Modified Microparticles of Calcium Alginate Gel for Controlled Release of Anesthetics

Abstract

ABSTRACTThe aim of this work is the development of controlled delivery system immobilized by local anesthetics on the basis of modified microparticles of calcium alginate gels. The kazkain, rikhlokain, lidokain and novokain were used as local anesthetics. Modified microparticles were obtained by syringed dropwise a solution of ansthetics in sodium alginate into solution of polymers such as chitosan or polyethyleneimine in calcium chloride. The obtained modified alginate microparticles were contained immobilized anesthetics in core of particles and a surface layer of polymer. Effects of polymer concentration and exposure duration on the thickness of polymer coating were determined. The release of anesthetics from the modified alginate gel particles into a physiological solution with different thickness of coating were studied. All the release data show the typical pattern for a matrix controlled mechanism. The cumulative amount of drug released from alginate gels was linearly related to the square root of the time and the release rate decreased this time. The process is controlled by the diffusion of anesthetics through the polymeric coating. The data shown a possibility of the regulation of the rate of anesthetics release from the modified alginate particles by way of alternation of thickness of the polymer coating. The anesthetic effect of the alginate microparticles containing drugs was tested on rats by method “tail flick” according two criteria: full analgesia – the absence of reaction on pain and sufficient analgesia – exceeding of pain threshold sensibility two and more times. Medical-biological tests show that the duration of anesthetic activity for the drug-containing alginate beads increases at 5-8 times in comparison of free drugs.