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Background: Orally administered drugs that transverse the intestinal membrane must be very soluble and lipophilic. This may not be so as most drugs are poorly soluble and thus possess poor bioavailability resulting in only a small fraction of the administered drugs absorbed into the systemic circulation and reach the target site. Thus, a major amount of the drug is wasted and the unabsorbed drug leads to undesired side effects in the gastrointestinal tract.

Objectives: The objective is to review some of the various drug delivery technologies used to formulate poorly soluble drug candidates through nanotechnology.

Methods: Formulating these compounds as pure drug nanoparticles is one of the newer drug-delivery strategies applied to this class of molecules. Nanocrystals, a carrier-free colloidal delivery system in nano-sized range, is an interesting approach for poorly soluble drugs. Several strategies are applied for nanocrystals production including precipitation, milling, high pressure homogenization and combination methods such as Nano- EdgeTM, SmartCrystal and Precipitation-lyophilization-homogenization (PLH) technology.

Results: Nanoparticle dispersions are stable and have a mean diameter of less than 1 micron. Drug nanoparticles have been shown to improve bioavailability and enhance drug exposure for oral and parenteral dosage forms. Nanocrystals provide special features including enhancement of saturation solubility, dissolution velocity and adhesiveness to surface/cell membranes.

Conclusions: Many publications reported useful advantages of nanocrystals to improve in vivo performances such as pharmacokinetics, pharmacodynamics, safety and targeted delivery which are discussed in this review.

Keywords: Nanoparticles, Nanocrystal Technology, Bioavailability, poorly water soluble compounds.