ABSTRACT

Background

Bortezomib (BTZ) as an anticancer drug has been used through the injection pathway.

Research design and methods

Two types of Cyclodextrin nanosponges (CDNSs) were synthesized and studied by DLS, TEM, FTIR, and DSC instruments for BTZ delivery. Both carriers were analyzed for loading efficiencies and in-vitro release. Cell studies and intestinal permeability of selected CDNS were determined using MTT and SPIP method, respectively.

Results

Both types of CDNSs, encapsulated BTZ in their nano-porous structure, but better loading was shown in CDNS 1:4. FTIR and DSC results proved considerable encapsulation of BTZ into CDNSs. The slow and prolonged release profile was observed for CDNS 1:4 in comparison with CDNS 1:2. Based on in-vitro results, BTZ-CDNS 1:4 was chosen as a selected nanosystem for further analysis. This nontoxic carrier revealed considerable uptake (93.9% in 3 h) against the MCF-7 cell line but indicated higher IC₅₀ in comparison with the plain drug. This carrier also could improve the rat intestinal permeability of BTZ almost 5.8 times.

Conclusion

CDNS 1:4 has the ability to be introduced as a nontoxic carrier for BTZ delivery with its high loading, controlled release manner, high cellular uptake, and permeability improvement characteristics.

中文翻译：

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用于硼替佐米递送的环糊精纳米海绵的制备和表征。

摘要

背景

硼替佐米（BTZ）作为抗癌药已通过注射途径使用。

研究设计与方法

合成了两种类型的环糊精纳米海绵（CDNS），并通过DLS，TEM，FTIR和DSC仪器研究了BTZ的传递。分析了两种载体的装载效率和体外释放。分别使用MTT和SPIP方法确定所选CDNS的细胞研究和肠道通透性。

结果

两种类型的CDNS均以纳米孔结构封装BTZ，但在CDNS 1：4中显示了更好的负载。FTIR和DSC结果证明了将BTZ大量封装到CDNS中。与CDNS 1：2相比，观察到CDNS 1：4的释放缓慢和延长。根据体外结果，BTZ-CDNS 1：4被选作进一步分析的纳米系统。这种无毒载体显示出对MCF-7细胞系的大量吸收（3小时内占93.9％），但与普通药物相比，IC ₅₀更高。这种载体还可以使大鼠的BTZ肠通透性提高近5.8倍。

结论

CDNS 1：4具有高负载，控释方式，高细胞吸收和通透性改善的特性，可以作为BTZ输送的无毒载体而引入。