<p>This work reports the tailor-made functional microgels for the anticancer drug doxorubicin’s (DOX) delivery to cancer cells. Disulfide crosslinked microgels were synthesized through water in oil (w/o) mini-emulsion polymerization, followed by surface functionalization with rhodamine amine (RhNH<sub>2</sub>, fluorescent active agent) and polysulfobetaine (zwitterion) brushes, respectively. Here, RhNH<sub>2</sub> responded to the microgel’s pH alteration by appearing in the emission range of fluorescence at 565–585&#xa0;nm, and the occurrence of polysulfobetaine lessened model protein adsorption, which is here bovine serum albumin (BSA) (~ 20% reduction). This multifaceted microgel was categorized using different characterizations. Synthesized microgels showed a % drug loading content (%DLC) of (8 ± 2)% as well as a % drug loading efficiency (%DLE) of (80 ± 5)%. The cytotoxic behavior of biopolymer-based microgel was computed over MDA-MB-231 (<i>IC</i><sub><i>50</i></sub> 125&#xa0;µg/mL) cancer cells through MTT assay, remarking that the designed microgel is non-toxic, although drug-loaded microgels exhibited consequential toxicity. To comprehend cell apoptosis along with the cancer cells’ response to drug-loaded microgels, FACS, and cell uptake (in vitro) investigations were performed. These fluorescent active, non-toxic, zwitterionic, and REDOX-responsive microgels could be a potential candidate for promoting a significant inhibitory impact on cancer cells.</p> Graphical Abstract <p></p>

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pH-triggered Fluorescent-Active Antifouling Microgels Having Disulfide Crosslinked Core for the Application of Site-Specific REDOX-Active Drug Delivery to the Triple Negative Cancer Cells MDA-MB-231

  • Moumita Shee,
  • Sovan Lal Banerjee,
  • Ankita Dey,
  • Piyali Basak,
  • Mahitosh Mandal,
  • Amit Kumar Das,
  • Narayan Chandra Das

摘要

This work reports the tailor-made functional microgels for the anticancer drug doxorubicin’s (DOX) delivery to cancer cells. Disulfide crosslinked microgels were synthesized through water in oil (w/o) mini-emulsion polymerization, followed by surface functionalization with rhodamine amine (RhNH2, fluorescent active agent) and polysulfobetaine (zwitterion) brushes, respectively. Here, RhNH2 responded to the microgel’s pH alteration by appearing in the emission range of fluorescence at 565–585 nm, and the occurrence of polysulfobetaine lessened model protein adsorption, which is here bovine serum albumin (BSA) (~ 20% reduction). This multifaceted microgel was categorized using different characterizations. Synthesized microgels showed a % drug loading content (%DLC) of (8 ± 2)% as well as a % drug loading efficiency (%DLE) of (80 ± 5)%. The cytotoxic behavior of biopolymer-based microgel was computed over MDA-MB-231 (IC50 125 µg/mL) cancer cells through MTT assay, remarking that the designed microgel is non-toxic, although drug-loaded microgels exhibited consequential toxicity. To comprehend cell apoptosis along with the cancer cells’ response to drug-loaded microgels, FACS, and cell uptake (in vitro) investigations were performed. These fluorescent active, non-toxic, zwitterionic, and REDOX-responsive microgels could be a potential candidate for promoting a significant inhibitory impact on cancer cells.

Graphical Abstract