: Examples of frequently used nanoparticles and active agents
Liposomes (L); liquid (N), solid (SN) nanoparticles; biodegradable (+), non-degradable (-)


 Active agent

 Carrier

 Application

 Mechanism of action

 aescin

 L+

 rosacea, couperosis

 vascular permeability ↓, oedema ↓

 amino acids

 L+

 dry skin

 moisturizer, radical scavenger

 eyebright

 L+

 eye care

 unknown

 azelaic acid

 L+

 acne, rosacea, perioral dermatitis (POD)

 5-α-reduktase inhibition

 boswellic acids

 L+, N+, SN+

 acne, POD, rosacea, neurodermatitis, erythema

 protease inhibition, 5-lipoxygenase inhibition

 carbon black

 SN-

 makeup

 pigment

 ceramidec

 SN+

 skin protection

 TEWL ↓

 coenzyme Q10

 N+, SN-

 anti-aging

 metabolism ↑

 caffeine

 L+

 microcirculation, cellulite

 peripheral vasodilatation, lipolysis

 various herbal extracts

 L+

 hyperpigmentation, laser

 tyrosinase inhibition

 fumaric acid

 L+

 psoriasis

 collagen metabolism ↑?

 hesperidin

 SN+

 anti-aging

 vascular permeability ↓, oedema ↓, antioxidant

 isoflavones

 L+

 estrogen effects

 phytohormones

 kigelia extract

 L+

 rosacea, couperosis

 vascular permeability ↓, oedema ↓

 butcher’s broom extract

 L+, N+

 rosacea, couperosis

 vascular permeability ↓, oedema ↓

 sodium ascorbyl phosphate

 L+

 hyperpigmentation, laser

 vitamin C, tyrosinase inhibition

 niacinamide

 L+

 acne, blemished skin, regeneration

 vitamin B3

 oils with bound linoleic acid

 N+

 barrier disorders,
erythema

 ceramide substrate, metabolisation through 15-Lipoxygenase (LOX)

 oils with bound α-linolenic acid

 N+

 erythema

 metabolism through 15-LOX

 oils with bound γ-linolenic acid

 N+

 neurodermatitis, erythema

 δ-desaturase defect, metabolism through 15-LOX

 phosphatidylcholine (with bound linoleic and α-linolenic acid)

 L+, N+

 acne, barrier-, cornification disorders

 ceramide substrate, metabolism through 15-LOX

 retinyl palmitate

 N+

 acne, scars, regeneration

 vitamin A

 rutin

 SN+

 rosacea, couperosis

 vascular permeability ↓, oedema ↓

 silver

 SN-

 inflammations

 antibacterial

 silica

 SN-

 makeup

 pigment

 spilanthol

 L+

 wrinkle reduction

 metabolisation through

 titanium dioxide

 SN-

 light protection, makeup

 UV filter, pigment

 tocopheryl acetate

 N+

 skin protection

 vitamin E

 tranexamic acid

 L+

 hyperpigmentation, rosacea

 tyrosinase inhibition, vascular permeability ↓

 grape seed extract

 L+

 anti-aging

 radical scavenger (OPC)

 zinc oxide

 SN+

 light protection

 UV filter

 zink salts

 L+

 acne, blemished skin

 superoxide dismutase (SOD)-substrate

References

  1. H. Lautenschläger, Nanopartikel von fest bis flüssig, medical Beauty Forum 2016 (2), 12-16
  2. H. Lautenschläger, Cosmeceuticals, medical Beauty Forum 2014 (4), 16-18
  3. H. Lautenschläger, Indikationsgemäße Anwendungen von Nanodispersionen, Vortrag auf der 19. Jahrestagung der Gesellschaft für Dermopharmazie (GD) in Berlin am 18.3.2015
  4. H. Lautenschläger, Geschichte und aktuelle Gesichtspunkte der Korneotherapie, Kosmetische Medizin 26 (2), 58-60 (2005)
  5. H. Lautenschläger, Mikrokosmos modularer dermaler Zusammensetzungen, Vortrag auf der 18. Jahrestagung der Gesellschaft für Dermopharmazie (GD) in Berlin am 9.4.2014
  6. J. Cornier, C.M. Keck, M. van de Voorde, Nanocosmetics – From Ideas to Products. Springer. (2019).
  7. H. Lautenschläger, Huckepack – Übersicht Trägersysteme, medical Beauty Forum 2013 (1), 16-18
  8. H. Lautenschläger, Nutzen von lamellaren Präparaten in der Hautpflege, im Hautschutz und in der dermatologischen Therapie, Vortrag auf der 17. Jahrestagung der Gesellschaft für Dermopharmazie (GD) in Mainz am 23.3.2013

Hans Lautenschläger & Cornelia Keck

Please note: The contribution is based on the state of the art at the revision date.

 
 
 
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