Drug Nanocrystals

    Lipid Nanoparticles




    Intellectual Property

PharmaSol's Nanopearls

Application areas:
Nanopearls are the cosmetic application of the pharmaceutical lipid nanoparticles, NLC. The particles can be incorporated into creams, lotions, gels, sticks etc. Features of dermally applied lipid nanoparticles are:

1. adhesion to skin
2. occlusion effect and consequently increased hydration
3. wrinkle smoothing of evenly applied placebo particles
4. drug release modification, modulation of penetration
5. protection of chemically labile compounds, e.g. retinol

Further examples of Nanopearls' application:
- increased efficiency of molecular UV-blockers and reduced side effects
- prolonged release of perfumes
- prolonged release of insect repellents

Technology description:

The lipid nanoparticles for cosmetic application are produced in an identical way to the pharmaceutical NLC. The cosmetic ingredients are dissolved in the lipid melt.
Topical formulations can be produced simply by producing a lipid particle dispersion with a higher solid content (e.g. 35-45%), which possesses a cream-like consistency. Alternatively, the lipid particle dispersions can be converted into gels by the addition of viscosity enhancers. Incorporation into creams or lotions is possible by replacing part of the water with a highly concentrated lipid particle suspension during the production process or blending it after production by admixing the lipid particle suspension. Adding the lipid nanoparticles to existing formulations has the smart feature that the existing advantages of established products can be combined with the new features of the lipid nanoparticle carrier.

Advantages over competing technologies:

Since the introduction of the liposomes by Dior in 1986, no carrier system that has since been placed on the market has received similar attention from customers. There are known physical stability problems with Liposomes, especially in o/w emulsions. These are avoided with lipid nanoparticles. In addition, due to their fluid character, the liposomes are not able to efficiently stabilise chemically labile compounds. Stabilisation against degradation is achieved by the lipid nanoparticles due to the solid character of the particle matrix.
Solid lipid nanoparticles (SLN) can also be used as a cosmetic carrier for dermal application. As outlined in the technology description for pharmaceutical NLC, these second generation particles have improved properties with regard to loading capacity of active ingredients, firm inclusion into the particle matrix and greater flexibility in modulating drug release.

Large scale production/costs:

Large scale production is easily achieved by high pressure homogenisation, and large capacity homogenisers with a homogenisation volume of 1 t/h can be used (e.g. Rannie 118). The highly concentrated lipid particle suspensions can be admixed to creams or lotions using traditional blending equipment available in the cosmetic industry.
The costs for excipients are relatively low because all standard cosmetic excipients, ranging from surfactants, stabilisers to solid lipids (m.p. > 40°C) and oils, can be used for admixing to the lipid blend.

IP position:

For an overview of patents and patent applications please click "Intellectual property".

Further Information regarding this topic can be obtained by reading:

Wissing, S. A., Müller, R. H., A novel sunscreen system based on tocopherol acetate incorporated into solid lipid nanoparticles (SLN), International Journal of Cosmetic Sciences 23, 233-243, 2001

Wissing, S. A., Mäder, K., Müller, R. H., Solid lipid nanoparticles (SLNTM) - a novel carrier for UV blockers, Die Pharmazie 10, 783-786, 2001

Wissing, S. A., Lippacher, A., Müller, R. H., Investigations on the occlusive properties of solid lipid nanoparticles (SLNTM), International Journal of Cosmetic Sciences 52, 313-324, 2001

Wissing, S., Müller, R. H., Solid lipid nanoparticles as carrier for sunscreens: in vitro release and in vivo skin penetration, Journal of Controlled Release 81, 225-233, 2002

Wissing, S. A., Müller, R. H., The influence of the crystallinity of lipid nanoparticles on their occlusive properties, Int. J. Pharm. 242, 377-379, 2002

Wissing, S. A., Müller, R. H., The development of an improved carrier system for sunscreen formulations based on crystalline lipid nanoparticles, Int. J. Pharm. 242, 373-375, 2002

Wissing, S. A., Müller, R. H., The influence of solid lipid nanoparticles (SLN) on skin hydration and viscoelasticity - in vivo study, Eur. J. Pharm. Biopharm. 56, 67-72, 2003

Wissing, S. A., Saupe, A., Müller, R. H., Nanostructured lipid carriers (NLC) for topical use - an overview, Eurocosmetics 5, 14-17, 2003

Wissing, S. A., Müller, R. H., In vitro and in vivo skin permeation of sunscreens from solid lipid nanoparticles (SLNTM), supercooled melts and emulsions, 4th World Meeting ADRITELF/APV/APGI, Florence, 1135-1136, 2002

Saupe, A., Wissing, S. A., Müller, R. H., Increasing the protection effect of titanium dioxide by incorporation in solid lipid nanoparticles (SLN), AAPS Annual Meeting, Salt Lake City, W5185, 2003

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