叶酸和聚乙二醇双修饰的壳聚糖纳米粒的制备及其性能表征

Preparation and Characterization of Folic Acid and PEG Conjugated Chitosan Nanoparticles

目的利用离子交联和化学交联相结合的方法制备壳聚糖纳米粒子(NPs),并对NPs分别进行了叶酸(FA)和聚乙二醇(PEG)的修饰。方法通过红外光谱进行结构验证;用扫描电镜和粒度分析仪对粒子的微观形态、粒径、电位等进行了表征;通过与Hela细胞摄取实验对其靶向作用进行验证。结果离子交联和化学交联相结合的方法制备壳聚糖纳米粒子粒径在200 nm左右并且粒径分布窄,修饰后的NPs(FA-NPs、PEG-NPs及FA+PEG-NPs)粒径不受功能基团修饰的影响。激光共聚焦试验证明FA-NPs及FA+PEG-NPs能显著提高细胞对粒子的摄取,而PEG-NPs则明显降低其对粒子的摄取。结论 FA+PEG-NPs有望成为一种新型的药物载体,用于抗癌药物对癌细胞的主动靶向。

OBJECTIVE An ionic gelation combined with chemical crosslinking method was developed to prepare chitosan nanoparticles, followed by conjugation with folate （FA） and polyethylene glycol （PEG）. METHODS The structures were verified by infrared spectroscopy. The morphology, diameter and Zeta electric potential of the nanoparticles were assayed by environmental scanning electron microscope and scattering particle analyzer. The specificity of the FA＋PEG-NPs targeting cancer cells was demonstrated by human adenocarcinoma Hela cells. RESULTS The chitosan NPs presented a narrow size distribution with an average diameter about 200 nm regardless of the type of functional group. Laser confocal scanning imaging proved that both FA＋PEG-NPs and FA-NPs could greatly enhance uptake by Hela cells. However, the PEG-NPs showed contrary results. CONCLUSION FA＋PEG-NPs can be applied as a new vehicle to actively deliver anticancer drugs to tumor cells.