Drug Delivery

Upsalite® in drug delivery systems

Many oral drug molecules (APIs*) suffer from poor solubility, thus resulting in a poor uptake (absorption) of the API into the systemic circulation, and in turn reduced efficacy. Pharmaceutical scientists can address this issue by formulating the API into a more or less advanced delivery system (tablet or capsule). A novel, innovative but yet simple way of addressing the issue of poor solubility is to use the mesoporous material Upsalite® to increase the solubility of poorly soluble APIs.

DrugDel2

*API= Active Pharmaceutical Ingredient

When an API is loaded into the pores of Upsalite®, it will be stored there in a so-called amorphous state. Amorphous forms of APIs, as opposed to a corresponding crystalline form of the same API, has the advantage that it dissolves more rapidly into the gut/intestinal fluids. Therefore, APIs administered in an amorphous form have better chance of being absorbed for example from the gastrointestinal tract, and thus reaching its target for effect.

DrudDel1

©Peng Zhang

Most APIs in registered pharmaceutical products are manufactured in their crystalline state, even though APIs in an amorphous state have advantages from a dissolution point of view. The reason is that APIs in an amorphous form are usually not stable over time. With Upsalite®, amorphous APIs can be stored over longer periods of time, opening up a new opportunity.

 

In addition to being a carrier for poorly soluble drugs, Upsalite® can also be manufactured with larger pores, something that can be used to increase drug load into the formulations for example.

 

Regardless of the pore size, particle size of Upsalite® powder can be modified to alter the release kinetics of the APIs from Upsalite®, thus enabling Upsalite® to be used as controlled/delayed release carrier.

 

Important properties of Upsalite®

  • Upsalite® is a mesoporous material available with pore sizes in the nm-range and particle sizes in the µm range.
  • Upsalite® can be manufactured with different pore sizes to tailor Upsalite® for specific APIs
  • Upsalite® can be manufactured in a wide range of particle sizes in order to tailor release kinetics
  • Upsalite® can be used to stabilize APIs in an amorphous form and thus improve solubility/bioavailability and shelf life in products
  • Upsalite® (magnesium carbonate) is already used in food (E504) and drugs (Rennie, Samarin, etc.)
  • Simple and environmentally friendly manufacturing process
  • Low manufacturing cost and inexpensive raw material

Applications of Upsalite®

  • Upsalite® in preclinical projects, to formulate poorly soluble compounds for in vivo.  Simple translation of the formulation into clinical testing.
  • Upsalite® to reformulate an API for patent extensions/ life cycle management
  • Upsalite® as a controlled release system, for directed delivery of drugs, for example colon delivery.
  • Upsalite® as a drug delivery system for local delivery, for example topical or vaginal
  • Upsalite® to reformulate BCS class II APIs for better bioavailability

 

Interested in a collaboration?

Are you interested in exploring the unique properties of Upsalite®?  Please contact tuulikki.lindmark [at] disruptivematerials.com