COVALENT ANESTHETIC-POLYMER CONJUGATES FOR PROLONGED LOCAL ANESTHESIA

Abstract: anesthetics covalently conjugated onto biodegradable and biocompatible hydrophilic polymers via hydrolysable linkages provide controlled release of local anesthetics in vivo in an effective amount for nerve blockade with reduced toxicity relative to the unconjugated anesthetic agent. the rate of anesthetic release can be tuned by changing the hydrophilicity of the polymer. exemplary formulations of poly (glycerol sebacate) (pgs), optionally including poly ethylene glycol (peg) polymers conjugated to tetrodotoxin (ttx) (pgs-peg-ttx and pgs-ttx), and methods of use thereof are provided nerve blockade from pgs-peg-ttx and pgs-ttx was associated with minimal systemic and local toxicity to the muscle and the peripheral nerves. tdp-ttx conjugates homogeneously dispersed into peg200 are also described. peg200 not only worked as a medium, but also worked as a chemical permeation enhancer (cpe) to enhance the effectiveness of ttx.

Inventor(s): Daniel S. Kohane, Chao Zhao

CPC Classification: A61K47/60 (PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES (devices or methods specially adapted for bringing pharmaceutical products into particular physical or administering forms ; chemical aspects of, or use of materials for deodorisation of air, for disinfection or sterilisation, or for bandages, dressings, absorbent pads or surgical articles ; soap compositions ))

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