Evaluation of crystalline lactose-PEG composite particles as potential carriers for DPI formulations
J T Pinto1,2, S Zellnitz1, T Guidi3, L De Smet4, E Roblegg1,2, A Paudel1,5
1 Research Center Pharmaceutical Engineering GmbH, Inffeldgasse 13, Graz, 8010, Austria
2 Institute of Pharmaceutical Sciences, Pharmaceutical Technology and Biopharmacy, University of Graz, 8010 Graz, Austria
3 Chiesi Farmaceutici S.p.A., Largo F. Belloli 11/A, Parma, 43122, Italy
4 Xedev bvba, Industriepark Rosteyne 4, Zelzate, 9060, Belgium
5 Institute for Process and Particle Engineering, Graz University of Technology, Inffeldgasse 13,
Graz, 8010, Austria
Summary
Crystalline α-lactose monohydrate is and has been for many years the preferred carrier in dry powder inhaler (DPI) formulations. It is accepted that carrier particles can impact DPI performance. So for many years lactose particles have been subjected to engineering in order to develop new improved DPI products able to tackle today’s patient needs. Consequently, it was the aim of the authors to evaluate if it is possible, via spray-drying and with the aid of polyethylene glycol (PEG), to engineer crystalline lactose particles with improved performance as DPI carriers. Thus, the present work showed, for the first time, that it is possible to produce, via spray-drying, predominately crystalline lactose particles with a size identical to other commercial available respirable grade lactoses. The produced composite lactose-PEG particles showed to be spherical with a surface composed mainly of PEG plate like structures, covering it as a structured shell. Blends prepared with the novel carriers and milled salbutamol sulphate in a 2% w/w ratio revealed to have an inferior in vitro aerodynamic performance than the mixtures containing a commercial grade lactose (Respitose®).
