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Micro- and nanoformulation of APIs using CO2 expanded solvents


*Corresponding authors
1. Institut de Ciència de Materials de Barcelona (ICMAB-CSIC), Campus Universitari de Bellaterra, 08193 Cerdanyola del Vallès, Spain
2. CIBER de Bioingeniería, Biomateriales y Nanomedicina (CIBER-BBN)
3. Nanomol Technologies SA, Módul de Recerca B, Campus Universitari de Bellaterra, 08193 Cerdanyola del Vallès, Spain


Nanomedicine, as the medical application of Nanotechnology, is a promising alternative to overcome the problems of the administration of APIs and biomolecules, either already existing drugs or new entities coming out from the discovery pipeline.
In this paper we endeavour to show the potentiality of DELOS Technology Platform, which uses CO2-expanded solvents, for the one-step production of active pharmaceutical ingredients (APIs) in the form of micro- or submicron crystalline powders or colloidal preparations, with tailored characteristics in terms of size, morphology,crystallinitiy and polymorphism. DELOS is an efficient easy scalable platform for the preparation of new micro and nanoformulations for improving protection of actives against early degradation, preventing their premature interaction with the biological environment, facilitate higher payloads, prolong their circulation life-time, improve drug targeting and solubility and provide controlled release of the therapeutics into the blood stream or the target tissues or organs.


Nowadays there is an increasing investment in new and more efficient drug delivery systems because the acceptance of new drugs is expensive, risky and slow. Pharmaceutical companies are keen to investigate new formulations that can deliver or target more effectively existing drugs, since this offers a new and less costly route to increase their product portfolio. Among the different strategies for giving added value to drugs, particle size reduction is probably one of the most investigated. For instance, micro- or nanosizing of poorly water soluble drugs can dramatically improve their bioavailability through the increase of their surface area and hence, their dissolution rate. Thus, aqueous suspensions of micro or nanoparticulate drugs can be administered orally or parenterally with an important enhancement in their pharmacokinetic behavior (1). Control over size and size distribution also becomes crucial when choosing a certain route of administration. For instance, to effectively deliver a pharmaceutical active compound via the pulmonary route, which is a particularly attractive treatment option for diseases where patients require frequent ...