Drug product development
Solubility & bioavailability enhancement
Does your molecule show poor solubility or bioavailability?
Xedev supports you with in-depth formulation and process development to overcome these barriers. By enhancing solubility and permeability, we ensure absorption of your molecule at the target site so it can deliver the desired pharmacological effect.
Our team applies the most suitable solubility enhancement techniques for your compound—including amorphous solid dispersions (ASDs), particle size reduction via e.g. nanosuspension or complexation via e.g. cyclodextrins.
We help you make early, confident decisions with your molecule and prepare for clinical success.
Amorphous Solid Dispersions (ASDs)
Amorphous Solid Dispersions (ASDs) are one of the most effective ways to improve drug solubility. In an ASD, your molecule is embedded amorphously into a solid matrix, typically a polymer (mixture). This amorphous state of the drug and the resulting supersaturation effect are critical to increasing the bioavailability of your molecule.
Xedev selects the most suitable technique for your compound to form an ASD: spray drying, hot melt extrusion (HME) and/or bead coating. Based on your compound’s specific characteristics and project needs.
Spray drying | HME | Bead coating | |
|---|---|---|---|
Suitable for thermo-sensitive compounds | |||
Limited API consumption in early phase | |||
Low operating cost/ energy consumption | |||
Continuous process/ ease of scaling | |||
Solvent-free |
Spray drying
As a world expert in spray drying, Xedev is your preferred partner for ASD formation via spray drying. During spray drying, a drug-polymer solution is atomized in a heated chamber and then rapidly dried to form a homogeneous dry powder.
We assist in ASD development via a stepwise and fast approach, taking into account the limited amount of API available during early preclinical development.
Small scale screening
Do you only have a limited amount of API available? Xedev performs polymer selection immediately via spray drying, excluding film casting experiments. Thanks to the valuable combination of Xedev’s expertise and our unique lab-scale spray dryer, we screen using only a limited amount of API (starting from 10 mg per concept).
Curious how Xedev evaluates the solid state of your first concepts?
Formulation selection
Preclinical production batches for PK and/or tox studies
Dosage form development
Depending on your need, Xedev formulates your ASD material as a suspension, capsule or tablet for further in vivo evaluation.
Do you want to know more about Xedev’s expertise in capsule and tablet preparation?
GMP production batches for clinical trials
All the material for your clinical studies is prepared at Xedev. No upscaling or tech transfer needed.
Interested in learning more about our GMP services?
Powders with your desired attributes
Did you know that – besides the formation of an ASD – spray drying allows you to produce powders with your desired size, shape, density, specific surface area and flowability by adjusting the process parameters?
Hot melt extrusion (HME)
Is your molecule poorly soluble in a wide range of solvents but thermally stable? Developing an ASD via Hot Melt Extrusion (HME) is the way forward! With this technique, API and polymer(s) are blended and pushed through a heated barrel containing transporting and kneading areas. The resulting extrudates require minimal downstream processing – such as cutting or milling – and can be filled into capsules or compressed into tablets.
Do you need assistance with the downstream processing of your extrudates?
Bead coating
Aiming for an ASD formulation that is immediately ready for patient use? Using bead coating, your drug-polymer solution is nebulized on inert beads loaded with your ASD in a fluid bed. After processing, these beads are ready to be filled into capsules, without further processing, ready for patient dosing!
Capsules & tablets
Is a powder form not your end goal? We can help you with the downstream processing of your molecule into capsules or tablets as well.
Other enabling technologies
Nanosuspensions
Reducing the particle size of your molecule via preparation of nanosuspensions is another possible strategy to enhance the bioavailability of your molecule and increase its therapeutic effect. A reduced particle size results in an increased available surface area and accelerates dissolution. We formulate your nanosuspension via bead milling, selecting the right stabilizer to reduce crystal growth.
To improve shelf life and stability of your formulation, we convert your nanosuspension into a solid form using spray drying.
Curious about Xedev’s capabilities to prepare solid dosage forms?
Inclusion complexation with cyclodextrins
Do you have a hydrophobic drug with low aqueous solubility?
Solubility enhancement via inclusion complexation might be the answer your problem. Complexation refers to the binding between a ligand (your compound) and another (small or large) molecule. Cyclodextrins are commonly used in this binding due to their unique structure: they possess a hydrophobic cavity and a hydrophilic surface.
Altering the physicochemical properties of your compound increases its solubility, stability, and safety. Xedev combines complexation with spray drying to deliver stable, processable powders with the right powder properties.
Lipid-based formulations
Lipid-based formulations (LBFs) are interesting for APIs with a high lipophilicity and a low melting point. For certain compounds, LBFs enhance permeability across the gastrointestinal barrier by forming an emulsion upon contact with bodily fluids. Through a screening approach, we help you select the right lipid (mixtures), surfactants, and cosolvents to boost bioavailability.