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The Primary Study on Miglitol Coated with Polyelectrolyte Complex Nanoparticles Based on Chitosan Including Preparation, Characterization and Optimization

Author: HuangWeiHua
Tutor: YangWuLi
School: Fudan University
Course: Chemical Engineering
Keywords: Polyelectrolyte complexes Nanoparticles Drug carrier Biodegradable Chitosan Polyaspartic acid Miglitol In vitro release
CLC: TB383.1
Type: Master's thesis
Year: 2009
Downloads: 88
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Abstract

Polyelectrolyte complexes (Polyelectrolyte complexes, PEC) refers to two with the opposite charge of the macromer is formed by the interaction of the electrostatic attractive force of the macromolecular complexes. As with the charge-imparting unique solution and bulk properties of such polymers, the last two decades has been widely applied. Commonly used in the preparation of polyelectrolyte complexes polyelectrolyte dimethyl rare propyl ammonium salt, polyacrylic acid salt, carboxymethyl cellulose, chitosan, polyphosphates, poly-lysine and the like. Chitosan (CS) is the deacetylation of chitin polycationic electrolyte, generally the degree of deacetylation is greater than 70% of chitin called chitosan. Natural chitosan has antibacterial, lowering cholesterol and blood lipids, and selectively to the tumor cell aggregation, inhibition of tumor cell growth, good biocompatibility can be organisms completely absorbed characteristics, which is widely used in biological pharmaceutical and preparation. Polyaspartic acid (PAsp) its toxicity, biocompatibility, self-degradation, metabolism, absorption and excretion of the body to be known as the \Because of its easy introduction of the side chain, synthetic monomers can be copolymerized with other amino acids, is unique in many polymer materials. Pharmaceutical preparation of nano-particles (also known as nanosphere having a diameter of 10-1000nm) has more advantages than the micron particles can macromolecules passed epithelial tissue, and to promote the penetration of the drug absorption, to effectively improve the bioavailability of the drug to reduce the side effects. 2 - (hydroxymethyl) -3,4,5 - similar to the piperidine triols structure of the drug and glucose, is a relatively new class of inhibitors bulk drug. Primarily for the treatment of insulin-dependent (type) I diabetes, 7-type Gauchen disease (a glucose cerebroside metabolism genetic disease), and the anti-AIDS. The clinical use of 2 - (hydroxymethyl) -3,4,5 - piperidine alcohol drug Miglitol (MiG columns alcohol), Miglustat. The formulations of these drugs capsules and tablets, as well as a small amount of the injection. 2 - (hydroxymethyl) -3,4,5 - the piperidine three alcohols drugs is extremely easy to dissolve in water, faster metabolism in the body, a significant burst release phenomenon. Often resulting in patients taking these drugs, all kinds of adverse reactions, such as abdominal pain, diarrhea, and other gastrointestinal discomfort, rash, and kidney damage. The work of this dissertation is to expand based on the above background, and trends. Main research interests lie in the use of electrostatic interactions between the polyelectrolyte preparation of chitosan - the polyaspartic acid load MiG column alcohols nanoparticles and its characterization and screening, and obtained the following results : (1) is wetted with a small amount of glacial acetic acid, and then adding a small amount of 75% hydrogen peroxide solution, and then dissolving the appropriate amount of deuterated water, and then was measured using Q-NMR nanoparticles Two polyelectrolyte molecular chain unit molar ratio n / n-^{(2) . And thus obtain the molecular chain unit of nanoparticles of chitosan and polyaspartic molar ratio n / n-^{(2) with feeding when n / N-of ^{(1) . Prepared by two methods (2) using the mixing method and the adsorption method miglitol drug loading for the sample drug nanoparticles, a detailed examination of chitosan molecular weight chitosan with aspartic acid unit molar ratio, and vote compound miglitol concentration, preparation temperature and the solution PH value of the drug embedded. The results showed that using molecular weight for 17.9kDa chitosan and molecular weight of 10.0kDa polyaspartic positive system Nanocrystalline particle diameter distribution is relatively uniform when the input miglitol concentration of 0.8%, The encapsulation efficiency and drug loading highest. (3) development of a simple, and precision high HPLC-ELSD analytical methods, miglitol drug detection. And on this basis, investigated the CS with PAsp units molar ratio is 1.6, miglitol feed concentration of 0.8% was stirred for 16 hours at 20 ° C and 50 ℃ obtained nanoparticles miglitol drug release effect. Found that using positive system formed containing drug nanoparticles drug nanoparticles embedded in internal pH = 4.0 medium slow-release effect is more obvious.}}}

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