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Synthesis and characterization of vincristine loaded folic acid–chitosan conjugated nanoparticles

机译：长春新碱负载的叶酸-壳聚糖共轭纳米颗粒的合成与表征

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Vincristine is an anticancer drug used to treat different types of cancer. However, vincristine has been reported to become resistant against some cancer such as small cell lung cancer cell lines due to decreased uptake, increased drug efflux etc. To increase the uptake, vincristine loaded folic acid–chitosan conjugated nanoparticles were synthesized using ionic gelation method at pH 2.5. 1H-NMR confirmed conjugation of folic acid with chitosan. Blank folic acid–chitosan conjugated nanoparticles had an average size of 897.5?±?0.90?nm, a polydispersity index of 0.738?±?0.30 and zeta potential of +11.2?±?0.43?mV and found to increase in vincristine loaded folic acid?chitosan nanoparticles at different formulations due to loading of vincristine in folic acid–chitosan conjugated nanoparticles. Fourier Transform Infrared Spectroscopy (FTIR) revealed different functional groups and loading of vincristine in chitosan nanoparticles. X-ray diffraction (XRD) was performed to confirm the crystalline nature of the drug after loading and face centered cubic (FCC) structure of nanoparticles. In vitro drug release study showed slow and sustained release of vincristine in phosphate buffered saline at pH 6.7. Scanning Electron Microscopy (SEM) revealed spherical and rough surface of nanoparticles. Transmission Electron Microscopy (TEM) confirmed loading of vincristine and size range of nanoparticles from 4.24 to 300?nm. Spectrophotometric analysis depicted maximum encapsulation efficiency and loading capacity of 81.25% and 10.31%, respectively. Since cancer cells express folate receptors on their surface, these vincristine loaded folic acid–chitosan conjugated nanoparticles could be used for targeted delivery against resistant cancer with some modifications.
机译：长春新碱是用于治疗不同类型癌症的抗癌药物。然而，据报道长春新碱由于摄取减少，药物外排增加等原因而对某些癌症（例如小细胞肺癌细胞系）具有耐药性。为了增加摄取，采用离子凝胶法在23℃合成了长春新碱负载的叶酸-壳聚糖共轭纳米颗粒。 pH值2.5。 1 H-NMR证实了叶酸与壳聚糖的结合。空白的叶酸-壳聚糖共轭纳米粒子的平均粒径为897.5？±？0.90？nm，多分散指数为0.738？±？0.30，ζ电位为+11.2？±？0.43？mV，发现长春新碱负载的叶酸会增加由于长春新碱在叶酸-壳聚糖共轭纳米粒子中的负载，因此壳聚糖纳米粒的配方不同。傅里叶变换红外光谱（FTIR）揭示了壳聚糖纳米颗粒中长春新碱的不同官能团和负载量。进行X射线衍射（XRD）以确认装载后的药物的晶体性质和纳米粒子的面心立方（FCC）结构。体外药物释放研究显示长春新碱在pH 6.7的磷酸盐缓冲盐水中缓慢且持续释放。扫描电子显微镜（SEM）显示了纳米颗粒的球形和粗糙表面。透射电子显微镜（TEM）证实长春新碱的负载量和纳米粒子的尺寸范围为4.24至300？nm。分光光度分析表明最大包封效率和装载量分别为81.25％和10.31％。由于癌细胞在其表面表达叶酸受体，因此这些经过长春新碱加载的叶酸-壳聚糖共轭纳米颗粒可以进行一些修饰，用于抗药性的靶向递送。

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