Formulation optimisation of topical treatment led to same efficacy with 30% less of the active pharmaceutical ingredient


A specialty pharmaceutical company requested MedPharm scientists to investigate a 5% cream formulation of a proprietary drug to see if the relatively high loading of the drug could be reduced. The aim was to achieve this without significantly changing the formulation’s excipients.

The MedPharm team went back to first principles and measured the solubility and stability of the active in the different excipients in the formulation. They showed that by adjusting the concentration of the excipients in the existing formulation to optimise the drug’s thermodynamic activity they could achieve the same penetration and permeation in IVPT experiments with a 3.75% cream. This reduction benefits patients by reducing their total exposure to the drug and significantly reduced the cost of manufacture of the product.

The activity of the 3.75% cream was subsequently demonstrated in the clinic in a Phase 3 trial by the client.