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Pullulan derivative with cationic and hydrophobic moieties as an appropriate macromolecule in the synthesis of nanoparticles for drug delivery.
International Journal of Biological Macromolecules ( IF 7.7 ) Pub Date : 2020-09-15 , DOI: 10.1016/j.ijbiomac.2020.09.064
Marieta Constantin 1 , Sanda Bucatariu 1 , Liviu Sacarescu 1 , Oana Maria Daraba 2 , Maria Anghelache 3 , Gheorghe Fundueanu 1
Affiliation  

A new amphiphilic pullulan derivative (DBAP-PO) was obtained by grafting tertiary butyl amine and octanoyl groups on the pullulan backbone as cationic and hydrophobic moieties, respectively. The structural characteristics of the modified polymer were investigated by FT-IR and 1H and 13C NMR spectroscopy.

The self-association ability in aqueous solution of DBAP-PO was studied by viscosity and fluorescence methods. The intrinsic viscosity of the polymer was determined by Wolf model. The critical aggregation concentration (CAC) value of 0.028 g/dL, determined by fluorescence measurements in the presence of pyrene, was confirmed by capillary viscosimetry and dynamic laser scattering (DLS). Dialysis method was used to demonstrate the capacity of the pullulan derivative to form spherical nanoparticles (d ~ 200 nm) loaded with model drug, sodium diclofenac (DF) (74% entrapment efficiency). The DF release was sustained and pH-dependent. In vitro cytotoxicity as well as morphological studies conducted on the human skin fibroblasts showed that DBAP-PO/DF nanoparticles do not exhibit cytotoxic effects at the pharmacologically relevant concentration of DF, maintaining the typical morphology of the cells.



中文翻译:

具有阳离子和疏水部分的支链淀粉衍生物作为合适的大分子,可合成用于药物递送的纳米颗粒。

通过将叔丁胺和辛酰基分别接枝在支链淀粉主链上作为阳离子和疏水部分,获得了一种新的两亲支链淀粉衍生物(DBAP-PO)。通过FT-IR,1 H和13 C NMR光谱研究了改性聚合物的结构特征。

通过粘度和荧光方法研究了DBAP-PO在水溶液中的自缔合能力。聚合物的特性粘度通过Wolf模型确定。通过capillary存在下的荧光测量确定的临界聚集浓度(CAC)值为0.028 g / dL,通过毛细管粘度测定法和动态激光散射(DLS)得以确认。透析方法用于证明支链淀粉衍生物形成负载有模型药物双氯芬酸钠(DF)的球形纳米颗粒(d〜200 nm)的能力(74%的包封率)。DF的释放是持续的并且是pH依赖性的。对人体皮肤成纤维细胞进行的体外细胞毒性和形态研究表明,DBAP-PO / DF纳米颗粒在药理学上相关的DF浓度下不表现出细胞毒性作用,

更新日期:2020-09-15
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