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Encapsulation and Delivery of an Osteosarcoma Stem Cell Active Gallium(III)‐Diflunisal Complex Using Polymeric Micelles

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The presence of osteosarcoma stem cells (OSC) in patients with osteosarcoma is associated to poor prognosis. Here we report the encapsulation of an OSC-active gallium(III) compound using polymeric nanoparticles and its delivery into osteosarcoma cells. The nanoparticle formulation improves bulk osteosarcoma cell and OSC potency relative to the payload while maintaining a similar mechanism of action as the payload.


Here we report the encapsulation of an osteosarcoma stem cell (OSC) potent gallium(III)-diflunisal complex 1 into polymeric nanoparticles, and its delivery into osteosarcoma cells. At the optimum feed (20 %, 1 NP20 ), nanoparticle encapsulation of 1 enhances potency towards bulk osteosarcoma cells and OSCs (cultured in monolayer and three-dimensional systems). Strikingly, the nanoparticle formulation exhibits up to 5645-fold greater potency towards OSCs than frontline anti-osteosarcoma drugs, doxorubicin and cisplatin. The nanoparticle formulation evokes a similar mechanism of action as the payload, which bodes well for future translation. Specifically, the nanoparticle formulation induces nuclear DNA damage, cyclooxygenase-2 downregulation, and caspase-dependent apoptosis. To the best of our knowledge, this is the first study to demonstrate that polymeric nanoparticles can be used to effectively deliver an OSC-active metal complex into osteosarcoma cells.

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