Drug nanocrystals: a state of the art formulation strategy for preparing the poorly water-soluble drugs

Erxi Che; Xin Zheng; Changshan Sun; Di Chang; Tongying Jiang; Siling Wang
February 2012
Asian Journal of Pharmaceutical Sciences;2012, Vol. 7 Issue 1, p85
Academic Journal
Nowadays, many drugs are abandoned early in discovery due to extremely low solubility both in aqueous and non-aqueous solvent which is a bottleneck in pharmaceutical industry. As traditional formulation strategies fail to solve the intractable issue, there comes to drug nanoscrystals regarded as universal, simple and industrially feasible. It includes buttom-up (anti-solvent precipitation, supercritical fluid process, spray-drying), top-down production strategies (pearl milling, high pressure homogenization, combination technologies), and the latest second generation nanocrystals technologies. In this mini review, the fundamental mechanisms for bioavailability enhancement of the hydrophobic molecules are presented. Related physical instabilities (sedimentation, agglomeration, crystal growth, and crystalline state conversion) and the methods to alleviate or tackle the stability problems are discussed. Particle size, size distribution, morphology, particle surface charge, and crystalline state are critical characteristics to determine the quality of the final nanocrystals products. Here, attention has been paid to the pros and cons of particular drug nanocrystals strategies, corresponding process parameters and patented techniques are summarized. Oral and parenteral administrations are two main applications of drug nanocrystals strategy. However, other administration routes are introduced as well, i.e. pulmonary and ocular deliveries which also show potential and promise for delivery of poorly-water soluble drugs.


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