The Primary Study On Miglitol Coated With Polyelectrolyte Complex Nanoparticles Based On Chitosan Including Preparation, Characterization And Optimization

Polyelectrolyte complexes(PECs) are formed by static interactions between macromolecules that carry oppositely charged polyions.In the recent twenty years, PECs have been studied broadly due to their special properties,and applied in many fields.The common polyelectrolytes which used to prepare PECs includes,dimethyl diallyl ammonium chloride,polyacrylate,carboxymethyl cellulose,chitosan, polyphosphates and poly lysine,etc.Chitosan(CS) is deacetylated from chitin.Natural chitosan shows remarkable capabilities of antibacterial,restraining the growth of tumor cells,lowering cholesterol and blood liquid,biocompatibility and absorption by organism.It has been widely applied in biomedicine and biomaterials.Due to its excellent biocompatibility,low toxicity and biodegradability,Poly (aspartic acid) is extensively applied in biomedicine as a kind of "green macromolecule".Poly(aspartic acid) has special property for grafting side chains and copolymerizing with other amino acid easily.The drug-loaded nanoparticles have shown superior capabilities than microparticles in their properties of easily penetrating epithelial cells,accelerating the osmotic absorption of drug,increasing the utilization ratio of medicine and decreasing the side effects.2-hydroxymethyl-3,4,5-piperidinetriols drug has similar structure to glucose,it is a kind of new raw medicines for the production of enzyme inhibitor,which mainly used to cure Type 1 Diabetes Mellitus,Type 7 Gauchen and anti AIDS. Respectively,Miglitol and Miglustat have been applied in clinical use.These drug are extremely hydrophilic and their metabolism in live body is very fast,which lead to many adverse reactions such as abdominal pain,skin rash and renal damage.Thus,the development of a novel drug carrier system for delivering Miglitol became important.Based on the previous research on polyelectrolyte complexes,in this context,we use the CS-PAsp polyelectrolyte complexes to encapsulate Miglitol via electrostatic interaction to prepare biocompatible drug carrier.The results of each part are listed as follows:(1) The repeated molar ratio of amino groups from CS to carboxyl groups from PAsp could influence the formation and morphology of nanoparticles.NMR method was used to determine the real repeated molar ratio in CS-PAsp nanoparticles, Compared with the initial amount of CS and PAsp,the relationship between real molar ratio and initial molar ratio was investigated.(2) The mixing method and the absorption method were used to prepare Migital/CS-PAsp nanoparticles.The factors which influence the encapsulation of Miglitol have been studied,including the molecular weight of CS,repeated molar ratio,concentration of Miglitol,temperature and pH value.By researching these factors,the drug-loaded CS-PAsp nanoparticles were prepared with favorable encapsulation efficiency and loading capability.(3) HPLC-ELSD analytical method was used to detect the Miglitol content in nanoparticles.This analytical method was simple and can be easily used to characterize the release behavior of Miglitol /CS-PAsp nanoparticles.The results showed that the Miglitol/CS-PAsp exhibited the properties of sustaining release at pH 4.0 by positive mixing method.