Antibiotic conjugated fluorescent carbon dots as a theranostic agent for controlled drug release, bioimaging, and enhanced antimicrobial activity.

Journal of drug delivery Pub Date : 2014-01-01 Epub Date: 2014-03-18 DOI:10.1155/2014/282193
Mukeshchand Thakur, Sunil Pandey, Ashmi Mewada, Vaibhav Patil, Monika Khade, Ekta Goshi, Madhuri Sharon
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Abstract

A novel report on microwave assisted synthesis of bright carbon dots (C-dots) using gum arabic (GA) and its use as molecular vehicle to ferry ciprofloxacin hydrochloride, a broad spectrum antibiotic, is reported in the present work. Density gradient centrifugation (DGC) was used to separate different types of C-dots. After careful analysis of the fractions obtained after centrifugation, ciprofloxacin was attached to synthesize ciprofloxacin conjugated with C-dots (Cipro @ C-dots conjugate). Release of ciprofloxacin was found to be extremely regulated under physiological conditions. Cipro @ C-dots were found to be biocompatible on Vero cells as compared to free ciprofloxacin (1.2 mM) even at very high concentrations. Bare C-dots ( ∼ 13 mg mL(-1)) were used for microbial imaging of the simplest eukaryotic model-Saccharomyces cerevisiae (yeast). Bright green fluorescent was obtained when live imaging was performed to view yeast cells under fluorescent microscope suggesting C-dots incorporation inside the cells. Cipro @ C-dots conjugate also showed enhanced antimicrobial activity against both model gram positive and gram negative microorganisms. Thus, the Cipro @ C-dots conjugate paves not only a way for bioimaging but also an efficient new nanocarrier for controlled drug release with high antimicrobial activity, thereby serving potential tool for theranostics.

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将抗生素共轭荧光碳点作为一种治疗剂,用于控制药物释放、生物成像和增强抗菌活性。
本研究报告新颖地介绍了利用阿拉伯树胶(GA)在微波辅助下合成亮碳点(C-dots),并将其作为分子载体,用于载运广谱抗生素盐酸环丙沙星。密度梯度离心法(DGC)用于分离不同类型的 C-点。对离心后得到的馏分进行仔细分析后,将环丙沙星附着在 C 点上,合成了与 C 点共轭的环丙沙星(Cipro @ C-dots conjugate)。研究发现,在生理条件下,环丙沙星的释放受到极大的调节。与游离环丙沙星(1.2 mM)相比,即使浓度很高,Cipro @ C-点在 Vero 细胞中的生物相容性也很好。裸 C-点(∼ 13 mg mL(-1))被用于最简单的真核生物模型--酿酒酵母(酵母)的微生物成像。在荧光显微镜下对酵母细胞进行活体成像时,可获得亮绿色荧光,表明 C 点已融入细胞内。Cipro @ C-点共轭物还显示出对模式革兰氏阳性和革兰氏阴性微生物都具有更强的抗菌活性。因此,Cipro @ C 点共轭物不仅为生物成像铺平了道路,而且还是一种高效的新型纳米载体,可用于控制药物释放并具有很高的抗菌活性,从而成为治疗学的潜在工具。
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Journal of drug delivery
Journal of drug delivery PHARMACOLOGY & PHARMACY-
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