Modified Microparticles of Calcium Alginate Gel for Controlled Release of Anesthetics
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1060-LL03-07
Modified Microparticles of Calcium Alginate Gel for Controlled Release of Anesthetics Erkesh O. Batyrbekov1, Turar N. Akylbekova2, and Rinat M. Iskakov3 1 Polymer, Instiyute of Chemical Sciences, 106 Valikhanov Street, Almaty, 050010, Kazakhstan 2 Institute of Chemical Sciences, 106 Valikhanov Street, Almaty, 050010, Kazakhstan 3 Institute of Chemical Scinces, 106 Vakikhanov Street, Almaty, 050010, Kazakhstan ABSTRACT The 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 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. Medicalbiological tests show that the duration of anesthetic activity for the drug-containing alginate beads increases at 5-8 times in comparison of free drugs. INTRODUCTION Controlled drug delivery technology using biodegradable polymers as carriers represents one of the actual and advanced areas of modern science and technology [1-3]. Among polymeric carriers, applied in drug delivery systems, microparticles based on alginic acid and its derivatives are of particular interest due to many advantages. These polymers are practically harmless, hydrophobic, able to form viscous water solutions and pastes, possess homogenizing, loosening and emulsifying properties. Alginic acid presents a polysaccharide, obtained from seaweed (laminaria) and consisting of repeated links of β-D-mannuronic and α-L-guluronic acids, interconnected with glucosidic bonds [4]. Alginic acid and its sodium and potassium salts have already found a wide application in pharmaceutical practice as loosening and binding remedies upon the production of tablets and preparatio
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