Chitosan beads and filler comprising such beads

Abstract

The present invention pertains to chitosan beads consisting of chitosan cross-linked with citrate ions. The present invention furthermore pertains to a filler comprising such chitosan-citrate beads. In one embodiment of the instant invention the filler is a dermal filler. In one further embodiment of the present invention the dermal filler is for the treatment of wrinkles and/or folds. In another embodiment of the instant invention the filler is for use in the treatment of a medical condition. The filler provided in the present invention may further comprise one or more active pharmaceutical ingredients. Further, the present invention pertains to a process for preparing the filler as claimed herein.

1 . A dermal filler comprising chitosan beads and an anesthetic agent, wherein the chitosan beads consist essentially of chitosan and citrate ions, wherein the chitosan has an average molecular weight of from about 50 kD to about 5000 kD and is deacetylated to a degree of from about 70% to about 100%, wherein the chitosan beads exhibit a mass median diameter of less than or equal to 1500 μm as determined by microscopical analysis. 
     
     
         2 . The dermal filler of  claim 1 , wherein the mass median diameter of the chitosan beads remains less than or equal to 1500 μm for a period of 6 months at 25° C.±2° C. and 60%±5% relative humidity as determined by laser diffraction analysis. 
     
     
         3 . The dermal filler of  claim 1 , wherein the chitosan beads have a shelf-life of 6 months at 25° C.±2° C. and 60%±5% relative humidity. 
     
     
         4 . The dermal filler of  claim 1 , further comprising at least one polysaccharide. 
     
     
         5 . The dermal filler of  claim 4 , wherein the polysaccharide is hyaluronic acid or a salt thereof. 
     
     
         6 . The dermal filler of  claim 1 , wherein the anesthetic agent is selected from procaine benzocaine, chloroprocaine, cocaine, cyclomethycaine, dimethodcaine, larocaine, propoxycaine, proparacaine, tretracaine, lidocaine, articaine, bupivacaine, carticaine, cinchocaine, etidocaine, levobupivacaine, mepivacaine, peperocaine, prilocaine, ropivacaine, and trimecaine. 
     
     
         7 . The dermal filler of  claim 1 , wherein the anesthetic agent is present in the dermal filler at a concentration from about 0.01% to 6% weight % (w/w %) based on the total weight of the composition. 
     
     
         8 . The dermal filler of  claim 1 , further comprising pharmaceutically acceptable isotonicity agents or preservatives. 
     
     
         9 . The dermal filler of  claim 1 , further comprising pharmaceutically acceptable exicipents selected from antioxidants, viscosity enhancers/modifiers, hydrating agents, bulking substances, tonicity agents, preservatives and surface active agents, or a mixture thereof. 
     
     
         10 . The dermal filler of  claim 1 , wherein the chitosan beads are present in the dermal filler in an amount effective for the treatment of wrinkles and/or folds. 
     
     
         11 . The dermal filler of  claim 1 , wherein the chitosan beads are present in the dermal filler in an amount effective for the treatment of frown lines, glabellar lines, nasal furrows, cheek wrinkles, crow's feet and perioral wrinkles, nasolabial folds, lip augmentation, forehead wrinkles, mild to moderate nasal furrows and acne scars. 
     
     
         12 . The dermal filler of  claim 1 , wherein the chitosan beads are present in the dermal filler in an amount effective for filling a lip in lip augmentation. 
     
     
         13 . The dermal filler of  claim 1 , wherein the chitosan beads are present in the dermal filler at a concentration from about 10% (v/v) to about 95% (v/v) to the total volume of the filler. 
     
     
         14 . The dermal filler of  claim 1 , wherein the chitosan beads are present in the filler at a concentration from about 25% (v/v) to about 95% (v/v) to the total volume of the filler. 
     
     
         15 . The dermal filler of  claim 1 , wherein the chitosan beads are present in the filler at a concentration from about 50% (v/v) to about 95% (v/v) to the total volume of the filler. 
     
     
         16 . The dermal filler of  claim 1 , wherein the chitosan beads are present in the filler at a concentration from about 75% (v/v) to about 95% (v/v) to the total volume of the filler. 
     
     
         17 . The dermal filler of  claim 1 , wherein the chitosan beads are present in the filler at a concentration from about 85% (v/v) to about 90% (v/v) to the total volume of the filler. 
     
     
         18 . The dermal filler of  claim 1 , wherein the dermal filler has a shelf-life of 6 months at 25° C.±2° C. and 60%±5% relative humidity.