叶酸协同EDC改性高脱乙酰度壳聚糖微球的制备及工艺探究

发布时间：2018-10-17 14:03

【摘要】：使用高脱乙酰度壳聚糖制备了靶向药物载体-叶酸改性壳聚糖微球。首先通过碱法制备了高脱乙酰度的壳聚糖,采用酸碱滴定法和傅里叶变换红外光谱(FTIR)对其结构进行了表征,结果表明,经脱乙酰化处理后的壳聚糖脱乙酰度高达93.8%。然后以高脱乙酰度壳聚糖制备了叶酸改性壳聚糖,创新性地发现用1∶1的二甲基亚砜和水的混合溶剂可以得到壳聚糖和叶酸反应的均相体系。通过不同的改性方案,得到了不同改性程度的壳聚糖,改性程度分别达到了2.60%、5.10%、8.75%和9.49%。最后用三聚磷酸钠交联制备了叶酸改性壳聚糖微球,并用激光粒度仪系统地分析了三聚磷酸钠和改性壳聚糖的用量比例及浓度对微球的粒径、Zeta电位的影响。研究发现,随着三聚磷酸钠与改性壳聚糖的比值增大,微球的粒径和Zeta电位都增大,当比值增加到一定的程度,微球的粒径会快速增加。对三聚磷酸钠和改性壳聚糖加入浓度的研究,发现浓度的增大将导致粒径的增大和Zeta电位的降低。
[Abstract]:Chitosan microspheres with high deacetylation degree were prepared with folic acid as the target drug carrier. Firstly, chitosan with high degree of deacetylation was prepared by alkali method. The structure of chitosan was characterized by acid-base titration and Fourier transform infrared spectroscopy (FTIR). The results showed that the deacetylation degree of chitosan after deacetylation was as high as 93.8%. Then folic acid modified chitosan was prepared from chitosan with high degree of deacetylation. It was found that the homogeneous system of chitosan and folic acid reaction could be obtained by using the mixture solvent of 1:1 dimethyl sulfoxide and water. Through different modification schemes, chitosan with different degree of modification was obtained, and the degree of modification reached 2.60% 5.10% and 9.49% respectively. Finally, folic acid modified chitosan microspheres were prepared by crosslinking sodium tripolyphosphate. The effects of the dosage and concentration of sodium tripolyphosphate and modified chitosan on the particle size and Zeta potential of the microspheres were systematically analyzed by laser particle size analyzer. It was found that the particle size and Zeta potential of the microspheres increased with the increase of the ratio of sodium tripolyphosphate to modified chitosan. When the ratio increased to a certain extent, the particle size of the microspheres would increase rapidly. The concentration of sodium tripolyphosphate and modified chitosan was studied. It was found that the increase of concentration would lead to the increase of particle size and the decrease of Zeta potential.
【作者单位】：四川大学皮革化学与工程教育部重点实验室;四川大学生物医学工程技术研究中心;
【基金】：国家自然科学基金(51473001)
【分类号】：TQ460.4;O636.1

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