National Engineering Research Center for Biomaterials, Sichuan University, Chengdu 610065, China.
College of Chemistry and Materials Engineering, Wenzhou University, Wenzhou 325027, China.
Carbohydr Polym. 2017 Oct 15;174:789-797. doi: 10.1016/j.carbpol.2017.07.012. Epub 2017 Jul 8.
Poly(pseudo)rotaxane (PPR) nanoparticles was facilely prepared using poly(ethylene glycol) (PEG) modified with protoporphyrin (PpIX) and α-cyclodextrin (α-CD) via host-guest interaction, the effect of α-CD number on the nanoparticle properties was investigated. The PEG with protoporphyrin (PEG-PpIX) end capping was synthesized via coupling reaction and the poly(pseudo)rotaxane nanoparticles with different amount of α-CD were fabricated by host-guest interaction between mPEG-PpIX and α-CDs. The final product was characterized by nuclear magnetic spectrum (H NMR), X-ray diffraction (XRD), atomic force microscope (AFM) and dynamic light scattering (DLS). The results showed that the poly(pseudo)rotaxane nanoparticles with uniform spherical shape was successfully prepared and doxorubicin (DOX) could be efficiently encapsulated in the nanoparticles. The amount of α-CDs in poly(pseudo)rotaxane nanoparticles was proportional to micellar size and drug release rate. The nanoparticles with higher α-CD number showed better anticancer efficacy in half maximal inhibitory concentration (IC) test. The cell internalization efficiency of DOX-loaded poly(pseudo)rotaxane nanoparticles could be further improved by lowering the α-CD number to receive smaller nanoparticle size.
聚(伪)轮烷(PPR)纳米粒子通过主客体相互作用,使用聚乙二醇(PEG)与原卟啉(PpIX)和α-环糊精(α-CD)进行修饰,可轻松制备,研究了α-CD 数量对纳米粒子性质的影响。通过偶联反应合成了末端带有原卟啉的聚乙二醇(PEG-PpIX),通过 mPEG-PpIX 与α-CDs 之间的主客体相互作用,制备了具有不同α-CD 数量的聚(伪)轮烷纳米粒子。通过核磁共振谱(H NMR)、X 射线衍射(XRD)、原子力显微镜(AFM)和动态光散射(DLS)对最终产物进行了表征。结果表明,成功制备了具有均匀球形的聚(伪)轮烷纳米粒子,并且阿霉素(DOX)可以有效地包封在纳米粒子中。聚(伪)轮烷纳米粒子中α-CD 的数量与胶束尺寸和药物释放速率成正比。具有较高α-CD 数量的纳米粒子在半最大抑制浓度(IC)测试中表现出更好的抗癌功效。通过降低α-CD 的数量以接收更小的纳米粒子尺寸,可以进一步提高载 DOX 的聚(伪)轮烷纳米粒子的细胞内化效率。