Dow extends UT Austin pact on solubilisation

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. It is estimated that around 40 per cent of all medicines on the market suffer from poor water solubility, and this proportion is rising to reflect the higher proportion of larger, more complex biological molecules in the drug industry's pipeline.

Even now, many orally-administered drugs display poor bioavailability when administered in conventional dosage forms, i.e., the rate and extent to which the drugs are absorbed is less than desirable. With several drugs, absorption may be as little as 30 per cent or less of the orally administered dose.

The expanded research agreement with UT Austin is intended to keep Dow's recently-launched BioAqueous solubilisation service business at the cutting edge. This was set up a year ago to apply particle engineering technologies to improve the bioavailability of poorly soluble drug compounds.

The BioAqueous solubilisation services focus on altering the particle size, surface area, or morphology of drugs to create nanostructured particles that can improve their ability to dissolve in the body. The business relies heavily on two nanoparticle engineering echnologies licensed from UT Austin, namely SFL (Spray Freezing Into Liquid) and EPAS (Evaporative Precipitation Into Aqueous Solution).

These processes produce extremely fine, readily absorbed particles - with a high surface area and good 'wetability', and can be applied to any mode of drug delivery: oral, injectable, topical or pulmonary, according to Bill Williams, professor of pharmacy at UT Austen.

In SFL, a drug's active ingredient is dissolved in an organic solvent, atomised and sprayed directly into a liquid that has been cooled to temperatures below -40 degrees Centigrade. The liquefied gas and frozen solvent are removed, leaving behind a powder of nano-sized active particles.

In EPAS a heated organic solution of the active agent is rapidly evaporated and atomised into an aqueous solution at normal temperatures and in the presence of chemical stabilizers that inhibit particle growth. It yields tiny, versatile active particles, comparable to those achieved with SFL.

Dow's Dowpharma unit, which runs BioAqueous, has already agreed to apply the solubilisation service to drug compounds from Bristol-Myers Squibb. BMS is the first major customer for the service.

The Dow and UT Austin collaboration is beginning its fifth year and has already improved the solubility profiles of compounds in a variety of therapeutic areas, including cardiovascular, metabolic, and antifungal drug compounds.