(230b) Stripfilms As Oral Dosage Platform for the Delivery of Nano-Particles of Active Pharmaceutical Ingredients (APIs)

We describe formation of stripfilms loaded with nano and low micron sized API particles to achieve desired delivery properties through maintaining of the high surface area of particles via particle engineering. As a platform to incorporate particle engineering, this approach will allow for a fundamental shift in the design of pharmaceutical products containing nano-particles without the need for first drying or recovering nano-particles in dry form. Our approach consists of forming stable nano-suspensions of BCS Class II drugs via three top-down and bottom-up approaches to achieve size range of 100–2000 nm, with API loading of 0.1 to 20 wt% in the suspensions. The API suspensions are stabilized via judicious use of polymer-surfactant combinations to achieve size stability ranging from 2 hours to 2 days. These suspensions are further processed to increase their polymer content by mixing with higher polymer containing aqueous gels or solutions. These film-precursors containing nano-APIs are formed into films, whose thickness is in the range of 50 to 200 microns, via the solvent-casting approach utilizing convective drying.

We have analyzed the retention of large API surface area in these films via re-dispersion in water, showing that this integrated particle engineering approach allows for maintaining high surface area of the API particles, which has been a non-trivial problem faced by the pharmaceutical industry. Films characterization confirms good API uniformity with API content linearly dependent on film thickness.  Dissolution of films also proves to be much faster than other dosage forms mainly due to the high surface area associated with thin films in combination with fast, full-recovery of small API particles during dissolution. This approach may be suitable for BCS Class II drugs requiring enhancements in bioavailability for producing clinical supplies. Stripfilms can also serve as a quick-to-market platform for flexible, uniform dose manufacturing of BCS Class II drugs.