Formation of Nanostructured Particles of Poorly Water Soluble Drugs and Recovery by Mechanical Techniques

Nanotechnologies : Life Science Apps

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Inventors

  • Keith Johnston, Ph.D. , Chemical Engineering
  • Robert Williams III, Ph.D. , College of Pharmacy
  • Michal Matteucci , Chemical Engineering

Background/unmet need

In the pharmaceutical industry, most new chemical entities being developed are poorly water soluble. Although there are several routinely used processes in the pharmaceutical industry to reduce the particle size, each has its limitations. This innovative process can be used to produce nanoparticles and microparticles containing pharmaceutical drug substances that are insoluble or poorly soluble in water. This will enhance the solubility and rate of dissolution of the drug substance, and enhance its bioavailability.

In addition, this process can be used to produce agricultural chemicals. The chemical agents are typically poorly water soluble and therefore must be formulated in much higher concentrations for adequate activity. This process may enable incorporation of these agents at lower concentrations in the agricultural chemical product so that lower amounts would be required to produce the same effect.

Invention Description

UT Austin inventors have devised a new process for rapidly separating nanoparticles of chemicals (pharmaceuticals, agricultural chemicals, nutraceuticals) from an aqueous suspension or dispersion. The dried particles may then be redispersed in water or other polar solvents to their original size and morphological form (for example, amorphous or a specific crystalline structure).

The particle recovery process involves agglomerating the nanoparticles to a larger flocculate, in order to be rapidly separated by standard methods, such as filtration or centrifugation. After separation, the particles are able to achieve enhanced solubility equal to or better than an identical formulation isolated by conventional means, such as freeze-drying or spray-drying. The flocculated particles can exhibit slower release kinetics than the original nanoparticles, allowing controlled release of the chemical agent. In addition, the particles may be mixed with other excipients to make pharmaceutical dosage forms including tablets, gels and capsules.

Previous processes used spray-drying, evaporation, freeze-drying, or spray-freezing to isolate nanoparticles from suspension. These processes can have a detrimental impact on the morphology of the particles. For example, the addition of heat or solvent removal may cause growth in the primary particle size or crystallization of amorphous domains.

The invention is a process to control the aggregation of the nanoparticles with excipients and stabilizers. The unique aspect of this novel separation process is that it may be utilized without changing the morphology of the drug particles. The current invention is capable of producing much smaller particle sizes and more monodisperse particle size distributions, as well as polymorphs, which enhance aqueous solubility.

Benefits/Advantages

  • Effectively controls nanoparticle aggregation through the use of stabilizers
  • Does not require freezing
  • May be used without altering the drug particle morphology
  • Produces small, monodisperse particles

Market potential/applications

Nanotechnology, pharmaceutical, and agricultural companies interested in innovative nanoparticle formation techniques

Development Stage

Proof of concept