叶酸偶联壳聚糖的合成与表征及其纳米粒在 HT-29 细胞中的摄取。
Synthesis and characterization of folate conjugated chitosan and cellular uptake of its nanoparticles in HT-29 cells.
机构信息
Centre for Material and Fiber Innovation, Deakin University, Geelong Vic 3217, Australia.
出版信息
Carbohydr Res. 2011 May 1;346(6):801-6. doi: 10.1016/j.carres.2011.01.027.
Folate-chitosan (FA-CS) conjugates synthesized by coupling FA with CS render new and improved functions because the original properties of CS are maintained and the targeting ligand of FA is incorporated. In this work, FA-CS conjugates were synthesized based on chemical linking of carboxylic group of FA with amino group of CS as confirmed by Fourier transform spectroscopy (FTIR) and nuclear magnetic resonance ((1)H NMR). FA-CS conjugates displayed less crystal nature when compared to CS. The FA-CS nanoparticles (NPs) were prepared by crosslinking FA-CS conjugates with sodium tripolyphosphate (STPP). Positively charged FA-CS nanoparticles were spherical in shape with a particle size of about 100 nm. Cellular uptake of CS or FA-CS nanoparticles was assayed by fluorescent microscopy using calcein as fluorescent marker in colon cancer cells (HT-29). The FA-CS nanoparticles exhibited improved uptake of HT-29 and could become a potential targeted drug delivery system for colorectal cancer.
叶酸壳聚糖（FA-CS）缀合物通过将 FA 与 CS 偶联合成，赋予新的和改进的功能，因为 CS 的原始性质得以保留，并且 FA 的靶向配体被掺入。在这项工作中，通过 FA 的羧基与 CS 的氨基之间的化学连接合成了 FA-CS 缀合物，这一点通过傅里叶变换光谱（FTIR）和核磁共振（1H NMR）得到了证实。与 CS 相比，FA-CS 缀合物显示出较少的晶体性质。通过将 FA-CS 缀合物与三聚磷酸钠（STPP）交联制备 FA-CS 纳米颗粒（NPs）。带正电荷的 FA-CS 纳米颗粒呈球形，粒径约为 100nm。通过荧光显微镜使用荧光标记物钙黄绿素测定结肠癌细胞（HT-29）中 CS 或 FA-CS 纳米颗粒的细胞摄取。FA-CS 纳米颗粒表现出对 HT-29 的摄取能力提高，可成为结直肠癌潜在的靶向药物递送系统。
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