Challenge
Therapeutic proteins are inherently unstable and are sensitive to temperature change, shearing, shaking, solvents, ionic strength, purity, protein concentration, pressure and freeze/thaw-drying cycles. Of all the various degradation pathways possible, aggregation is one of the most common and a cause for great concern. Formulation is a key component that is required in order to produce a stable and efficacious biologic medicine.
Many excipients are used within biologic drug formulations, including a range of surfactants called polysorbates. As a potential functional alternative to surfactants within biologic formulations, KLEPTOSEô‚¡´ can act as an inhibitor of protein aggregation in liquid formulations by:
Shielding hydrophobic interactions to block potential protein-protein interaction which causes aggregation.
Displacing proteins induced by air-water interface.
Experiment objective
To benchmark KLEPTOSE® HP/HPB against polysorbates in commercial mAb formulations.
Conclusion
We have shown that KLEPTOSE® BioPharma (hydroxypropyl beta cyclodextrin) represents a promising alternative to surfactants commonly used within biologic formulations, such as polysorbates Tween 20 and 80. Formulations containing KLEPTOSE® BioPharma perform better than the reference formulations containing polysorbates, when subjected to stress conditions of shaking (1400 rpm) and temperature (40°C). It represents a functional alternative to surfactants within biologic formulations.