Giulia Milanedi began her presentation by introducing herself and the topic of formulation strategies to improve the viability of APIs with BCS classification II and IV. She provided an overview of Ardena, a Europe-based company with facilities across the continent, including drug substance facilities in the Netherlands and Sweden, a bio-analytics facility in the Netherlands, and drug product manufacturing sites in Belgium and Spain. Ardena supports customers from early drug substance development to GMP manufacturing for clinical trials, with analytical and regulatory services to aid in drug substance and product characterisation and regulatory submissions.
Milanedi highlighted the challenge of poor solubility and low bioavailability of new chemical entities classified as BCS class II or IV. She explained that conventional dosage forms were insufficient for these molecules, necessitating the use of enabling technologies to improve solubility and bioavailability. Ardena employs a screening tool to apply different enabling technologies, focusing on nanosuspension, amorphous solid dispersion manufacturing via spray drying, and lipid formulation.
She elaborated on nanosuspension, describing it as a colloidal dispersion of hydrophobic particles in a hydrophilic medium, usually water. The manufacturing methods included top-down processes like media milling and bottom-up processes like precipitation. Ardena primarily uses milling devices to achieve nanosuspension, starting with small batch sizes for screening and development before scaling up to larger batches. Milanedi presented a case study involving an API with poor water solubility, detailing the screening and development process, including the use of polymers and surfactants to stabilise the nanosuspension.
Milanedi then discussed amorphous solid dispersion, focusing on spray drying as the primary method. She explained the process of solubilising the API and polymer in organic solvents, atomising the solution into small droplets, and drying them to form amorphous solid dispersions. She provided an example of a project where they screened polymers for precipitation inhibition and upscaled the process for larger batch manufacturing.
Finally, Milanedi covered lipid formulations, particularly self-emulsifying drug delivery systems suitable for APIs soluble in lipids. She described the screening process for solubility in oils and surfactants and the evaluation of emulsification properties. She concluded by summarising the importance of enabling technologies for improving bioavailability and the need to screen multiple technologies in parallel.
