An Elegant Micronization Method Enabling The Formulation Of Biopharmaceuticals

By Audrey Hecka, PhD., Senior Scientist, and Elizabeth Jones, PhD., Associate Scientist, DSM Biomedical

Advances in drug delivery forms that help improve efficacy and ease of compliance are enabling a patient-centric approach to treatment plans. Sustained release drug delivery systems (DDS) offer effective therapies in the treatment of serious chronic diseases, with numerous advantages over traditional therapies. These treatments also make a tremendous difference for patients by limiting systemic side-effects and addressing the challenge of compliancy with regards to taking medications.

Leveraging therapeutic-loaded microspheres can help achieve the goal of improved DDS design. The Solid-in-Oil-in-Water (SOW) emulsification process to produce microspheres offers a significant advantage, such as avoiding degradation of the API at the water/organic solvent interface, but achieving good encapsulation efficiencies and suitable release profiles can be challenging with an API raw material that is not suitable in terms of particle size range.

Micronization of the API raw material is a key process to help increase the loading efficiency and lower the burst of the obtained microspheres, and applying lyophilization-based micronization methodology at a small scale helps to support challenging formulation development projects from early technical feasibility to the preparation of samples for preclinical studies.