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.
*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.
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