Preparation, characterization, and in vitro release of folic acid-conjugated chitosan nanoparticles loaded with methotrexate for targeted delivery
Preparation, characterization, and in vitro release of folic acid-conjugated chitosan nanoparticles loaded with methotrexate for targeted delivery
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DOI：
10.1007/s00289-011-0674-x
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发表时间：
2012-04-01
期刊：
影响因子：
3.2
通讯作者：
Xu, Yi
中科院分区：
文献类型：
--
作者：
Ji, Jingou;Wu, Danjun;Xu, Yi
为降低甲氨蝶呤（MTX）的毒性，提高纳米粒的靶向性，以三聚磷酸钠为交联剂，制备了甲氨蝶呤-叶酸（FA）壳聚糖（CS）纳米粒。通过H-1-NMR和FT-IR证实了FA与CS的偶联。通过红外光谱对所制备的FA-CS纳米粒子进行表征，证实FA-CS与交联剂之间发生了交联反应。进行X射线衍射以揭示包封后药物的结晶性质。纳米颗粒的平均直径范围为293.9 +/- A 24.2至401.5 +/- A 20.4 nm，具有窄的粒度分布。在磷酸盐缓冲液（pH 6.8）中的体外释放模式表明，MTX负载的纳米颗粒的特性似乎具有初始突释效应，然后缓慢，持续的药物释放。FA或低分子量FA缀合物片段也从纳米颗粒中释放，这可能具有降低MTX在体内的毒性作用的潜力。
To reduce the toxicity of methotrexate (MTX) and increase the targeting of nanoparticles, the MTX-loaded chitosan (CS) covalently bonded with folic acid (FA) nanoparticles were prepared, and sodium tripolyphosphate was used as the cross-linking agent. FA was successfully conjugated to CS confirmed by H-1-NMR and Fourier transform infrared spectrometer (FT-IR). The prepared FA-CS nanoparticles were characterized by FT-IR spectroscopy to confirm the cross-linking reaction between FA-CS and cross-linking agent. X-ray diffraction was performed to reveal the crystalline nature of the drug after encapsulation. The average diameters of the nanoparticles ranged from 293.9 +/- A 24.2 to 401.5 +/- A 20.4 nm with a narrow particle size distribution. In vitro release pattern in phosphate buffer saline (pH 6.8) indicated that the characteristics of the MTX-loaded nanoparticles appeared to have an initial burst effect and followed by a slow, sustained drug release. FA or low molecular weight FA conjugate fragments were also released from the nanoparticles, which might have potential to reduce toxic effects of MTX within the body.