Composition comprising hyaluronic acid and mepivacaine

Abstract

Compositions and methods for the surface appearance of the skin a subject are provided. An injectable composition comprising at least hyaluronic acid or a salt thereof; and an effective amount of at least mepivacaine or a salt thereof are provided. The hyaluronic acid optionally has an average molecular weight ranging from 50,000 to 10,000,000 Daltons, and may be crosslinked hyaluronic acids, non-crosslinked hyaluronic acids, or a combination, in some embodiments. The compositions and methods of the present invention are useful for treating and preventing the cutaneous signs of chronological aging and/or induced by external factors such as stress, air pollution, tobacco or prolonged exposure to ultraviolet (UV) exposure, impaired surface appearance of the skin, impaired viscoelastic or biomechanical properties of the skin, and/or the long-lasting filling of volume defects of the skin.

1 . A composition which is sterilized and injectable, the composition comprising an effective amount of:
 at least hyaluronic acid or a salt thereof; and   an effective amount of at least mepivacaine or a salt thereof as anesthetic agent,   wherein the hyaluronic acid is selected from the group consisting of crosslinked hyaluronic acids, non-crosslinked hyaluronic acids, and a mixture thereof.   
     
     
         2 . The composition according to  claim 1 , wherein the hyaluronic acid has an average molecular weight ranging from 50 000 to 10 000 000 Daltons. 
     
     
         3 . The composition according to  claim 1 , wherein the composition comprises from 0.1 to 5% by weight of hyaluronic acid relative to the total weight of the composition. 
     
     
         4 . The composition according to  claim 1 , wherein the hyaluronic acid is crosslinked with a degree of modification ranging from 0.1 to 20%. 
     
     
         5 . The composition according to  claim 1 , wherein the composition comprises from 0.01 to 5% by weight of anesthetic agent(s), based on the total weight of the composition. 
     
     
         6 . The composition according to  claim 1 , wherein the composition further comprises at least a balanced salt solution. 
     
     
         7 . The composition according to  claim 6 , wherein the balanced salt solution is a KH 2 PO 4 /K 2 HPO 4  saline buffer. 
     
     
         8 . The composition according to  claim 1 , wherein the composition further comprises at least one compound selected from the group consisting of an alpha-lipoic acid: N-acetyl-L-cysteine; reduced glutathion; amino acid such as L-Arginine, L-Isoleucine, L-leucine, monohydrated L-Lysine, Glycine, L-Valine, L-Threonine, L-Proline; pyridoxine hydrochloride; dehydrated zinc acetate; pentahydrates copper sulfate; and a mixture thereof. 
     
     
         9 . An injection device comprising a composition according to  claim 1 . 
     
     
         10 . The injection device according to  claim 9 , wherein the hyaluronic acid has an average molecular weight ranging from 50 000 to 10 000 000 Daltons. 
     
     
         11 . The injection device according to  claim 9 , wherein the hyaluronic acid is selected from the group consisting of crosslinked hyaluronic acids, non-crosslinked hyaluronic acids, and a mixture thereof. 
     
     
         12 . The injection device according to  claim 9 , wherein the composition comprises from 0.1 to 5% by weight of hyaluronic acid relative to the total weight of the composition. 
     
     
         13 . The injection device according to  claim 9 , wherein the hyaluronic acid is crosslinked with a degree of modification ranging from 0.1 to 20%. 
     
     
         14 . The injection device according to  claim 9 , wherein the composition comprises from 0.01 to 5% by weight of anesthetic agent(s), based on the total weight of the composition. 
     
     
         15 . The injection device according to  claim 9 , wherein the composition further comprises at least a balanced salt solution, preferably the balanced salt solution is a KH 2 PO 4 /K 2 HPO 4  saline buffer. 
     
     
         16 . The injection device according to  claim 9 , wherein said injection device is suitable for intraepidermal and/or intradermal and/or subcutaneous injection. 
     
     
         17 . The injection device according to  claim 9 , wherein said injection device is selected from a syringe, a set of microsyringes, a laser device, a hydraulic device, an injection gun, a needleless injection device, a rolling with microneedles. 
     
     
         18 . The injection device according to  claim 9 , wherein said injection device adapted to the technique of mesotherapy. 
     
     
         19 . The injection device according to  claim 9 , wherein said injection device comprises a hypodermic needle or cannula. 
     
     
         20 . The injection device according to  claim 9 , wherein the needle or the cannula has a diameter ranging between 18 and 34 G and a length varying from 4 to 70 mm. 
     
     
         21 . A method for preparing a composition as recited in  claim 1  which comprises the step of:
 (a) providing at least one gel of hyaluronic acid or a salt thereof, wherein the hyaluronic acid is selected from the group consisting of crosslinked hyaluronic acids, non-crosslinked hyaluronic acids, and a mixture thereof, 
 (b) adding to said gel of hyaluronic acid at least mepivacaine or a salt thereof as anesthetic agent, 
 (c) sterilizing the mixture obtained in step (b).