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Photoactivatable Surface-Functionalized Diatom Microalgae for Colorectal Cancer Targeted Delivery and Enhanced Cytotoxicity of Anticancer Complexes.
Pharmaceutics ( IF 5.4 ) Pub Date : 2020-05-25 , DOI: 10.3390/pharmaceutics12050480
Joachim Delasoie 1 , Philippe Schiel 1 , Sandra Vojnovic 2 , Jasmina Nikodinovic-Runic 2 , Fabio Zobi 1
Affiliation  

Systemic toxicity and severe side effects are commonly associated with anticancer chemotherapies. New strategies based on enhanced drug selectivity and targeted delivery to cancer cells while leaving healthy tissue undamaged can reduce the global patient burden. Herein, we report the design, synthesis and characterization of a bio-inspired hybrid multifunctional drug delivery system based on diatom microalgae. The microalgae’s surface was chemically functionalized with hybrid vitamin B12-photoactivatable molecules and the materials further loaded with highly active rhenium(I) tricarbonyl anticancer complexes. The constructs showed enhanced adherence to colorectal cancer (CRC) cells and slow release of the chemotherapeutic drugs. The overall toxicity of the hybrid multifunctional drug delivery system was further enhanced by photoactivation of the microalgae surface. Depending on the construct and anticancer drug, a 2-fold increase in the cytotoxic efficacy of the drug was observed upon light irradiation. The use of this targeted drug delivery strategy, together with selective spatial–temporal light activation, may lead to lower effective concentration of anticancer drugs, thereby reducing medication doses, possible side effects and overall burden for the patient.

中文翻译:

用于结肠直肠癌的光活化表面功能化硅藻微藻靶向递送和增强的抗癌复合物细胞毒性。

全身毒性和严重的副作用通常与抗癌化学疗法有关。基于增强的药物选择性和靶向递送至癌细胞而又不损害健康组织的新策略可以减轻全球患者的负担。本文中,我们报告了基于硅藻微藻的生物启发的混合多功能药物递送系统的设计,合成和表征。微藻的表面已用杂化维生素B 12化学功能化-可光活化的分子,并且该材料进一步负载了高活性tri(I)三羰基抗癌复合物。该构建体显示出对结直肠癌细胞(CRC)的粘附增强,并且化疗药物的释放缓慢。通过微藻表面的光活化进一步增强了混合多功能药物递送系统的总体毒性。取决于构建体和抗癌药物,在光照射下观察到该药物的细胞毒性功效增加了2倍。使用这种有针对性的药物输送策略,以及选择性的时空光激活,可能会导致抗癌药物的有效浓度降低,从而降低药物剂量,可能的副作用和患者的整体负担。
更新日期:2020-05-25
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