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An Iowa State University researcher has developed a method for preparing nanoparticles that may enable microencapsulation of drugs for site-specific drug delivery.

Entrapment and subsequent rapid release of mock hydrophobic drugs has been shown experimentally, and ISU is seeking partners interested in commercializing this technology

Many potential drug candidates identified through high through-put screening have limited water solubility and thus are not advanced further in the drug development process.  Surfactant micelles can be used to solublize hydrophic agents in water; however, their utility for drug delivery is limited by the requirement for high critical micelle concentration (CMC), low thermodynamic stability, and because micelle assembly is highly variable.  Polymeric micelles have several advantages over surfactant micelles, including the tendency to aggregate at much lower concentrations, better thermodynamic stability and the ability to entrap or covalently attach a drug or other cargo with subsequent controlled release.  Unfortunately, physically trapped drugs can leak out the micelles prematurely but covalent attachment between the drug and delivery vessel places severe limits on their structures and also adds complexity to the formulation and production of the ultimate therapeutic package. To overcome these drawbacks, an ISU researcher has developed a method for simple preparation of nanoparticles for biomedical and chemical applications.  This method produces surface-crosslinked micelles (SCMs) that have numerous residual alkynes on the surface; multivalent modification can be accomplished easily by adding azide-functionalized polymers or ligands after crosslinking through “click” chemistry. The surface charge may be simply tuned by the cross-linked surfactants or through post-modification. The SCMs have been shown experimentally to be able to release entrapped cargo very rapidly and may have utility for drug delivery and other biomedical and chemical applications.

• Economical (production of the nanoparticles does not require iterative synthesis or rare metals)

• Simple (surface-functionalization is carried out in one-pot after crosslinking)

• Versatile (synthesis method is applicable to micelles, organic or inorganic nanoparticles, liposomes, globular or rod-like reversed micelles)

• Controllable (stimuli-triggered release can be engineered into the particles)

Drug delivery; controlled release; multivalent ligand design; solubilization