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Aminated Polysaccharide-Based Nanoassemblies as Stable Biocompatible Vehicles Enabling Crossing of Biological Barriers: An Effective Transdermal Delivery of Diclofenac Medicine
ACS Applied Bio Materials ( IF 4.6 ) Pub Date : 2020-03-19 , DOI: 10.1021/acsabm.0c00048
Yael Cohen 1, 2 , Roi Rutenberg 1, 2, 3 , Guy Cohen 4 , Boris Veltman 1, 2 , Raanan Gvirtz 4 , Elazar Fallik 1 , Dganit Danino 5 , Evgeni Eltzov 1 , Elena Poverenov 1
Affiliation  

A series of stable polysaccharide derivatives that spontaneously self-assemble into nanocarriers was synthesized by applying a reductive amination on chitosan. The prepared nanocarriers were comprehensively studied and found to allow encapsulation of molecular cargo in both aqueous and lipidic media and deliver this cargo across biological barriers. The nanocarriers have demonstrated effective transdermal delivery of diclofenac (Voltaren), a nonsteroidal anti-inflammatory drug, by increasing its skin permeation up to 100 vs the tested control. The modified polysaccharides were studied with a panel of three types of bioreporter bacteria sensitive to genotoxic and cytotoxic stresses. These studies showed the general safety of the prepared nanocarriers and provided insights concerning their activity in collaboration with the aliphatic side chain length. The described nanocarriers could be applied as tunable biocompatible vehicles for the delivery of medicines, cosmetic agents, and in other applications.

中文翻译:

基于胺化多糖的纳米组装体作为稳定的生物相容性载体,能够跨越生物屏障:双氯芬酸药物的有效透皮给药

通过在壳聚糖上进行还原胺化,合成了一系列自发自组装成纳米载体的稳定多糖衍生物。对制备的纳米载体进行了全面研究,发现允许将分子货物封装在水性和脂质介质中,并将这种货物运送穿过生物屏障。纳米载体已证明双氯芬酸 (Voltaren) 是一种非甾体抗炎药的有效透皮递送,与测试对照相比,其皮肤渗透性提高了 100。用一组对基因毒性和细胞毒性应激敏感的三种类型的生物报道细菌对改性多糖进行了研究。这些研究显示了制备的纳米载体的一般安全性,并提供了有关它们与脂肪族侧链长度合作的活性的见解。所描述的纳米载体可以用作可调节的生物相容性载体,用于药物、美容剂的输送和其他应用。
更新日期:2020-04-23
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