Lipid nanocapsules, preparation process and use as medicine

Abstract

The invention concerns nanocapsules, in particular with an average size less than 50 nm, consisting of an essentially lipid core liquid or semiliquid at room temperature, coated with an essentially lipid film solid at room temperature having a thickness of 2-10 nm. The invention also concerns a method for preparing same which consists in producing a reverse phase of an aqueous emulsion brought about by several temperature raising and lowering cycles. Said lipid nanocapsules are particularly designed for producing a medicine.

1 .- 21 . (canceled) 
   
   
       22 . Nanocapsules with an average size of less than 150 nm, consisting of a core that is liquid or semi-liquid at room temperature, and a film coating that is solid at room temperature coating said core, wherein:
 said film consists essentially of a lecithin and contains a PEG-hydroxystearate,   said core consists essentially of a fatty substance that is liquid or semi-liquid at room temperature and contains a pharmaceutically active principle.   
   
   
       23 . The lipid nanocapsules as claimed in  claim 22 , wherein the average size is less than 100 nm. 
   
   
       24 . The lipid nanocapsules as claimed in  claim 23 , wherein the average size is less than 50 nm. 
   
   
       25 . The lipid nanocapsules as claimed in  claim 22 , wherein the thickness of the solid film is between 2 and 10 nm. 
   
   
       26 . The nanocapsules as claimed in  claim 22 , wherein the fatty substance is a triglyceride or a fatty acid ester. 
   
   
       27 . The nanocapsules as claimed in  claim 26 , wherein the fatty substance represents 20% to 60% by weight of the nanocapsules. 
   
   
       28 . The nanocapsules as claimed in  claim 27 , wherein the fatty substance represents 25% to 50% by weight of the nanocapsules. 
   
   
       29 . The lipid nanocapsules as claimed in  claim 26 , wherein the triglyceride constituting the core of the nanocapsules is chosen from C 8  to C 12  triglycerides and mixtures thereof. 
   
   
       30 . The lipid nanocapsules as claimed in  claim 29 , wherein the C 8  to C 12  triglycerides are capric or caprylic acid triglycerides. 
   
   
       31 . The lipid nanocapsules as claimed in  claim 28 , wherein the fatty acid ester constituting the core of the nanocapsules is chosen from C 8  to C 18  fatty acid esters and mixtures thereof. 
   
   
       32 . The lipid nanocapsules as claimed in  claim 31 , wherein the C 8  to C 18  fatty acid esters are chosen from ethyl palmilate, ethyl oleate, ethyl myristate, isopropyl myristate and octyldodecyl myristate, and mixtures thereof. 
   
   
       33 . The lipid nanocapsules as claimed in  claim 31 , wherein the fatty acid ester is C 8  to C 12 . 
   
   
       34 . The nanocapsules as claimed in  claim 22 , wherein the lecithin has a phosphatidylcholine proportion between 40% and 90%. 
   
   
       35 . The nanocapsules as claimed in  claim 22 , wherein the PEG-hydroxystearate represents 2% to 10% by weight of the nanocapsules. 
   
   
       36 . The nanocapsules as claimed in  claim 22 , wherein the PEG-hydroxystearate is polyethylene glycol-660 2-hydroxystearate. 
   
   
       37 . The nanocapsules as claimed in  claim 22 , wherein the lecithin is soybean lecithin. 
   
   
       38 . The nanocapsules as claimed in  claim 37 , characterized in that the soybean lecithin is Lipoid S75-3®. 
   
   
       39 . A method of administering a pharmaceutically active agent, comprising administering orally the nanocapsule of  claim 22  to a subject in need thereof. 
   
   
       40 . A pharmaceutical composition for oral administration, comprising the nanocapsule of  claim 22 .