Solubility enhancement with Dispersome? technology

Poor drug solubility is one of the biggest challenges preventing the development of novel drugs. Up to 90 % of all new drug molecules are poorly soluble, which can be a problem as the drug must dissolve in order to be absorbed and reach its pharmacological target. Many otherwise promising drug candidates are discontinued during early-stage development due to poor bioavailability resulting from poor solubility. Learn more about it in the edition of "The Excipients Week"

Dispersome?is a technology based on a natural, biodegradable excipient. The technology uses high quality whey protein, an environmentally friendly by-product from cheese production, to improve the solubility and bioavailability of poorly soluble drugs.

The Dispersome? platform allows formulating poorly soluble small molecule drugs as stable amorphous dispersions with a high drug load. The amorphous form of a drug can increase its inherent solubility and by increasing solubility and dissolution rate the Dispersome? technology can improve bioavailability of drugs and reduce the dose required. To form a Dispersome? formulation the crystalline drug compound is simply mixed with the whey protein beta-lactoglobulin (BLG) and processed into an amorphous mixture.

A unique enabling excipient

The Dispersome? technology stabilizes the amorphous form by forming a unique drug dispersion in a protein-based matrix, resulting in exceptional drug loading and dissolution enhancement. Whey proteins have demonstrated an excellent ability to form amorphous mixtures and are both inexpensive to manufacture and safe to use. Compared with conventional polymeric excipients such as PVP, PVPVA and HPMCAS, BLG allows higher drug loading (>50%) and dissolution rate while maintaining stability.

The Dispersome? technology not only makes it possible to develop drugs that would otherwise never reach the market. In many cases, the technology outperforms other technological solutions on key parameters with major improvements in both drug loading, solubility, and bioavailability. Moreover, by replacing the use of fossil polymers and reducing the amount of drug needed per tablet, it saves resources in the manufacture and reduces toxic drug waste into the aquatic environment.

Beta-lactoglobulin as pharmaceutical excipient

Proteins comprise a new group of excipients for preparing amorphous solid dispersions. Beta-lactoglobulin (BLG), the main component in Dispersomes, results in superior drug solubility compared to other proteins. Zerion Pharma has a strong IP portfolio covering protein-based excipients for solid dispersions with patent life beyond 2040.

Stable formulations with high drug loading

The use of Dispersome? technology enables drug loadings above 50% w/w while maintaining stability and improving API solubility. At a drug loading of 50%, stable amorphous formulations are obtained for more than 80% of all drugs tested.

A safe and manufacturable excipient

Zerion Pharma works with a world leading supplier to source and qualify our Pharma-Grade BLG material, ensuring high quality and large scale. BLG is a natural ingredient used in food and nutrition products and is easy to integrate in your existing processes.

Superior outcomes, compatible technology

By increasing drug solubility, the Dispersome? platform aims at improving oral bioavailability and therapeutic outcomes for patients. Dispersome? formulations are compatible with standard pharmaceutical processes and Spray Drying provides a scalable manufacturing solution for Dispersomes.

Improved dissolution profile

Dispersome? formulation achieves a superior dissolution rate and better solubility compared to other solid dispersions when addressing a poorly soluble drug, ZN-X.

Interested to learn more? Get in touch with Korbinian L?bmann from Zerion Pharma or go to Zerion Pharma - A new frontier in drug formulation.

#excipients #solubility #pharmaceuticals