Drug Delivery R&D Addresses Manufacturability at the Particle Level

12/02/2004

MFIC Corp. and Dow Chemical are both working with academia on separate initiatives to improve solubility and drug delivery through the manipulation of particle size. What follows are excerpts of recent statements by both companies.

MFIC and UMass Lowell

Microfluidics, the operating subsidiary of MFIC Corp., announced today that University of Massachusetts-Lowell scientists are using Microfluidizer materials processing equipment to develop water soluble plant sterols for use as cholesterol-blocking food additives. If the research proves successful, food and pharmaceutical companies may be able to use Microfluidizer processors to develop foods, beverages, and dietary supplements that inhibit the absorption of cholesterol in the intestines, significantly reducing blood cholesterol levels and the risk of heart disease, the nation's leading cause of death.

The research is being conducted at UMass Lowell's Center for Health and Disease Research by Professor Robert Nicolosi, director of the center. Nicolosi is using the Microfluidizer processor to develop a variety of other products, including foods and beverages fortified with cancer-fighting antioxidants and orange juice fortified with vitamin E that will not precipitate from the juice.

"Many nutrients are lipid- or 'fat'-soluble," said Nicolosi. "We are using the high-pressure Microfluidizer processor to take lipid soluble nutrients and make them water soluble in a nano-emulsion."

If Nicolosi is successful, his work could lead to a new generation of more effective nutritional foods and supplements. Foods that are nutritionally enhanced with vitamins, herbs and nutritional supplements are known as nutraceuticals, a $46 billion market in 2002 that will grow to more than $74 billion by 2007, according to Business Communications Company, an industry and market research firm in Norwalk, Conn.

Plant sterols and animal sterols share a similar chemical structure and mutually limit each other's solubility and uptake in the small intestine. But where animal sterols or cholesterol remains in the body for a long time once it is absorbed, plant sterols are poorly absorbed and are quickly excreted from the body. Long-term clinical trials established 50 years ago that plant sterols lower blood cholesterol by inhibiting the absorption of cholesterol from the small intestine and that they have no adverse effect even in large doses. The problem is that Americans do not eat nearly enough plant sterols to have a beneficial impact on blood cholesterol. Nicolosi hopes to change that.

"If we can develop the product, the impact on human health could be significant," said Nicolosi. "By ingesting one or two grams of plant sterol each day, you could lower your blood cholesterol by 15 percent. Studies show that for each one percent lowering of blood cholesterol you lower your risk of heart disease by two percent." That means that a 15 percent lowering of blood cholesterol can be associated with a 30 percent reduction in the risk of heart disease.

Dow and UT Austin

The Dow Chemical Company and The University of Texas at Austin (UT-Austin) have renewed their ongoing research collaboration to develop and commercialize drug solubilization technology for critical pharmaceutical applications. The expanded research agreement supports continued growth for BioAqueousSM solubilization services, an offering of the Dowpharma business unit of The Dow Chemical Company, which apply particle engineering technologies to improve the bioavailability of poorly soluble drug compounds.

Increasing the bioavailability of poorly soluble drug compounds is one of the greatest challenges the pharmaceutical industry faces for more effective delivery of small molecule drug compounds. "Dowpharma's collaboration with the University of Texas at Austin is oriented towards rapidly bringing novel drug delivery solutions to our pharmaceutical clients," said Nick Hyde, business director, Dowpharma.

He added, "Our strengths in applied research and development, scale-up and commercialization, combined with UT-Austin's core research capabilities has resulted in the development of unique solutions to one of the largest roadblocks in small molecule drug development today. This expanded agreement exemplifies our commitment to the evolution of innovative technology to meet the pharmaceutical market's needs."

The Dow/UT-Austin collaboration begins its fifth year by advancing targeted therapeutic application development and continues to draw on previous research on initial technology discovery and proof-of-concept achievements.

"Our collaborative research has demonstrated the applicability of our particle engineering technologies to improve the performance and bioavailability of poorly soluble drug compounds, whether they are newly discovered or already in existence," said Edmund J. Elder, Ph.D., pharmaceutics director, Dowpharma. He added, "So far, we've been able to demonstrate the applicability of our technologies to compounds in a variety of therapeutic areas, including cardiovascular, metabolic, and antifungal drug compounds."

BioAqueous solubilization services developed by Dow show the ability to alter particle size, surface area, or morphology to create nanostructured particles that can improve a drug's ability to dissolve in the body. Based on the specific challenges of a particular drug compound, an initial feasibility study employs Dow's portfolio of advanced particle engineering technologies to develop customized solutions to meet the desired performance objectives of the compound. Beyond a feasibility study, BioAqueous solubilization services include support through all stages of development, optimization, and production of clinical and commercial supplies.