Trapping liquid drugs inside crystals

The objective of this work is to embed liquid or volatile pharmaceuticals inside crystalline materials, in order to tune their delivery properties in medicine or agrochemistry, and to explore new regulatory and intellectual properties issues. Liquid or volatile formulations of active pharmaceutical ingredients (APIs) are intrinsically less stable and durable than solid forms; in fact most drugs are formulated as solid dosage because they tend to be stable, reproducible, and amenable to purification. Most drugs and agrochemicals are manufactured and distributed as crystalline materials, and their action involves the delivery of the active molecule by a solubilization process either in the body or on the environment. However some important compounds for the human health or for the environment occur as liquids at room temperature. The formation of co-crystals has been demonstrated as a means of tuning solubility properties of solid phases, and therefore it is widely investigated by companies and by solid state scientists especially in the fields of pharmaceuticals, agrochemicals, pigments, dyestuffs, foods, and explosives. In spite of this extremely high interest towards co-crystallization as a tool to alter solubility, practically no emphasis has been paid to using it as a means to stabilize volatile or labile or low-melting products. In this work we trap and stabilize volatile and liquid APIs and agrochemicals in crystalline matrices by engineering suitable co-crystals. These new materials alter the physic state of the active ingredients allowing to expand the phase space accessible to manufacturing and delivery. We have defined a benchmark of molecules relevant to human health and environment that have been combined with suitable partners according to the well known methods of crystal engineering in order to obtain cocrystals. The first successful results will be discussed; the Figure shows a cocrystal of propofol, a worldwide use anesthetic.

Crystallography at your door

The idea at the basis of the project 'Crystallography at your door' is to associate crystallography with cultural, artistic, and natural beauty by creating a virtual list of `Crystallographic sites in Italy'. One of the challenges that science in general has to face is to increase awareness of the impact that research has on daily life, culture and history. In addition, crystallography is not a discipline generally known to public, and while the words chemistry, physics, biology immediately bring to people at least some memories of lessons at high schools, crystallography remains an obscure term. However the natural beauty of crystals related to their regular shape, symmetry, colours has since the dawn of humankind fascinated people; even nowadays concepts related to crystals are widely used in marketing to convey to the buyers the idea of cleanliness, purity and freshness of many products, that are not necessarily related to crystalline materials. On the wave of IYCr2014 the Italian Crystallographic Association promotes initiatives to bring people closer to crystallography [1]; one of these is aimed at stimulating people to look around for places where crystallography may be seen 'in action' in all its facets: mines, saltworks, historical places related to the work of crystallographers, museums, and most of all buildings or masterpieces of art where symmetry has been exploited to create beauty. Italy has a unique strength in the artistic and cultural heritage fields; in the last years the public awareness towards the richness of Italy in this area has been growing and has being fostered by media and public institutions. A list of 'italian crystallographic sites' has been compiled and is being continuously extended on the IYCr2014 italian website[1]; it will be advertised at tourist offices and an applet for smartphones will be implemented.

CrystalinItaly

The actions for celebrating IYCr2014 in Italy are coordinated by the Associazione Italiana di Cristallografia (AIC), with the contribution of the Società Italiana di Mineralogia e Petrologia (SIMP) and of the Società Italiana di Luce di Sincrotrone (SILS). All the activities are gathered in a dedicated website, www.iycr2014.it, created to convey to the public and media all the information related to crystallography and on the activities that will take place in Italy. The general initiatives organized in Italy intend to be the basis for long term actions with two main objectives: to reach general public and to reach especially high school teachers. The high school teachers are key figures to build a better perception of crystallography for the next generations: previous experience in outreach and divulgation towards schools shows that teachers are highly influential to direct students' future careers. To reach high school teachers and to increase their motivation in teaching crystallography in the science syllabus, a completely new teaching pamphlet has been created, to provide a written modern, clear, and friendly instrument to learn and explain the simplest concepts related to crystallography, linked to everyday life and complemented with simple experiments. This will be distributed freely to teachers and students. To reach general public is a second important aim, where the challenge is to increase awareness of the impact that crystallography has on daily life, culture and history. An initiative to bring crystallography at everybody's door has been launched, consisting in the creation of a list of the Italian crystallographic sites, that has been put on the web site and will be implemented in an applet for smartphones. Moreover, the exhibition 'Cristalli!' is being organized in several places, having being launched in Padua with thousands of visitors in 5 months.