Proof of concept and business case for Upsalite® as solubility enhances for poorly soluble drugs.
| Reference number | |
| Coordinator | DISRUPTIVE MATERIALS AB |
| Funding from Vinnova | SEK 2 000 000 |
| Project duration | October 2014 - September 2016 |
| Status | Completed |
Purpose and goal
The aim of the project was to show that Upsalite can be used as drug delivery platform in order to improve the solubility of poorly soluble molecules, and thereby improving the bioavailability. The aim of the project was to show a ´Proof-of-Concept (PoC)´ both in vitro and in vivo.
Expected results and effects
The in vitro results (comparison between celecoxib in a commercial formulation and celecoxib loaded into Upsalite) showed that the loaded celecoxib had a faster dissolution rate than the commercial formulation. Further, the in vivo results showed that the Upsalite formulations resulted in higher bioavailability.
Planned approach and implementation
The in vitro dissolution experiments were performed in a USPII dissolution bath at pH 1.2 (to resemble gastric fluid) and pH 6.8 (to resemble intestinal fluid). The animal study was conducted in rabbits (n=3/group). Upsalite formulations (oral gavage) were compared to Celebra® (the content of the capsule emptied to be administered as an oral gavage). Further, the influence of particle size on the bioavailability was studied where small and large particles of celecoxib loaded Upsalite were compared.