Micronized Hydrophobic Agents/Drugs for Superior Performance Medical and Otherwise (Case 1429)

Principal Investigator:

 

Edith Mathiowitz, PhD, Professor

Department of Bio Med Molecular Pharmacology, Physiology & Biotechnology

Brown University

Providence, RI

 

Brief Description:

 

Many hydrophobic agents, active and non-active, have utility in a variety of in vivo settings – medical and otherwise.  Although techniques exist for preparing and formulating hydrophobic agents, current state-of-the-art is limited.  Some conventional formulation methods cause a loss of bioactivity, while others produce relatively large drug particles or particles of inconsistent sizes that lead to drug delivery problems. 

 

One formulation method is the generation of microstructures (microparticles, microcapsules, microspheres); all have important applications as delivery vehicles in many industries, i.e., pharmaceutical, agricultural, textile and cosmetics.  As such, a drug, catalyst, gas, salt, fertilizer, fuel, dye, fragrance or any number of other hydrophobic agents is encapsulated in a polymer matrix and delivered, either instantaneously or in a controlled manner, to a site in response to an external influence such as pH, heat, radiation, pressure, etc.  Microencapsulation techniques exist that can produce a variety of particle types and sizes under various conditions, and microparticle size is often an important factor in determining the release rate of an encapsulated material.  Moreover, physical and chemical properties (e.g., hydrophobicity, molecular weight, chemical/thermal stability, etc.) of the materials and agents employed affect encapsulation, and thus determine the appropriate encapsulation method for a given application.  These multi-step microencapsulation methods often result in significant losses and typically involve solidifying emulsified liquid polymer droplets by changing temperature, evaporating solvent, or adding chemical cross-linking agents.  With bioactive agents, these properties and parameters can be particularly important in the encapsulation process, as loss in bioactivity resulting from processing steps and/or low yields can determine efficacy, effectiveness and overall performance of a drug or treatment. 

 

An improved formulation process is needed for easier and more effective preparation of hydrophobic agents/drugs to achieve enhanced micro-encapsulation and successful targeted drug delivery, which has important medical, performance, and financial implications.

 

The technology is a new method, with associated compositions/products, for micronizing hydrophobic agents or drugs using a set of solvents and solutions.  The micronized hydrophobic agents/drugs have enhanced properties and dramatic advantages over non-micronized in encapsulated delivery.  These include: reduced particle size (less than 1 micron); increased crystallinity (over 95% possible) for improved release; and significantly enhanced bioactivity and relative bioavailability (100%) when administered to an individual.  Also, the final preparation can contain less than 5%, or no, polymer carrier and be free of surfactant.

 

The innovative micronization process is flexible and conditions, steps and solvents can be easily modified and substitutions made depending on the hydrophobic drug/agent involved.  Note that micronized drugs may be administered directly or further manipulated pharmacologically, e.g., encapsulated as microparticles, as mentioned.  Microparticles for the encapsulation of the micronized hydrophobic agent may be prepared from a wide variety of polymers (biodegradable, non-biodegradable, bioadhesive) and by different methods (e.g., hot melt encapsulation, spray drying, solvent evaporation microencapsulation, PIN, among others).  A wide range of non-active hydrophobic agents can be micronized including, but not limited to: adhesives, gases, pesticides/herbicides/biocides, fragrances/flavors, antifoulants, dies/inks/pigments, salts, oils/fuels, cosmetics, catalysts, detergents, curing agents, foods, metals, paints, photographic agents, plasticizers, propellants, and the like.  While, bioactive hydrophobic agents include, among a plethora of others: adrenergic agent, steroid, amino acid, hormone, antibiotic, protein, etc.  Finally, micronized hydrophobic drugs can be administered in several forms/preparations, through conventional routes, mixed with pharmaceutically-acceptable excipients, buffers, and other additives, and can be administered as is or as a pharmaceutical salt.

 

Applications are numerous, in a plethora of markets.  Examples of applications include: drug manufacturing and delivery; agricultural soil/crop protection; food and beverage grade additives – flavor/color enhancement, curing agents, or antifoulants; cosmetics and other personal consumer product additives – fragrance, pigments, detergents, antifoulants or topical treatment; building/construction products and supplies for painting, curing, cleaning, binding; and/or wherever hydrophobic agents are used.  Markets also are extensive, and examples include:  pharmaceutical – therapeutic, diagnostic, and medical devices (drug delivery); agricultural/environmental – diagnostics/testing/treatment; food and beverage; fuels; plastics; industrial chemical/process catalysts; building/construction/industrial products and supplies, among others.

 

Information:

 

US patent 8,524,829 is issued (09/03/2013)

US patent 6,746,635 is issued (06/08/2004)

Canada patent 2,456,806 is issued (10/18/2011)

 

Patent Information:
For Information, Contact:
Margaret Shabashevich,
Manager of Operations
Technology Ventures Office
Brown University
401-863-7499 TVO_Patents@brown.edu
Inventors:
Edith Mathiowitz
Keywords:
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