Three-armed RGD-decorated starPLA-PEG nanoshuttle for docetaxel delivery.

Evidence from laboratory and animal studies provides groundwork for understanding mechanisms and potential before human studies continue.

• Level A · Stronger Clinical Evidence
• Level B · Emerging clinical evidence with positive signals
• Level C · Early human research exploring benefits
• Level D · Scientific groundwork from lab and animal studies
• Emerging · Emerging topic under active research

Abstract (original English)

A novel star-shaped amphiphilic copolymer based on three poly(lactide)-block-poly(ethylene glycol) (PLA-PEG) terminal arms extending from a glycerol multifunctional core was newly synthesized and decorated with the tumor-targeting ligand cyclic-RGDyK peptide (Arg-Gly-Asp-D-Tyr-Lys) to be eventually formulated in polymeric micelles incorporating a suitable anticancer drug (i.e., Docetaxel, DTX; drug loading 16 %, encapsulation efficiency 69 %). The biological profile of unloaded micelles (RGD-NanoStar) was studied on Human Adipose-derived Mesenchymal Stem Cells (Ad-MSCs) as health control, pointing out the absence of toxicity. Surprisingly, an unprecedented effect on cell viability was exerted by RGD-NanoStar, comparable to that of the free DTX, on tumoral MDA-MB 468 Human Breast Adenocarcinoma cells, specifically starting from 48 h of culture (about 40 % and 60 % of dead cells at 48 and 72 h, respectively, at all tested concentrations). RGD-NanoStar reduced the cell viability also of tumoral U87 Human Glioblastoma cells, compared to cells only, at 72 h (about 25 % of dead cells) demonstrating a time-dependent effect exerted by the highest concentrations. The effects of DTX-loaded micelles (RGD-NanoStar/DTX) on U87 and MDA-MB 468 cell lines were evaluated by MTT, cell morphology analysis, and scratch test. A compromised cell morphology was observed without significant difference

Evidence level

Evidence from laboratory and animal studies provides groundwork for understanding mechanisms and potential before human studies continue.

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