The number of drugs coming from synthesis and being poorly soluble in water is steadily increasing. At present, 40% of the drugs in the development pipelines and approximately 60% of the drugs coming directly from synthesis are poorly soluble. Particle size reduction to micron scale is a suitable method to enhance the bioavailability of poorly soluble drugs. However, in many cases micronization cannot solve the bioavailability problem. As a consequence, next step moves from micronization to nanonization, i.e. production of drug nanocrystals. This step has been possible thank to the recent development of new nanotechnologies. Drug nanocrystals are nanoparticles composed of 100% drug without any matrix material and with a mean particle size below 1µm. In the present chapter, the techniques used at the laboratory scale and industrial scale for the production of nanocrystals will be presented, divided in bottom-up, top-down, and combined technologies. The physicochemical and technological methods for the characterization of nanocrystals will be considered as an essential tool in the drug product development. An overview of the nanocrystals on the market and under development will be also presented.
2. Advanced techniques in nanocrystallization of active pharmaceutical ingredients
MARTENA, VALENTINA;DI MARTINO, Piera
2012-01-01
Abstract
The number of drugs coming from synthesis and being poorly soluble in water is steadily increasing. At present, 40% of the drugs in the development pipelines and approximately 60% of the drugs coming directly from synthesis are poorly soluble. Particle size reduction to micron scale is a suitable method to enhance the bioavailability of poorly soluble drugs. However, in many cases micronization cannot solve the bioavailability problem. As a consequence, next step moves from micronization to nanonization, i.e. production of drug nanocrystals. This step has been possible thank to the recent development of new nanotechnologies. Drug nanocrystals are nanoparticles composed of 100% drug without any matrix material and with a mean particle size below 1µm. In the present chapter, the techniques used at the laboratory scale and industrial scale for the production of nanocrystals will be presented, divided in bottom-up, top-down, and combined technologies. The physicochemical and technological methods for the characterization of nanocrystals will be considered as an essential tool in the drug product development. An overview of the nanocrystals on the market and under development will be also presented.I documenti in IRIS sono protetti da copyright e tutti i diritti sono riservati, salvo diversa indicazione.
