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Early testing shows promise for drug solubilization in fight against fungal infections of heart

University Of Texas At Austin : 08 November, 2004  (Technical Article)
Early testing indicates a new technology developed by a research team at The University of Texas at Austin holds strong promise in the fight against pulmonary fungal infections, a serious threat to lung transplant patients, patients undergoing chemotherapy treatment and HIV/AIDS patients.
Dr. Robert O. Williams III, professor of pharmaceutics, said fungal infections represent 9 percent of all hospital acquired infections and results in an annual cost of $2.6 billion or about $72,000 per patient.

“Transplant patients are particularly susceptible to infections since their immune system is suppressed to prevent the body from rejecting the transplant,” he said. “Lung transplant patients find themselves especially vulnerable since it is difficult to get traditional fungal fighting medications to the lungs before the body eliminates them.”

The promising findings will be discussed this week in Baltimore at the national meeting of the American Association of Pharmaceutical Scientists.

Williams and Dr. Keith Johnston, professor of chemical engineering at the university, have developed the technologies that produce nanoparticles of a variety of pharmaceuticals. Because of their tiny size and increased surface area, the treated particles are broken down in the body quickly and the rate of absorption is increased.

The two researchers and their teams and The Dow Chemical Company recently announced the renewal of their ongoing collaboration to develop and commercialize drug solubilization technology. The technology is expected to enable the production of stronger, faster-acting pharmaceuticals and expanding treatment choices for doctors and patients.

For the fungal drug research, Williams and Johnston have worked in collaboration with two professors and a lung transplant physician in San Antonio. Drs. Robert Talbert and Davis Burgess are on the university pharmacotherapy faculty at the University Health Science Center in San Antonio. Dr. Jay Peters is a pulmonary surgeon at the UT Health Science Center in San Antonio. In addition, they have worked closely with Dr. Jason McDonville, a research fellow at the university.

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.

Johnston’s and Williams’ twin drug delivery powerhouses, called pray Freezing Into Liquid and Evaporative Precipitation into Aqueous Solution, are separate processes for producing extremely fine, readily absorbed (bioavailable) particles. The conventional mechanical approach for particle size reduction of drugs is based on the same principles as a grinder for peppercorns.

In the new processes, Johnston said that “the particles are engineered with smart stabilizers by precipitation from solution.” In the stomach or small intestine, the high surface area particles are wetted instantly and dissolve in less than a minute rather than tens of minutes, in some cases. The drugs are then absorbed into the bloodstream instead of being expelled through the colon.

The Dow Chemical Company has licensed the technologies, which Williams calls very broad. “You can apply it to oral, injectable, topical or pulmonary therapies: any mode of drug delivery,” he said.

The pharmaceutical industry is targeting ailments as diverse as microbial infections, arthritis, diabetes, asthma, even schizophrenia. Every year, pharmaceutical companies give up on promising but poorly soluble pharmaceuticals because they have low bioavailability in the bloodstream, and existing solubilization technologies can’t solve the problem. The new alternatives for solubilization developed at the university can help pharmaceutical companies bring more new drugs to market, giving doctors and patients more treatment options. Some drugs that were once thought to be impractical due to poor dissolution may now be reconsidered.

The two technologies, which were licensed through The University of Texas at Austin’s Office of Technology Commercialization, have become part of BioAqueous solubilization services, an offering of the Dowpharma business unit of The Dow Chemical Company which apply particle engineering technologies to enhance drug solubilization and improve bioavailability of poorly soluble drugs.
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