Superior dissolution improvements
The HyNap platform technology has been proven superior in a head-to-head comparison with traditional solid dispersion technologies such as spray drying and hot-melt extrusion. In a study performed by a major US pharmaceutical company , itraconazole formulations manufactured by various technologies with the same excipients and drug load were compared side-by-side. The graph shows the superior dissolution properties accomplished using XSpray’s HyNap composition.
This superior property has also been demonstrated for all tested PKIs for which solubility improvements typically range between 2-100 times. The nature of one HyNap PKI has been further investigated in collaboration with world leading academic collaborators and published in two scientifical papers. (1, 2)
– Jesson G, Brisander M, Andersson P, Demirbüker M, Derand H, Lennernäs H and Malmsten M. Carbon dioxide-mediated generation of hybrid nanoparticles for improved bioavailability of protein kinase inhibitors. Pharm Res. 2014 Mar;31(3):694-705.
– Colombo S, Brisander M, Haglöf J, Sjövall P, Andersson P, Østergaard J, and Malmsten M. Matrix effects in nilotinib formulations with pH-responsive polymer produced by carbon dioxide-mediated precipitation. Int J Pharm. 2015 Oct 15;494(1):205-17.
Hybrid Nano Particles (HyNap™)
HyNap is a supercritical fluid (SCF) technology that formulates compounds as HyNap™ – hybrid nanoparticles. The particles are stable amorphous solid dispersions and can be formed using a wide range of excipients.
HyNap™ A wide variety of solid dispersion systems have been successfully tested resulting in enhanced solubility as shown for example for Itraconazole.
Amorphous product with good stability can be produced through the tuning of process parameters. In the graph, XRPD shows that the product is still amorphous after six months storage at ambient conditions.
Since HyNap™ technology is based on supercritical extraction, the effective removal of solvent is ensured resulting in very low residual solvent amounts.
Since nanoparticles have inherently high particle surface area to mass ratio improved dissolution rates are achieved. HyNap™ technology is able to produce nanoparticles with consistent particle size below 200 nm. Adjusting process parameters, such as temperature, pressure and solvent choice, allow easy control of particle size and size distribution.
Amorphous or Crystalline
Nanoparticles can be produced from biomolecules as well as small organic molecules. Moderate temperatures are used in the process, allowing processing of thermolabile compounds. Both amorphous and highly crystalline particles can be formed.
High Drug Load
HyNap™ technology is compatible with a wide range of excipients that can be used to increase stability and/or wettability in amounts from >50% down to trace amounts. The active pharmaceutical ingredient (API) can also be processed without any excipients, generating a drug product with high drug load.
The Process and Manufacturing Features
HyNap™ technology is based on XSpray’s in-depth knowledge of supercritical fluid (SCF) technology, solid state properties, formulation science and the drug development process.
The technology uses supercritical fluid as an antisolvent for controlled precipitation of the API. The technology delivers better quality pharmaceutical particles and offers a superior process compared to alternative techniques.
Whilst offering all of the inherent benefits of traditional supercritical fluid technology, it has the added advantage of being fully scalable from discovery to drug manufacture.
XSpray offers manufacturing meeting US and EU regulatory standards. Your API is processed under cGMP conditions, providing high quality drug particles and powders for use in clinical studies. Manufacturing is carried out in collaboration with Galenica AB, an established Swedish CRO based in Malmö, Sweden. Galenica operates state-of-the-art GMP suites and is authorized and audited by the Swedish Medical Agency for GMP production of clinical trial material for Phase I-III. In addition to manufacturing, packaging and release testing services are also available.