Technical Data
Advantages of Lipodisq® Technology:
Lipodisq® offers clear benefits over competitive delivery technologies:
Exceptionally small particle size
Typically 10-40 nm depending on the chosen actives to be carried as measured by dynamic light scattering:
Unloaded Lipodisq® sample after one years ageing, peak 1: 12.96 nm, 77.3% intensity
(size distribution data provided by an independent test laboratory Malvern Instruments – Nanosizer)
High water solubility
Lipodisq® shows high water solubility, despite the fact that they contain highly water insoluble active agents within a hydrophobic core.
High particle load capacity
In contrast to other delivery systems such as liposomes (typically loading capacity ~ 5% dry weight) Lipodisq® can carry up to 30% active by dry weight and levels of 25% loading are commonly encountered with steroidal-like compounds, e.g. triterpines.
Stability to dilution and on storage in solution
Unlike micellar systems that break down upon dilution, Lipodisq® is structurally stable and maintains its integrity upon dilution while retaining their size upon aging in aqueous solution.
Approved and available raw materials
The materials used to manufacture Lipodisq® are approved for cosmetic (INCI) and/or pharmaceutical (EP/USP grade) use and are readily available from speciality chemical suppliers in both Europe and Japan and can be easily manufactured on a large scale using conventional plant and equipment.
Optical clarity
Due to the small size of the particles, i.e. in the range of 10-40 nm, aqueous solutions of the Lipodisq® remain water clear in the presence of water insoluble actives.
Easy to use, transport, store and resolubilise
Lipodisq® forms spontaneously under standard conditions available to most cosmetic and personal care product manufacturers. The resulting solutions can then be stored in liquid form. Lipodisq® solutions can be freeze dried/spray dried into a powder and readily resolubilised into water when required.
Biomimetic by design
The structure of Lipodisq® is based upon natural high density lipoproteins, which are responsible for transporting fats around the bloodstream and are present throughout the animal kingdom i.e. from insects to mammals. Lipodisq® is assembled from membrane forming phospholipids, biodegradable surfactant and co-surfactant chaperones.
Wide range of active agents
A wide range of cosmetic and pharmaceutical active agents can be carried by Lipodisq®
In Vivo Skin Penetration
Lipodisq® penetrates the skin to a depth of 15-20 layers through the stratum corneum todeliver the contents to the deeper living layers of the skin and underlying tissues, e.g. nerves, muscles etc., before degrading and being lost as the skin is shed.
A novel Near-infrared chemical imaging technique (NIR-CI, Malvern Instruments Ltd) has been used to track the progress of a Lipodisq®-bound marker dye through the skin.
Left: NIR-CI spectroscopic image of marker dye contained on tape strips removed from skin, 1st (top left) to 16th (bottom right) strip, showing accumulation of dye in 14th strip. Right: averaged NIR-CI signal of scanned pixel data from tape strips 1-16.
For more detailed experimental information see Malvern Instruments Application Note pdf below
Evaluating Skin Penetration using NIR-CI
See: Cosmetics and Toiletries, September 2010, vol 125, Number 9, Pages 52-57.
Environmentally Responsive Nanoparticles for Delivery as Assessed via Light Scattering and Near-infrared Imaging.
http://www.cosmeticsandtoiletries.com
Strong IP position
Malvern Cosmeceutics Ltd has developed an extensive portfolio of patents and patent applications protecting Lipodisq® technology. Generation one patents cover non-degradable Lipodisq® formulations; granted UK patent GB2426703 and related PCT application (WO2006129127) in principle territories of interest, including Europe, USA, Canada, Australia, China, India and Japan. Generation two biodegradable Lipodisq® is covered by PCT application (WO2008065451).