Unleash your drug’s potential: Highway to Clinic Platform for enhanced bioavailability
In the realm of pharmaceutical development, achieving optimal bioavailability is paramount to ensure the efficacy and safety of drug products. Bioavailability refers to the extent and rate at which the active moiety (drug or metabolite) enters the systemic circulation, thereby accessing the site of action. However, many drug compounds exhibit poor bioavailability due to various factors such as low solubility, poor permeability, and susceptibility to metabolism. Our Highway to Clinic platform offers a comprehensive approach, screening different drug product innovative formulation technologies, to overcome these challenges. Eurofins CDMO provides the expertise and support required to select and optimize the most suitable formulation technology for your drug candidate.
Key technologies for Bioavailability Enhancement
To address the challenges associated with poor bioavailability, we have developed a program of technologies aiming for improved drug solubility and permeability. Identifying the most suitable formulation technology early in your development process is our main driver.
- Aqueous Solutions (solubility enhancement)
- Nano/Micro suspensions
- Lipid Formulations
- Amorphous Solid Dispersions (ASDs)
Aqueous Solutions
Administration of an API in a dissolved form allows bypassing the dissolution step, thus accelerating the absorption phase.
Our formulation experts have proven track experience in selecting the best approaches to overcome the low aqueous solubility of new chemical entities e.g. modification of the API via salt formation, incorporation of solubilizing excipients such as complexing agents, surfactants or co-solvents.
Nano/Micro suspensions
Reducing drug particle size to micro- or even nanometer scale leads to a drastic increase of the surface area available for solvation and thus improved dissolution kinetics.
At Eurofins CDMO, we have extensive experience in top-down particle size reduction processes via wet milling followed by stabilization of these nanosuspensions.
Lipid Formulations
These formulations typically consist of lipids, surfactants, and co-solvents, which solubilize the drug and facilitate its absorption in the gastrointestinal tract.
Self-emulsifying drug delivery systems (SEDDS) are a prime example of lipid formulations designed to enhance drug solubility and bioavailability. Upon administration, SEDDS spontaneously form oil-in-water emulsions, increasing drug solubilization and promoting absorption through lymphatic transport.
Amorphous Solid Dispersions
ASDs represent an innovative approach for bioavailability enhancement by dispersing poorly water-soluble drugs in a polymer matrix.
Unlike crystalline drug formulations, amorphous drugs exhibit higher energy states and greater molecular mobility, leading to enhanced dissolution rates and improved bioavailability.
By preventing drug recrystallization and maintaining a high-energy amorphous state, ASDs enhance drug solubility, dissolution kinetics, and absorption.
At Eurofins CDMO, we have in-house expertise to produce ASDs via spray-drying and bead-coating technologies.
From liquid to solid dosage form
For pre-clinical and/or phase 1 clinical studies liquid dosage forms offer advantages such as:
- Dose flexibility
- Lower API requirement
- Rapid development
- Ease of production at larger scale
Eurofins CDMO also offers state-of-the-art capabilities for the solidification of a liquid formulation (e.g. in view of later clinical phases) using an optimized approach which is determined by the route of administration, final dosage form, and API characteristics. Possible solidification techniques are:
- Freeze drying: Sublimation of solutions, (nano-)suspensions and SEDDS.
- Spray drying: Atomization of solutions and (nano-)suspensions followed by evaporation of the solvents via fast drying.
- Bead coating: Spraying of liquid formulations on an inert core with parallel drying process.
- Granulation: Spraying of liquid solutions or suspensions on an inert powder in combination with polymeric binders.
- Adsorption on solid carriers: Loading of SEDDS on an inert powder.
As a final step, the solidified drug product can be downstream processed into a patient-compliant final dosage form such as powders for reconstitution, capsules, tablets or multiparticulate products.
Your complete journey from pre-formulation up to clinical supply
Our Highway to Clinic platform is a fast-track program which covers a wide range of activities such as:
- Drug substance characterization
- Pre-formulation studies
- Complete analytical support, method development and method validation
- Formulation development and optimization
- Production for PK and toxicity studies
- Accelerated Stability Assessment Program (ASAP) studies for drug product prototype ranking and shelf-life predictions
- Stress studies and stability studies
- Upscaling activities and manufacturing process transfer to GMP
- GMP manufacturing
- QC release and stability testing and QA release
- Clinical Trial Supply
Eurofins CDMO is committed to provide a dedicated team of technical experts involved from early development to clinical manufacturing ensuring a seamless transition from development to GMP.
Main Benefits of the Highway to Clinic platform:
- Accelerated drug development: Identifying the most suitable formulation technology early in the development process by evaluating multiple formulation technologies streamlines the drug development timelines and reduces costs.
- Enhanced Bioavailability: Overcoming solubility and absorption limitations significantly improve drug bioavailability, leading to better therapeutic outcomes.
- Liquid and solid dosage forms: For pre-clinical and/or phase 1 clinical studies, liquid dosage forms offer more flexibility and faster development. Furthermore, Eurofins CDMO also offers state-of-the-art capabilities for the solidification of these technologies in view of phase II, phase III or commercial productions.
Partner with Eurofins CDMO to accelerate your drug development