Nanoformulations containing encapsulted omega-3 fatty acids

Abstract

Disclosed is a method for making and using insoluble, biodegradable, nanoparticles containing the omega-3 fatty acids EPA and DHA in selected ratios. Tests show a surprising effect that the nanoformulation is twice as potent and at least five times more sustained leading to at least tenfold (2×5) higher bioavailability at equal dose (1% v/v).

1 . A process for making an aqueous suspension of a nanoparticles that comprise at least one omega-3 fatty acid oil encapsulated by a coating agent, wherein said omega-3 fatty acid oil comprises at least one of eicosapentaenoic acid (EPA) or docosahexaenoic acid (DHA), wherein said process comprises: impacting at least (a) a first microjet fluid stream comprising a mixture of EPA or DHA with a solvent for omega-fatty acid oils against (b) a second microjet fluid stream comprising water in a microreactor at a temperature and flow rate of each stream sufficient to produce turbulent mixing upon impact and produce said suspension of encapsulated EPA and DHA at an average particle size; wherein said fatty acid nanoparticles in the suspension have an average particle size within the range of 25-500 nm and that exhibit a polydispersity index (PDI) of less than 0.40. 
     
     
         2 . A process according to  claim 1  wherein said temperature is within a range of 25°-95° C. 
     
     
         3 . A process according to  claim 1  wherein the flow rate of the first stream and the second stream are each greater than 0.1 ml/min and impinge on each other at a relative speed of greater than 25 m/s. 
     
     
         4 . A process according to  claim 3  wherein the streams impinge at a relative speed within the range of 50-350 m/s with a Reynolds number of more than 100. 
     
     
         5 . A process according to  claim 4  wherein the first stream and second stream each having a driving pressure within the range of 0.5-100 bar through a nozzle. 
     
     
         6 . A process according to  claim 1  wherein the molar ratio of solvent to water is within the range of 0.1-100. 
     
     
         7 . A process according to  claim 1  wherein the at least one omega-3 fatty acid oil comprises a mixture of EPA and DHA at a weight ratio of EPA:DHA within the range of about 1:2 to about 10:1. 
     
     
         8 . A process according to  claim 1  wherein the fatty acid oil is a mixture of EPA and DHA having a higher concentration by weight of EPA than DHA; the coating agent comprises a gelatin, a gum derivative or a polymer; and the particulates further comprise one or more stabilizing agents or surfactants. 
     
     
         9 . A process according to  claim 1  wherein the coating agent comprises a chitosan, gelatin, gliadin, lectin-gliadin, methacrylic acid/ethylacrylate co-polymer, polypropylcyanoacrylate, polylactic co-glyconic acid (PLGA), sulfobutylated polyvinylalcohol-PLGA, lectin-PLGA, polyethyleneglycolpolylactic acid, polyethylenemethacrylate (PMMA), polymethylvinylether-co-maleic anhydride, polyethylene oxide-polyoxypropylene (PEO-POP), poly(N-isopropylacrylamide), poly(N-vinylacetamide), poly(t-butylmethacrylate), polycaprolactone (PCL), polystyrene, or hydroxypropylmethylcellulose phthalate. 
     
     
         10 . A process according to  claim 1  wherein the nanoparticle solids in suspension comprise an encapsulated fatty acid oil mixture that comprises 25-100% of at least one fatty acid chosen from eicosapentaenoic acid (EPA) and docosahexaenoic acid (DHA). 
     
     
         11 . A process according to  claim 1  wherein the fatty acid oil nanoparticles comprise a mixture of EPA and DHA, and further comprises at least one other fatty acid other than EPA and DHA in a form chosen from ethyl ester, triglyceride and free fatty acid. 
     
     
         12 . A process according to  claim 1  wherein said suspension is suitable for incorporation into a food, beverage, or consumable capsule.