Nanosuspensions as particulate drug formulations in therapy: Rationale for development and what we can expect for the future

Nanosizing: a formulation approach for poorly-water-soluble compounds.

The present invention relates to imidazo[1,2-a]pyrimidine derivatives, that are useful for treating cellular proliferative diseases, for treating disorders associated with MET activity, and for inhibiting the receptor tyrosine kinase MET. The invention also related to compositions which comprise these compounds, and methods of using them to treat cancer in mammals.

Tyrosine kinase inhibitors

Methods are provided for inhibiting stenosis following vascular trauma or disease in a mammalian host, comprising administering to the host a therapeutically effective dosage of a therapeutic conjugate containing a vascular smooth muscle binding protein that associates in a specific manner with a cell surface of the vascular smooth muscle cell, coupled to a therapeutic agent dosage form that inhibits a cellular activity of the muscle cell. Methods are also provided for the direct and/or targeted delivery of therapeutic agents to vascular smooth muscle cells that cause a dilation and fixation of the vascular lumen by inhibiting smooth muscle cell contraction, thereby constituting a biological stent.

Therapeutic inhibitor of vascular smooth muscle cells

Nanosuspensions have emerged as a promising strategy for the efficient delivery of hydrophobic drugs because of their versatile features and unique advantages. Techniques such as media milling and high-pressure homogenization have been used commercially for producing nanosuspensions. Recently, the engineering of nanosuspensions employing emulsions and microemulsions as templates has been addressed in the literature. The unique features of nanosuspensions have enabled their use in various dosage forms, including specialized delivery systems such as mucoadhesive hydrogels. Rapid strides have been made in the delivery of nanosuspensions by parenteral, peroral, ocular and pulmonary routes. Currently, efforts are being directed to extending their applications in site-specific drug delivery.

http://depa.fquim.unam.mx/amyd/archivero/Nanosuspensiones_5211.pdf

Nanosuspensions: a promising drug delivery strategy.

Dispersible particles consisting essentially of a crystalline drug substance having a surface modifier adsorbed on the surface thereof in an amount sufficient to maintain an effective average particle size of less than about 400 nm, methods for the preparation of such particles and dispersions containing the particles. Pharmaceutical compositions containing the particles exhibit unexpected bioavailability and are useful in methods of treating mammals.

Surface modified drug nanoparticles

An X-ray contrast composition comprising particles consisting essentially of a non-radioactive crystalline organic x-ray contrast agent having a surface modifier adsorbed on the surface thereof in an amount sufficient to maintain an effective average particle size of less than 400 nm, and a pharmaceutically acceptable carrier therefor is useful in x-ray diagnostic medical imaging methods. The agents can be delivered to a specific tissue or fluid site, for example, the blood pool, liver or spleen. In one embodiment involving intravenous administration, preferred compositions provide effective imaging of the blood pool for remarkably long times.

X-ray contrast compositions useful in medical imaging

PURPOSE: To obtain medicine particles having a particle size of submicron CONSTITUTION: The medicine particles having an effective average particle size of less than about 400nm is provided by dispersing a medicine and a hard grinding vehicle in a liquid dispersion medium and subsequently wet-grinding the medicine The application of a surface-modifying agent during or after the wet-grinding treatment enables the adsorption of the modifying agent to the surfaces of the particles The particles form stable dispersions, and are useful for preparing pharmaceutical preparations high in bioefficiency

Liversidge Gary G

Papers

Surface modified drug nanoparticles

X-ray contrast compositions useful in medical imaging

Surface-modified drug particle

Oberflächenmodifizierte Arzneimittel-Nanopartikel

Medicinal substance particles, method of their preparing, stable dispersion, agent containing medicinal substance as particles