When the size of the material is reduced to less than 100 nanometers, the realm
of quantum physics takes over and materials begin to demonstrate entirely new
properties. Hence nano-design of drugs by various techniques like milling, high
pressure homogenization, controlled precipitation etc., are explored to produce,
drug nanocrystals, nanoparticles, nanoprecipitates, nanosuspensions (which for
ease of understanding commonly mentioned as nanocrystals). As decreased
size will increase the solubility of drugs hence, this technology is explored to
increase oral bioavailability of sparingly water soluble drugs.
On the other hand engineering of nanocrystals will avoid the use of toxic
solvents and surfactants to develop injectable solutions of sparingly water
soluble drugs. It is also possible to develop formulations for various routes of
administration where size is the critical factor (injectables, ophthalmics and
topical preparation).
NanoCrystal Technology from Elan (See illustration bellow), is one of the
earliest scalable technology for nanosizing the drugs, Rapamune was the first
product based on this technology approved in USA. Rapamune was previously
available only as an oral solution in bottles or sachets. The oral solution requires
refrigeration storage, and must be mixed with water or orange juice prior to
administration. The new tablet developed with NanoCrystal technology provides
patients with more convenient administration and storage than Rapamune oral
solution. In 2000, Elan Pharmaceuticals received FDA approval for its
NanoCrystal technology, by reformulating Rapamune®, a Wyeth drug
(sirolimus). The new formulation overcame the drug’s relative insolubility by
reducing the particle size to less than 200nm, and subsequently coating the
active compound with GRAS (Generally Regarded As Safe) surface stabilizers.
Many nanotechnologies are developed and are under investigation for their
application. As this area of research is in its early stage of growth one can hope
for many more surprises and new applications. We tried to enlist some of the
products which have seen the day of light and also those which soon hit the
market bellow.
Dowpharma
Elan
PharmaSol
SkyePharma
Spherics
| Product |
Drug |
Technology by/licenced to |
| Rapamune |
Sirolimus |
Elan/Wyeth |
| Emend |
Aprepitatnt |
Elan/Merck |
| Tricor |
Fenofibrate |
Elan/Abbot |
| Triglide |
Fenofibrate |
SkyePharma/First Horizon Pharmaceuticals |
Oral bioavailability of cyclosporine: Solid lipid nanoparticles (SLN((R)))
versus drug nanocrystals.NEW
International Journal of Pharmaceutics, 2006, In Press.
Critical freezing rate in freeze drying nanocrystal dispersions
Journal of Controlled Release, 2006, 111, 185-192
Nanoparticle engineering processes for enhancing the dissolution rates of
poorly water soluble drugs
Drug Development and Industrial Pharmacy, 2004, 30, 233-245
The role of solid nanoparticle technology in the parenteral delivery of poorly
water-soluble drugs
International Journal of Pharmaceutics, 2004,284, 109-122.
Application of supercritical carbon dioxide in energetic materials processes:
Macromolecular Biosciences, 2005, 5, 1118-1124.
Patent Watch
System and method for milling materials
Reed , et al. USPT, 6,976,647 December 20, 2005
Water-insoluble drug particle process
Pace, et al. USPT, 6,682,761, January 27, 2004.
Process for preparing micronized polypeptide drugs
Platz , et al. USPT 5,354,562, October 11, 1994
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