By Salvatore Salamone

December 15, 2003 | A recent deal between the small nanotech company C Sixty and pharmaceutical giant Merck signals what many believe will be a compelling new application of nanotechnology -- the direct use of “nanoparticles” as drugs.

Until now, life science-related nanotechnology efforts focused on areas such as building single-molecule pathogen-detection systems (see Detecting Deadly Agents in Small Places, Bio-IT World, June 2003, page 11 and improving discovery tools like microarrays and genechips. Other leading-edge work has focused on using nanotechnology to deliver drugs to a specific target such as a cell or tumor.

The Merck/C Sixty deal proposes something quite different -- using nanotech particles called buckminsterfullerenes (fullerenes, for short) to directly fight diseases. Merck declines to discuss specifics, but in a prepared statement, Dennis Choi, executive vice president, neurosciences, at Merck Research Laboratories, said, “This agreement is expected to help accelerate our efforts in the area of antioxidant therapeutics.”

 Fullerenes, often called buckyballs, are soccer ball-shaped structures composed of 60 carbon atoms. “We’ve found that the fullerene core has some pretty amazing electro-chemical properties,” says Russ Lebovitz, vice president of R&D and business development at C Sixty. “Fullerenes make good anti-oxidants and they can [quench] free radicals in biological systems.”

From a therapeutics standpoint, this property has potential treatment applications in diseases such as ALS and Parkinson’s in which free radicals form around a cell and eventually kill it. If a fullerene could be delivered to a site containing free radicals, there’s a chance the buckyball could neutralize the particles and prevent or mitigate cell damage.

The trick is getting the buckyball to the affected site. That’s where another interesting property of fullerenes comes into play. Some industry experts refer to fullerenes as “pin cushions” because they can be used to “hold” other molecules in very specific 3-D orientations. Result: “You can modify the surface [of a fullerene] to make it soluble to get it into blood or a cell,” Lebovitz says.

Clearly, nanotechnology’s star is rising in the life sciences. Earlier this year, National Cancer Institute director Andrew C. von Eschenbach announced a “challenge goal” to eliminate the suffering and deaths from cancer by 2015. In discussing the goal, Mihail Rocco, senior advisor for nanotechnology at the National Science Foundation, said in an October UPI news report, “Basically, without nanotechnology, it would be impossible to address this issue.”

Rocco noted that nanotech tools and techniques will allow doctors to “detect cancer much earlier and to treat it immediately” before the disease has time to produce tumors.

Although the anti-oxidant capability of fullerenes has long been known, most drug-related buckyball research has been limited to academic labs. This is primarily because of scarce fullerene supplies and their resulting high costs.

The quantity of fullerenes needed for manufacturing a successful drug “would have exhausted the complete supply of fullerenes a few years ago,” Lebovitz says. That’s changing as companies like C Sixty partner with third parties that specialize in the manufacturing of fullerenes.

C Sixty, for instance, buys from Nano-C, which uses technology licensed from MIT that enables production of commercial quantities of fullerenes. Nano-C says its approach cuts the market price of fullerenes from about $25 per gram in 2001 to $10 per gram now. This price drop should have a major impact on the use of fullerenes in biotech.

Says Gordon Fowler, CEO of Nano-C: “While researchers have noted the anti-oxidant and radical scavenging ability of fullerenes for many years, one of the problems with their adoption has been the cost.”