Out-licensing

Production of Stable Mixture of Drug and Excipient Particles

Introduction/Background

Some potentially promising drugs have difficulty in real-world use due to poor solubility in water, and thus low bioavailability in the patient. Producing small micro– or nano-sized drug particles can help solve this problem by increasing the surface area of the drug, which in turn increases dissolution rate and bioavailability. In addition, small particles are also ideal for pulmonary based delivery through aerosol and inhalation. Unfortunately, these small drug particles tend to aggregate, or agglomerate, after formation, which increases their average size and minimizes these advantages. Additionally, such agglomeration can adversely affect quality control by making the formulation less consistent and by limiting the drug's shelf life. Traditional mixing methods cannot overcome this problem, either due to a lack of efficiency or because the high energies required risk altering the drug's crystal structure. Supercritical carbon dioxide (SCCO2) is used commercially in the pharmaceutical and food industries in such processes as drug particle production and decaffeination of coffee.

Aims/Hypothesis

Novel methods are required for particle formation and excipient mixing.

Research

In the Auburn process, dissolved drug is injected into a tank containing SCCO2 in which excipient particles are already suspended. This produces drug particles of a desired size that are simultaneously mixed with excipient particles. The excipient particles interact with the drug particles, limiting the formation of drug-drug particles, and therefore limiting agglomeration. The simultaneous mixing of drug and excipient particles is inherent in the process. Very fine drug particles can actually be deposited on the surface of excipient particles.

Conclusion

Auburn University is seeking a licensee or development partner for a process to produce fine drug particles that do not aggregate after production. Using a modification of a well-established process, drug particles are formed in the presence of excipient (filler) particles. This works to keep drug particle size small, and therefore drug quality high. Additionally, two process steps (particle formation and mixing) are combined into one. This has potential application in the formulation of hydrophobic drugs for oral and pulmonary delivery.

Relevance/Opportunity

This technology is available for exclusive or nonexclusive licensing. Joint development opportunities include funded research or testing of a target drug.

Preclinical

A patent application has been filed