High drug load formulations based on nanocrystals matching the performance of solid dispersions while reducing pill size and pill burden.
- The increased complexity of novel small molecules requires innovative drug delivery methodologies to enhance solubility
Nanoform’s unique particles enable high drug loadings and fewer, smaller tablets.
Small molecules for oral administration still dominate approvals and development pipelines, however, the majority are undruggable due to low solubility and require enabling technologies. When traditional solubility-enhancing techniques such as the use of salts and micronized formulations fail to enhance solubility and bioavailability, formulators often turn to advanced formulation strategies, including amorphous solid dispersions (ASD). Though ASDs have enabled the druggability of dozens of APIs, their development often demands that patient and environmental considerations are compromised. Two thirds of marketed drugs developed as a solid dispersion contain at least two-thirds excipients, meaning the pill burden and/or the size of the tablets can be large.
As the nanoforming process itself does not rely on the use of polymers, it is possible to develop pills that are much smaller than their ASD counterparts, and/or reduce pill burden through high drug loading in nanocrystals and nanocrystalline intermediates.
Advantages of CESS® nanoparticles over ASDs:
- Higher drug loading in the final dosage form, reducing pill size and/or pill burden
- Similar or outperforming in vivo performance compared to ASDs,
- Reduced in vivo variability in exposure
- Elimination/reduction of food effect
- In contrast to ASDs, Nanoformed particles typically exhibit excellent long-term stability
- Easier to handle material, elimination of secondary drying and simpler formulation
- Nanoforming does not require organic solvents, such as those used in spray drying (e.g., dichloromethane, acetone), and so has a lower carbon footprint.
If you are interested in nanoparticle-based formulations matching the performance of ASDs and enabling high drug load final dosage form, contact us.