Novel microemulsion and micelle systems for solubilizing drugs

Abstract

A microemulsion delivery system for water insoluble or sparingly water soluble drugs that comprises a long polymer chain surfactant component and a short fatty acid surfactant component, with the amount of each being selected to provide stable microemulsion or micellar systems.

1 - 24 . Cancelled  
     
     
         25 . A microemulsion composition for intravenous delivery comprising an oil phase and an aqueous phase, wherein the oil phase comprises: 
 an oil-soluble drug;    a long chain polymer surfactant component; and    a short chain fatty acid surfactant component;    and wherein the amounts of the long chain polymer and short chain fatty acid surfactant components are selected to provide for spontaneous formation of thermodynamically stable microemulsion droplets of the oil phase having a particle size from 10 nm to 100 nm.    
     
     
         26 . The composition of  claim 25 , wherein the oil-soluble drug is a solid.  
     
     
         27 . The composition of  claim 26 , wherein the long chain polymer surfactant component is selected from the group consisting of polyoxyethylene alkyl esters, polyoxyethylene glycols, polyvinylpyrrolidone, polyvinylalcohol, tyloxapol, and poloxamer.  
     
     
         28 . The composition of  claim 27 , wherein the long chain polymer surfactant component is a poloxamer.  
     
     
         29 . The composition of  claim 26 , wherein the short chain fatty acid surfactant component is a C 8  to C 16  component.  
     
     
         30 . The composition of  claim 29 , wherein the short chain fatty acid surfactant component is a C 8  to C 12  component.  
     
     
         31 . The composition of  claim 26 , wherein the long chain polymer surfactant component is a poloxamer and the short chain fatty acid surfactant component is a laurate.  
     
     
         32 . The composition of  claim 26 , wherein the total amount of long chain polymer surfactant component and short chain fatty acid surfactant component does not exceed 4.65% by weight.  
     
     
         33 . The composition of  claim 26 , wherein the interfacial tension of the oil-soluble drug with an emulsifier combination comprising the long chain polymer surfactant component and the short chain fatty acid surfactant component is less than 0.1 dynes per cm.  
     
     
         34 . The composition of  claim 26 , wherein the oil-soluble drug is selected from the group consisting of analgesics, anesthetics, antibiotics, antidepressants, antidiabetics, antifungals, antihypertensives, anti-inflammatories, antineoplastics, immunosuppressives, sedatives, antianginals, antipsychotics, antimanics, antiarthritics, antigouts, anticoagulants, antithrombolytics, anticonvulsants, antiparkinsons, antibacterials, antivirals, and anti-infectives.  
     
     
         35 . The composition of  claim 34 , wherein the oil-soluble drug is an anesthetic.  
     
     
         36 . The composition of  claim 35 , wherein the oil-soluble drug is an aryl containing molecule.  
     
     
         37 . The composition of  claim 25 , wherein the oil-soluble drug is an oil-soluble vitamin.  
     
     
         38 . The composition of  claim 26 , wherein the long chain polymer surfactant component and the short chain fatty acid surfactant component are selected from the GRAS list.  
     
     
         39 . The composition of  claim 26 , wherein the ratio of long chain polymer surfactant component to short chain fatty acid surfactant component is from 10:100 to 25:80 wt/wt.  
     
     
         40 . The composition of  claim 26 , wherein the long chain polymer surfactant component has a molecular weight greater than 1000, and the short chain fatty acid surfactant component has a molecular weight less than 1000.  
     
     
         41 . The composition of  claim 39 , wherein the amount of oil-soluble drug is from 0.1% to 1.0%.  
     
     
         42 . The composition of  claim 26 , wherein the oil-soluble drug is a mixture of the base form and the salt form of the drug.  
     
     
         43 . The composition of  claim 26 , wherein the drug transfer rate is controlled by control of the character and nature of micelle formation of the microemulsion droplets.  
     
     
         44 . A method of controlling intravenous drug delivery and transfer rate of an oil-soluble drug comprising: 
 administering a composition comprising microdroplets of the oil-soluble drug and an emulsifier combination comprising a long chain polymer surfactant component and a short chain fatty acid surfactant component, the amounts of each component being selected to provide for spontaneous formation of thermodynamically stable microemulsion droplets having a particle size from 10 nm to 100 nm and to control intravenous delivery and transfer rate as desired.    
     
     
         45 . A microemulsion composition for drug delivery comprising an oil phase and an aqueous phase, wherein the oil phase comprises: 
 an oil-soluble drug; and    an emulsifier combination comprising a long chain polymer surfactant component and a short chain fatty acid surfactant component;    and wherein the amounts of the long chain polymer surfactant component and the short chain fatty acid surfactant component are selected to provide for spontaneous formation of thermodynamically stable microemulsion droplets of the oil phase having a particle size from 10 nm to 100 nm and wherein the interfacial tension of the oil-soluble drug with the emulsifier combination is less than 0.1 dynes per cm.    
     
     
         46 . The method of  claim 44 , wherein the oil-soluble drug is a solid.  
     
     
         47 . The microemulsion composition of  claim 25  comprising at least two oil-soluble drugs.