Drug Delivery

Upsalite® in drug delivery

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

DrugDel2

When a drug is loaded into the pores of Upsalite®, it will be stored there in a so-called amorphous state. Amorphous forms of drugs, as opposed to a corresponding crystalline form of the same drug, have the advantage that it dissolves more rapidly into the gastrointestinal fluids. Therefore, drugs 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 drugs in registered pharmaceutical products are present in their crystalline state, despite that fact that drugs in an amorphous state have advantages from a dissolution point of view. The reason for that is that drugs in an amorphous form are usually not physically stable over time. With Upsalite®, however, drugs in an amorphous state can be stored and reamin stable over longer periods of time. This opens up new opportunities in drug delivery and and in the formulation of poorly soluble molecules into effective successful products.

Characteristics

  • 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 drugs
  • Upsalite® can be manufactured in a wide range of particle sizes in order to tailor release kinetics
  • Upsalite®  consists of magnesium carbonate, which is already used in food (E504) and drug products (Rennie, Samarin, etc.)
  • Simple and environmentally friendly manufacturing process

Applications

  • Upsalite® in preclinical projects, to formulate poorly soluble NCEs (New Chemical Entities) for in vivo studies. Simple translation of the formulation into clinical testing.
  • Upsalite® to reformulate a known drug for improved performance (Life Cycle Management or New Therapeutic Entities/505(b)2)
  • Upsalite® as a Modified Release system

 

Interested in a collaboration?

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