Novel complexes comprising collagen peptides and curcuminoids and compositions thereof

Abstract

Formulations comprising complexes of peptides with hydrophobic bioactive molecules are described herein. The invention more specifically relates to collagen peptide and curcuminoid complexes and compositions comprising the complexes. The compositions and formulations comprising the protein hydrolysate peptide-hydrophobic bioactive molecule complexes are water-soluble, stable at physiological and acidic pH, synergistically enhance the systemic bioavailability of the biomolecules and peptides, and are capable of delivering a high therapeutically effective amount of the bioactive molecules via oral route. The compositions and formulations comprising the collagen peptide-curcuminoid complexes provide significantly high levels of bioavailable curcuminoids that are water soluble and stable at physiological and acidic pH along with significant anti-inflammatory effects offered by collagen peptides. The invention further provides a process for preparing the peptide-bioactive molecule complexes, compositions and oral formulations comprising the collagen peptide-curcuminoid complex.

1 . A water soluble pharmaceutical composition comprising:
 a) an effective amount of one or more hydrophobic bioactive molecules;   b) water-soluble peptides derived from protein hydrolysates; and   c) an emulsifying agent;   
       wherein the water soluble protein hydrolysate peptides form an amorphous, nano-sized non-covalent complex with the hydrophobic bioactive molecules. 
     
     
         2 . The pharmaceutical composition of  claim 1 , wherein the hydrophobic bioactive molecules are selected from the group consisting of curcuminoids, gingerol, flavonoids, stilbenes, carotenoids, saponins, terpenes, terpenoids, and chlorophyll. 
     
     
         3 . The pharmaceutical composition of  claim 1 , wherein the hydrophobic bioactive molecules are curcuminoids. 
     
     
         4 . The pharmaceutical composition of  claim 1 , wherein the hydrophobic bioactive molecules are present at a concentration in the range of 1 to 25% in the composition. 
     
     
         5 . The pharmaceutical composition of  claim 1 , wherein the peptides are present at a concentration in the range of 10 to 90% in the composition. 
     
     
         6 . The pharmaceutical composition of  claim 1 , wherein the protein hydrolysate peptides are 1000-5000 Da in size. 
     
     
         7 . The pharmaceutical composition of  claim 1 , wherein the emulsifier is selected from the group consisting of lecithin, polysorbate, propylene glycol, sorbitol, glycerol, polyglycerol esters, Quillaja extract, and sugar esters. 
     
     
         8 . The pharmaceutical composition of  claim 1 , wherein the protein hydrolysate peptides are collagen peptides. 
     
     
         9 . The pharmaceutical composition of  claim 1 , wherein the curcuminoids are complexed and encapsulated in the collagen peptide matrix. 
     
     
         10 . The pharmaceutical composition of  claim 1 , wherein the bioactive molecules comprising the composition exhibit enhanced solubility and stability as compared to unformulated bioactive molecules. 
     
     
         11 . The pharmaceutical composition of  claim 1 , wherein the bioactive molecules comprising the composition exhibit increased bioavailability, increased absorption and longer half-life of the bioactive molecules after oral administration to a subject, as compared to unformulated bioactive molecules. 
     
     
         12 . The pharmaceutical composition of  claim 1 , wherein the bioactive molecules comprising the composition exhibit increased cellular permeability, as compared to unformulated bioactive molecules. 
     
     
         13 . The pharmaceutical composition of  claim 1 , wherein it exhibits enhanced anti-inflammatory as compared to unformulated bioactive molecules. 
     
     
         14 . The pharmaceutical composition of  claim 1 , wherein it is orally administered either as capsules, tablets, softgels, beadlets, liquid solution, liquid suspension, liquid emulsion or as powder sachets for enhanced bioavailability of the bioactive molecules. 
     
     
         15 . The pharmaceutical composition of  claim 1 , wherein it is administered orally at a dose of 100 to 500 mg/dose in the form of tablets, capsules or softgel. 
     
     
         16 . The pharmaceutical composition of  claim 1 , wherein it is administered orally at a dose of 1000 mg to 5000 mg per sachet, once or twice a day, to deliver minimum 100 to 500 mg of bioactive molecules along with 1 to 10 g of peptides/dosage/day. 
     
     
         17 . The pharmaceutical composition of  claim 14 , wherein the collagen bioactive molecule complex is amorphous. 
     
     
         18 . A method of preparing water soluble pharmaceutical composition of  claim 1 , comprising the steps of:
 a. micronisation of curcuminoids followed by emulsification by homogenisation with an emulsifier;   b. dissolving collagen peptides in water at a concentration range of 20 to 95%;   c. complex formation of curcuminoids with the collagen peptide matrix by sonication with emulsified curcuminoids from step (a) with the dissolved collagen peptides from step (b)   d. encapsulation of the complex from step (c) by making sub-micron sized micelle suspension by ultrasound mediated homogenisation; and   e. drying the submicron sized micelles from step (d) by spray drying or freeze drying.   
     
     
         19 . The method of  claim 18 , wherein the emulsifier is selected from the group consisting of lecithin, polysorbate, propylene glycol, sorbitol, glycerol, polyglycerol esters, Quillaja extract, and sugar esters.