Journal
INTERNATIONAL JOURNAL OF BIOLOGICAL MACROMOLECULES
Volume 169, Issue -, Pages 206-215Publisher
ELSEVIER
DOI: 10.1016/j.ijbiomac.2020.12.094
Keywords
Nanocomposite; Carbon dots; Targeted drug delivery
Funding
- Key R&D project of Shandong Province [2019GSF107031]
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A novel nanocomposite was developed in this study for real-time imaging and therapeutic targeting of activated macrophages in the colon. The nanocomposite, formed by the covalent conjugation of Man-NPs with CDs, showed high drug casing density, negative charge, and specific uptake by inflamed macrophages, suggesting potential for treating inflammatory bowel disease.
In the present experimental series, we have developed a novel nanocomposite to target activated macrophages in the colon with real time imaging and therapeutic capabilities. This binary nanocomposite was formed by the covalent conjugation of mannosylated NPs (Man-NPs) with carbon dots (CDs). Man-NPs were prepared using a self-assembly method based on mannosylated decamethylenediamine-grafted carboxymethyl inulin amphiphilic acid. While, the CDs were synthesized using a simple bottom-up process using citric acid monohydrate and diethylenetriamine, which were tightly bonded to the Man-NPs surface by carbodimide coupling. The resulting nanocomposite had a uniform size of 241.3 nm with a negative charge and a high drug casing density of 25.54 wt% and blue self-fluorescence were emitted. Whereas, in vitro observation of cellular uptake indicated the greater nanocomposite uptake in inflamed macrophage as compared to the untreated macrophage and mannose receptor-negative cell lines, 4T1 respectively. However, in vivo bio distribution exhibited a large number (60%) of CDs/Man-NPs nanocomposite accumulated in the inflamed colon of colitis mice. It should be noted that the novel nanocomposite, as macrophage-targeted drug delivery, could have promise for the treatment of inflammatory bowel disease (IBD). (C) 2020 Published by Elsevier B.V.
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