A growing number of new chemical entities are highly insoluble, leading to problems with bioavailability. Drug manufacturers therefore have to find ways of improving solubility if the product is to succeed. This also has to be done as quickly and efficiently as possible, with speed of the essence in every drug development program.
This playbook looks at why insolubility is an issue, and the properties that affect solubility, such as the molecule’s structure; its physical attributes (particle size and dissolution rate); its chemical attributes, including compatibility with excipients; and its biological properties.
It will also consider methods used to improve solubility and bioavailability, including:
- Spray drying, including the temperature shift process and volatile processing aids
- Particle size reduction, including micronization and nano-milling
- Hot melt extrusion
- Continuous bioavailability techniques
It takes a closer look at the particular challenges associated with oncology drugs, where the proportion of insoluble drugs in development is particularly high. Many insoluble anticancer drugs have already been successfully commercialized.
Finally, it will consider the importance of selecting the right partner to help improve the bioavailability of an insoluble molecule and get it into – and through – the clinic as fast as possible.