Curcumin solid lipid particles and methods for their preparation and use

Abstract

Solid lipid particles comprising a lipid hydrophobic matrix and from about 5 wt. % to about 30 wt. % of curcumin, and methods of making and treatment thereof.

1 . Solid lipid particles comprising: a lipid hydrophobic matrix; and from about 5 wt. % to about 30 wt. % of curcumin, wherein said lipid hydrophobic matrix is substantially free of water and wherein said solid lipid particles have an average particle size diameter ranging from 100 μm to 1500 μm. 
     
     
         2 . The solid lipid particles according to  claim 1 , wherein the lipid hydrophobic matrix has a melting point ranging from about 15° C. to about 85° C. 
     
     
         3 . The solid lipid particles according to  claim 1 , wherein the lipid hydrophobic matrix has a melting point ranging from about 30° C. to about 45° C. 
     
     
         4 . The solid lipid particles according to  claim 1 , wherein the lipid hydrophobic matrix optionally contains at least one surfactant. 
     
     
         5 . The solid lipid particles according to  claim 1 , wherein the curcumin has an average particle size diameter ranging from about 0.1 μm to about 10 μm. 
     
     
         6 . (canceled) 
     
     
         7 . The solid lipid particles according to  claim 1 , wherein the solid lipid particles have a substantially spherical shape. 
     
     
         8 . The solid lipid particles according to  claim 1 , wherein the lipid hydrophobic matrix comprises at least one of:
 a mixture of monoglycerides, diglycerides, and triglycerides having a carbon number ranging from C 6  to C 40 ,   esters of fatty acids having a carbon number ranging from C 6  to C 12  with ethylene glycol or propylene glycol;   a mixture of triglyceridies having medium chain length; or   a mixture of glycerides having a carbon number ranging from C 18  to C 24 .   
     
     
         9 . The solid lipid particles according to  claim 1 , wherein the lipid hydrophobic matrix comprises a mixture of a wax and at least one non-neutralized fatty acid. 
     
     
         10 . A process for preparing solid lipid particles according to  claim 1 , wherein the process comprises:
 dispersing a lipid phase having a melting point ranging from about 15° C. to about 85° C. in a gel phase at a temperature above the melting point of the lipid phase to form a dispersion;   cooling the dispersion to obtain solid lipid particles;   separating the solid lipid particles; and   optionally, washing the solid lipid particles;   wherein the solid lipid particles comprise a lipid hydrophobic matrix; and from about 5 wt. % to about 30 wt. % of curcumin.   
     
     
         11 . The process according to  claim 9 , wherein the solid lipid particle further comprise surfactant. 
     
     
         12 . A pharmaceutical composition comprising one or more solid lipid particles according to  claim 9 . 
     
     
         13 . A solid lipid particle according to  claim 1 , comprising
 about 5 wt. % to about 15 wt. % curcumin   about 5 wt. % to about 30 wt. % lecithin, preferably 10 to 15 wt %, and more preferably   about 15 wt. %; about 5 wt. % to about 15 wt. % glycerol behenate, preferably about 5 wt %;   and at least about 40 wt. % mixture of monoglycerides, diglycerides, and triglycerides having a carbon number ranging from C 6  to C 40 , preferably about 50 wt %, or about 65 wt %.   
     
     
         14 . The solid lipid particle of  claim 13  comprising
 about 15 wt. % curcumin 
 about 15 wt. % lecithin; 
 about 5 wt. % glycerol behenate; and 
 about 65 wt. % mixture of monoglycerides, diglycerides, and triglycerides having a carbon number ranging from C 6  to C 40 . 
 
     
     
         15 . (canceled) 
     
     
         16 . The solid lipid particle of  claim 1  comprising
 15 wt. % curcumin 
 20 wt. % propylene glycol monocaprylate, 
 10 wt. % propylene glycol dicaprylate/dicaprate, 
 5 wt. % glycerol behenate, and 
 50 wt. % a mixture of monoglycerides, diglycerides, and triglycerides having a carbon number ranging from C 6  to C 40 . 
 
     
     
         17 . The solid lipid particle of  claim 15  comprising:
 15 wt. % curcumin wherein the curcumin has an average particle size diameter from about 0.1 μm to about 10 μm; 
 20 wt. % propylene glycol caprylate; 
 10 wt. % propylene glycol dicaprylate/dicaprate; 
 5 wt. % glycerol behenate, and 
 50 wt. % a mixture of monoglycerides, diglycerides, and triglycerides having a carbon number ranging from C 6  to C 40 . 
 
     
     
         18 . A solid lipid particle according to  claim 1 , wherein the curcumin is comprised in an amount of from 5% wt to 15% wt and wherein said solid lipid particle comprises:
 5% wt to 30% wt propylene glycol monocaprylate,   5% wt to 30% wt propylene glycol dicaprylate/dicaprate,   5% wt to 15% wt glycerol behenate,   and at least 40% wt a mixture of monoglycerides, diglicerides, and triglicerides having a carbon number ranging from C6 to C40.