准纳米魔芋葡甘露聚糖载药微球的制备及其体外释药性能研究

发布时间：2018-02-25 19:36

本文关键词： 魔芋葡甘露聚糖电喷雾交联剂释药模型　出处：《重庆大学》2014年硕士论文　论文类型：学位论文

【摘要】：随着纳米技术的兴起以及人类对于人体各种屏障认识的不断深入，纳米药物载体因可降低药物自身毒副作用，并具有靶向与缓、控释特性而越来越受到人们的青睐。研制各种新型的纳米载药系统有助于推进各种疾病的防治，并且可以减少某些药物在人体代谢过程中产生的毒性。本文以人体结肠部位酶（β-葡甘露聚糖酶）特异性降解材料——魔芋葡甘露聚糖（KGM）为药物载体，双氯芬酸钠为模型药物，研究了魔芋葡甘露聚糖及其载药微胶囊的高压静电喷雾制备技术，获得了载药准纳米微胶囊，考察了交联剂种类、微胶囊粒径与体外药物释放特性的关系，获得了如下实验结果： ①高压静电喷雾技术是一种优良的微胶囊制备技术，具有制备条件温和、微胶囊粒径可控、且粒径分布均匀的特点。当电压-6.5kV，，正负极间距离为1cm，5.0mg/mL,KGM溶液：无水乙醇1：1（V/V），双氯芬酸钠浓度1.0mg/mL的实验条件下，可制备出平均粒径为1.474μm的准纳米魔芋葡甘露聚糖载药微胶囊； ②交联魔芋葡甘露聚糖仍可被魔芋葡甘露聚糖酶降解，但在人工胃酸中无材料降解和药物释放。 ③准纳米KGM载药微球克服了微米级KGM载药微球的药物突释效应，且准纳米KGM载药微球具有较好的药物缓释作用。 ④使用不同的交联剂可以方便地调节准纳米KGM载药微球的药物释放规律，即可以方便地实现药物控制释放。综上所述，利用高压静电喷雾技术，可以方便地制备准纳米魔芋葡甘露聚糖载药微球，采用不同的交联剂模式可以获得预期的体外释放模型。因此，KGM有望成为一种优良的结肠定位缓、控释药物载体。
[Abstract]:With the rise of nano - technology and the deepening of human ' s understanding of human body ' s various barriers , the nano - drug carrier is more and more popular because it can reduce the toxic side effect of the drug , and has the characteristics of targeting and slow release and controlled release , and the development of various new nano - drug - loading systems can help to advance the prevention and treatment of various diseases , and can reduce the toxicity of certain drugs in the metabolism of human body . The high - pressure electrostatic spray preparation technology of konjac glucomannan and its drug - carrying microcapsules was studied by using human colon site enzyme ( 尾 - glucosidase ) as drug carrier and diclofenac sodium as model drug . The relationship between the type of cross - linking agent , the size of microcapsule and drug release in vitro was studied . The experimental results were obtained as follows : ( 1 ) High - voltage electrostatic spraying technology is an excellent preparation technology of microcapsules , which has the characteristics of mild preparation condition , controllable particle size and uniform particle size distribution . When voltage - 6.5kV , the distance between positive and negative electrodes is 1cm , 5.0mg / mL , KGM solution : absolute ethyl alcohol 1 : 1 ( V / V ) , diclofenac sodium concentration is 1.0 mg / mL , a quasi - nano konjak glucomannan carrier microcapsule with an average particle diameter of 1.47渭m can be prepared ; ( 2 ) Cross - linked konjac glucomannan can still be degraded by konjac glucomannan , but there is no material degradation and drug release in artificial gastric acid . ( 3 ) the quasi - nano KGM drug - loaded microsphere overcomes the drug burst effect of the micron - level KGM drug - loaded microsphere , and the quasi - nano KGM drug - loaded microsphere has better drug sustained - release effect . ( 4 ) the drug release rule of the quasi - nano KGM drug - loaded microspheres can be conveniently adjusted by using different cross - linking agents , and the drug control release can be conveniently realized . In conclusion , by using high - voltage electrostatic spraying technology , it is easy to prepare quasi - nano konjac glucomannan drug - carrying microspheres , and the expected in vitro release model can be obtained by adopting different cross - linking agent modes . Therefore , the KGM is expected to be an excellent colonic positioning slow - release drug carrier .

【学位授予单位】：重庆大学
【学位级别】：硕士
【学位授予年份】：2014
【分类号】：R943;R96

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