Process and Apparatuses For Preparing Nanoparticle Compositions with Amphiphilic Copolymers and Their Use

Abstract

This invention discloses a process for making nanoparticles of amphiphilic copolymers by flash precipitation. Nanoparticles may be of amphiphilic copolymer alone or may contain an additive target molecule, preferably an organic active. The inclusion of additive target molecules in amphiphilic copolymer nanoparticles can alter their water solubility characteristics, fluid dynamics, and/or stability. Changing an additive target molecule's solubility and stability in a nanoparticle can make a water insoluble compound suitable for pharmaceutical administration as well as specifically target the molecule to a specific area of a patient's body. The process affords the production of nanoparticles at high absolute active content, at high yield, high productivity, and high processing rates while using unusually low amounts of amphiphilic copolymers. Furthermore, the resulting particles exhibit sufficient stability for post processing as desired. The invention also discloses two apparatuses for the production of nanoparticles of amphiphilic copolymers by flash precipitation.

1 - 103 . (canceled) 
     
     
         104 : A process to functionalize pre-existing particles by precipitation with at least one amphiphilic copolymer comprising:
 dispersing the pre-existing particles into a first solvent at a controlled temperature and pressure;   dissolving at least one amphiphilic copolymer in a second solvent capable of mixing with the first solvent; and   mixing the first and second solvents together at a mixing velocity sufficient to produce a surface functionalization of the pre-existing particles by selective precipitation of at least one amphilyte portion of at least one amphiphilic copolymer while at least one amphilyte portion of the same copolymer remains soluble.   
     
     
         105 : The process of  claim 104 , wherein the pre-existing particles are nanoparticles or microparticles. 
     
     
         106 : The process of  claim 104 , wherein the pre-existing particles and at least one amphiphilic copolymer are mixed in at least a 1:1 ratio by weight. 
     
     
         107 : The process of  claim 104 , wherein the average size of the pre-existing particles after functionalization is within 30% of the initial size. 
     
     
         108 : The process of  claim 104 , wherein the average initial size of the pre-existing particles is at least 2380 nm. 
     
     
         109 : The process of  claim 104 , wherein the average size of the pre-existing particles is less than 50 μm. 
     
     
         110 : The process of  claim 104 , wherein the pre-existing particles are comprised from molecules selected from the group consisting of biologically active compounds, organic active compounds, pharmaceutical organic actives, pharmaceutical precursors, anti-inflammatories, anti-depressants, anti-oxidants, proteins, and water insoluble vitamins. 
     
     
         111 : The process of  claim 104 , wherein the pre-existing particles are selected from the group consisting a ceramic, a latex, a glass, and a metal. 
     
     
         112 : The process of  claim 104 , wherein the pre-existing particles are selected from the group consisting an organic active compound, an agricultural active, an agricultural active precursor, a biocide, an herbicide, a pesticide, a fungicide, and an insecticide. 
     
     
         113 : The process of  claim 104 , wherein at least one amphiphilic copolymer has a total molecular weight of between about 1000 and 50,000 g/mole. 
     
     
         114 : The process of  claim 104 , wherein at least one amphiphilic copolymer exhibits a surface tension in water by no more than 50 dynes/cm at a concentration of 0.1 wt %. 
     
     
         115 : The process of  claim 104 , wherein at least one amphiphilic copolymer comprises a block, graft or random copolymer. 
     
     
         116 . (canceled)