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Substance solubility
January 2018
by Ilene Schneider  |  Email the author


HELSINKI, Finland—Drug discovery is a slow and costly process—at present, discovering and developing a new drug can cost more than $1 billion and take 13.5 years on average. At the early stages of drug discovery, there are thousands of molecules to be studied, but only small amounts of the substances available.
Information about the solubility of the substance is a critical success factor for drug development. After potency, solubility is one of the most important properties of a drug. Solubility is crucial because a substance that does not dissolve will not enter the bloodstream and cannot be effective in the body. In the absence of measuring the solubility of small amounts, the early stages of drug discovery have been focusing on the pharmacological and toxicological effects of the drug candidate.
Researchers at the University of Helsinki say that they have developed a new method to determine the solubility of pharmaceutical substances with samples 1,000 times smaller than ever before. The technique could have a great impact at the beginning of the drug development processes, providing more information with smaller samples and enabling faster development of new drugs.
“Single Particle Analysis, SPA, is the world’s first method for accurately measuring solubility from very small amounts of a substance,” according to a news release. “It is both significantly more precise and significantly faster than current technologies used in drug development. While other current methods measure how much of the substance has been dissolved in the liquid, this method turns the process around: a computer program analyzes microscope images to see how much the solid dissolving particle has diminished.”
Postdoctoral researcher Sami Svanbäck developed the innovation in his doctoral dissertation in Prof. Jouko Yliruusi’s research group at the University of Helsinki’s Faculty of Pharmacy. The idea originally arose from theoretical musing and the hypothesis that the dissolution of a substance could be determined by means of machine vision, from individual particles. This led to the development of the method and the instrument.
“SPA is a unique method based on optical shape recognition, and therefore requires no complicated chemical analyses or understanding of the chemical structure of the substance,” Svanbäck explained. “SPA uses machine vision and optical shape recognition to operate on particles that are invisible to the human eye. SPA focuses on the physical size. As a particle diminishes, we can determine how fast it dissolves. And best of all, SPA is appropriate for most substances, not just pharmaceuticals.”
The SPA method enables the determination of a drug’s solubility in the drug discovery process. It examines very small amounts of substance to help find the most viable candidate for further development. SPA is a multidisciplinary combination of physical chemistry, optics, fluidics, machine vision, engineering and software design.
Svanbäck believes that SPA is at the “cutting edge of personalized medicine,” noting that “In the near future, all patients will receive the medication and dosage specifically tailored to them. For this reason, it must also be possible to predict and change the solubility and release of each drug in the body of the individual. Here, SPA could help by providing extensive solubility data quickly and precisely.”
After successful proof-of-concept studies with some of the largest pharmaceutical companies in the world, Yliruusi’s team is ready to launch its start-up company in January 2018. The patent application is currently in the international stage.
The other founders of the start-up include Yliruusi from the Faculty of Pharmacy, who has extensive experience in drug discovery, having participated in bringing more than 200 pharmaceutical products to market, and Kari Jussila, business world and technology professional. Start-up investor Harry Santamäki and product development guru Ville Voipio will be serving as advisers.
Svanbäck summarized, “Single particle analysis offers a completely new way to address the central challenges of drug discovery: expense and duration. SPA can significantly speed up early-stage decision-making by providing crucial—and previously unattainable—information about substances in development, making SPA the missing link of drug discovery. SPA thus enables holistic drug development based on both pharmacology and physical chemistry.”
Code: E011804



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