Topical formulations

ERCO Pharma’s technologies makes it possible to study how modifications of your transdermal formulation changes the partitioning of the API and associated permeation enhancers into the skin barrier. This, combined with permeation simulations, allows us to guide you through the process of choosing the optimal permeation enhancers for maximized transdermal transport.

Partitioning is important for transdermal delivery

Transdermal drug delivery is not only a matter offinding the correct permeation enhancers for your active pharmaceutical ingredient (API), it also requires a topical formulation that promotes partitioning of both excipients and the API, into the barrier structure.

This is an effect that is challenging to measure experimentally and often only data regarding the flux from different formulation compositions is available.

Our detailed simulation techniques enable us to predict the partitioning of your API, and excipients, from the formulation and into the skin’s barrier structure. This data can then be used to optimize the API solubility in the formulation, which will make it possible to improve the flux across the skin.

Increased understanding of the interaction between formulation and barrier

Understanding how the formulation affects the barrier is of utmost importance when designing an effective transdermal delivery system for your API. Knowing where the API is passing slowly through the human skin barrier enables a choice of suitable permeation enhancers.

The atomistic resolution gives us detailed information regarding the effect of each permeation enhancer, at concentrations based on the formulation. This includes how they affect the barrier structure as well as the permeability and flux.

Combined with experimental knowledge, this methodology serves as a powerful tool when determining the mechanism of action for the formulation’s transdermal transport properties.

Molecular modeling as a tool in formulation development

Maximized transport of an API across the human skin barrier depends on its formulation solubility, partitioning into the skin barrier, as well as the permeation enhancing effects of the formulation excipients. Molecular modeling is a powerful tool capable of investigating these properties, and is able to deliver data unobtainable by, and complementary to, conventional experimental methods.

When integrated into an existing workflow, molecular modeling increases the knowledge extracted from the investigated system and enables a detailed description of the molecular interactions during the transdermal delivery.

Taken together, the data generated from molecular modeling and experiments enhances the effectiveness of the formulation development process and will make it easier to get new permeation enhancers accepted for use in future transdermal products.

Read more about our molecular modeling approach here or click the image to the right.