Technology selection for bioavailability enhancement

At Lonza, we appreciate that choosing the best enabling technology (or technologies) for achieving adequate bioavailability (BA) can be complex.  Candidate molecules and target product profiles are increasingly challenging.  Problem statements may need to be redefined.  The need for accelerated timelines is commonplace.  Trial and error approaches are inefficient, costly and waste precious new chemical entity.

That’s why we have developed a fundamental, model-based approach to technology selection.  Predictive modeling, reference maps across key compound parameters and technology selection methodologies are in place which facilitate rapid selection of enabling technology for addressing BA challenges.  Our proprietary approach has been developed through the investigation and advancement of over 4000 molecules, and is based on a set of overriding principles:

  • A full understanding of the BA-limiting factors is crucial and includes both physicochemical and biological factors
  • The diverse needs of drug compounds cannot be addressed by any single technology
  • Development success, and rapid advancement of a compound, is more probable with matching the compound properties and drug product needs early in the development process
  • In many cases, more than one technology can be utilized successfully and commercial considerations such as desired dosing format can play a decisive role
  • Speed to clinic and market is best ensured by a focus on manufacturability during product design, thereby reducing the need for reformulation and facilitating rapid scale-up

These established technology selection methodologies are integral to our SimpliFiH® Solutions first-in-human service offering for the rapid advancement of BA-challenged molecules. Additionally, phase-appropriate and specialized processing equipment ensure rapid scale-up from concept to clinic and commercialization.

View our on-demand webinar which focuses on some of the key considerations for selecting and evaluating the appropriate technology for improving the oral bioavailability of poorly soluble compounds, centered around using a hypothesis driven approach to formulation.

View our webinar on-demand

Technology Selection for Improving the Oral Bioavailability of Poorly Soluble Compounds

Reference maps

Using our collective expertise in formulation science, our product development teams focus on the key physical and chemical properties of a compound and its dosage form requirements, working collaboratively with customers to develop tailored problem statements specific to the compound.  These problem statements are used to guide preliminary decisions regarding the selection of the most appropriate technology that offers the highest potential for performance, stability and manufacturability.

One tool utilized in choosing the right technology is 'reference maps' that have been developed across all key compound parameters and enabling technologies: particle size reduction, solid dispersions and lipid/liquid-based formulations:


These reference maps are a key component of our technology selection technologies having been developed through intensive research and modeling of thousands of compounds. QBD principles are also incorporated into the product design phase to ensure ultimate manufacturability of the formulation. In addition, specialized lab-scale processing equipment has been developed, based on science of scale studies, to rapidly evaluate technology approaches while minimizing NCE requirements.

Related content

Bioavailability Enhancement Technologies
Tech brief
Formulation Selection and In Vitro Screening for Oral Bioavailability Enhancement
Presentation slides
A Mechanistic Physiologically-Based Biopharmaceutics Modeling (PBBM) Approach to Assess the In Vivo Performance of an Orally Administered Drug Product: From IVIVC to IVIVP
Peer-reviewed publication
Technology Selection for Oral Bioavailability Enhancement Programs