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Review
. 2008;3(3):295-309.
doi: 10.2147/ijn.s595.

Nanocrystal technology, drug delivery and clinical applications

Affiliations
Review

Nanocrystal technology, drug delivery and clinical applications

Jens-Uwe A H Junghanns et al. Int J Nanomedicine. 2008.

Abstract

Nanotechnology will affect our lives tremendously over the next decade in very different fields, including medicine and pharmacy. Transfer of materials into the nanodimension changes their physical properties which were used in pharmaceutics to develop a new innovative formulation principle for poorly soluble drugs: the drug nanocrystals. The drug nanocrystals do not belong to the future; the first products are already on the market. The industrially relevant production technologies, pearl milling and high pressure homogenization, are reviewed. The physics behind the drug nanocrystals and changes of their physical properties are discussed. The marketed products are presented and the special physical effects ofnanocrystals explained which are utilized in each market product. Examples of products in the development pipelines (clinical phases) are presented and the benefits for in vivo administration of drug nanocrystals are summarized in an overview.

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Figures

Figure 1
Figure 1
Surface enlargement and increase in number of crystals by particle size diminution. Used with permission from Junghanns (2006).
Figure 2
Figure 2
Comparison of a microcrystal (A) and a nanocrystal (B) and their surface curvature and concentration gradient over the diffusional distance (h). Abbreviations: cs, drug-saturated water at surface (M, microcrystal; N, nanocrystal); Cx, bulk concentration at diffusional distance; h, diffusional distance. dc/dt ~ (cs − cx)/h. Used with permission from Junghanns (2006).
Figure 3
Figure 3
Increasing dissolution pressure over a flat surface, a microparticle, and a nanoparticle. Abbreviations: p, dissolution pressure; a, flat surface; b, microparticle; c, nanoparticle. Used with permission from Junghanns (2006).
Figure 4
Figure 4
Increase in saturation solubility of BaSO4 in water as a function of the particle size calculated using the Kelvin equation. Used with permission from Anger (2005).
Figure 5
Figure 5
Basic principle of high pressure homogenization using a piston gap homogenizer. Used with permission from Junghanns (2006).
Figure 6
Figure 6
Scanning electron microscopic picture of a nanosuspension prepared with high pressure homogenization. Used with permission from Möschwitzer (2005).
Figure 7
Figure 7
Structural formula of sirolimus.
Figure 8
Figure 8
Packaging of Rapamune®.
Figure 9
Figure 9
Structural formula of aprepitant.
Figure 10
Figure 10
Packaging of Emend®.
Figure 11
Figure 11
Structural formula of fenofibrate.
Figure 12
Figure 12
Packaging of Tricor®.
Figure 13
Figure 13
Structural formula of megestrol acetate.
Figure 14
Figure 14
Packaging of Megace® ES.

References

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