Turning zein-based nanostructures into oral lyophilizates to address paediatric needs

Paediatric patients suffer from a lack of oral medications tailored to their various needs, including safe administration and adaptable dosing. This study intends to address the issue through the formulation of zein-based nanostructures containing loratadine, subsequently included in oral lyophilizates to obtain easy-to-administer dosage forms. The nanostructures were obtained through antisolvent precipitation, the purified nanosuspensions being mixed with appropriate excipients and freeze-dried. The optimal formulations for the nanostructures and oral lyophilizates were determined through experimental design. The nanosuspensions were analysed in terms of particle size, size distribution, surface potential, drug content and encapsulation efficiency. The oral lyophilizates were tested for hardness, disintegration time and optical contact angle. The presence of nanostructures in the final product was evaluated through electron microscopy. Nanostructures of approximately 300 nm, with an encapsulation efficiency of 95 %, were obtained, as well as oral lyophilizates with satisfying mechanical and disintegration properties. A design space proved that oral lyophilizates with an adequate quality profile can be obtained within a wide range of nanosuspension content. This study demonstrates that stable nanosuspensions can be obtained using natural excipients, while also highlighting an easy manner to create formulations where the active substance dose can be easily varied depending on patient needs. • Zein nanostructures are easily prepared from safe, naturally occurring substances. • Oral lyophilizates allow for a child-friendly formulation with only two excipients. • Experimental design was used to enable dose customisation of the final product. • The particular release profile opens new avenues in paediatric drug development.