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葉酸協(xié)同EDC改性高脫乙酰度殼聚糖微球的制備及工藝探究

發(fā)布時間:2018-10-17 14:03
【摘要】:使用高脫乙酰度殼聚糖制備了靶向藥物載體-葉酸改性殼聚糖微球。首先通過堿法制備了高脫乙酰度的殼聚糖,采用酸堿滴定法和傅里葉變換紅外光譜(FTIR)對其結(jié)構(gòu)進(jìn)行了表征,結(jié)果表明,經(jīng)脫乙;幚砗蟮臍ぞ厶敲撘阴6雀哌_(dá)93.8%。然后以高脫乙酰度殼聚糖制備了葉酸改性殼聚糖,創(chuàng)新性地發(fā)現(xiàn)用1∶1的二甲基亞砜和水的混合溶劑可以得到殼聚糖和葉酸反應(yīng)的均相體系。通過不同的改性方案,得到了不同改性程度的殼聚糖,改性程度分別達(dá)到了2.60%、5.10%、8.75%和9.49%。最后用三聚磷酸鈉交聯(lián)制備了葉酸改性殼聚糖微球,并用激光粒度儀系統(tǒng)地分析了三聚磷酸鈉和改性殼聚糖的用量比例及濃度對微球的粒徑、Zeta電位的影響。研究發(fā)現(xiàn),隨著三聚磷酸鈉與改性殼聚糖的比值增大,微球的粒徑和Zeta電位都增大,當(dāng)比值增加到一定的程度,微球的粒徑會快速增加。對三聚磷酸鈉和改性殼聚糖加入濃度的研究,發(fā)現(xiàn)濃度的增大將導(dǎo)致粒徑的增大和Zeta電位的降低。
[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.
【作者單位】: 四川大學(xué)皮革化學(xué)與工程教育部重點實驗室;四川大學(xué)生物醫(yī)學(xué)工程技術(shù)研究中心;
【基金】:國家自然科學(xué)基金(51473001)
【分類號】:TQ460.4;O636.1

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