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Bi-functional nature of nanoceria: pro-drug and drug-carrier potentiality towards receptor-mediated targeting of doxorubicin
New Journal of Chemistry ( IF 2.7 ) Pub Date : 2020-09-02 , DOI: 10.1039/d0nj02895a Madhura A. Damle 1, 2, 3, 4, 5 , Varsha G. Shetty 6, 7, 8, 9, 10 , Alok P. Jakhade 1, 2, 3, 4, 5 , Ruchika Kaul-Ghanekar 6, 7, 8, 9, 10 , Rajeev C. Chikate 1, 2, 3, 4, 5
New Journal of Chemistry ( IF 2.7 ) Pub Date : 2020-09-02 , DOI: 10.1039/d0nj02895a Madhura A. Damle 1, 2, 3, 4, 5 , Varsha G. Shetty 6, 7, 8, 9, 10 , Alok P. Jakhade 1, 2, 3, 4, 5 , Ruchika Kaul-Ghanekar 6, 7, 8, 9, 10 , Rajeev C. Chikate 1, 2, 3, 4, 5
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Nanoceria is considered to be a promising material for the modulation of its pro-and anti-oxidant activities due to its tuneable Ce3+/Ce4+ ratios under different physiological conditions. In the present study, we explored the feasibility of CeO2 NPs as a pro-drug and drug carrying vehicle towards receptor-mediated targeted delivery of doxorubicin (DOX) to MCF-7 cancer cells. The surface-engineered, substancilly smaller sized (3–4 nm) particles of CeO2-loaded DOX-nanoconjugates possess excellent dispersibility in water, with surface charges in the range of +17.03 to −7.68 mV. The functionalised nanoceria exhibits a quasi-reversible Ce3+/Ce4+ redox couple at a considerably lower redox potential, while the amount of DOX loaded on the nanoceria was found to be in the range of 2.3–12%. The DNA binding and cleavage activities of CeO2 NPs suggest their beneficial binding with phosphate linkages that induces DNA damage. Uncoated and PEGylated CeO2 NPs possess significant anticancer activity against MCF-7, with the latter exhibiting better activity at 2.5 μg mL−1 due to its interference in cellular redox reactions induced by reactive oxygen species (ROS). Moreover, the synergic conjugation of nanoceria with DOX resulted in excellent cytotoxicity of these nanoconjugates against MCF-7 cells at an extremely low concentration (57.5 ng mL−1) of DOX. This feature can be ascribed to the enhanced uptake of nanoceria as well as site targeting of DOX nanoconjugates facilitated by the folic acid (FA) via folate receptors. Thus, it may be concluded that nanoceria behaves in a dual manner both as a pro-drug and an efficient nanocarrier for delivery of DOX at a specific site.
中文翻译：
纳米氧化铈的双功能性质：前药和药物载体对受体介导的阿霉素靶向的潜力
由于其在不同的生理条件下可调节的Ce 3+ / Ce 4+比例，纳米氧化铈被认为是一种有前途的调节其抗氧化和抗氧化活性的材料。在本研究中，我们探讨了CeO 2 NPs作为前药和载药媒介物对受体介导的阿霉素（DOX）向MCF-7癌细胞靶向递送的可行性。负载CeO 2的DOX-纳米共轭物的表面工程化，尺寸较小（3-4 nm）的粒子在水中的分散性极好，表面电荷范围为+17.03至-7.68 mV。功能化的纳米氧化铈表现出准可逆的Ce 3+ / Ce 4+氧化还原对的氧化还原电势要低得多，而纳米氧化铈上负载的DOX量在2.3–12％的范围内。CeO 2 NPs的DNA结合和裂解活性表明它们与诱导DNA损伤的磷酸酯键的有益结合。未包被和聚乙二醇化的CeO 2 NP对MCF-7具有显着的抗癌活性，由于MCF-7对活性氧（ROS）诱导的细胞氧化还原反应的干扰，在2.5μgmL -1下表现出更好的活性。此外，纳米氧化铈与DOX的协同缀合导致这些纳米缀合物以极低的浓度（57.5 ng mL -1）对MCF-7细胞具有优异的细胞毒性。）。此特征可归因于叶酸（FA）经由叶酸受体促进的纳米氧化铈的吸收增强以及DOX纳米缀合物的位点靶向。因此，可以得出结论，纳米氧化铈以双重方式既充当前药又作为用于在特定部位递送DOX的有效纳米载体。
更新日期：2020-10-15
中文翻译：
纳米氧化铈的双功能性质：前药和药物载体对受体介导的阿霉素靶向的潜力
由于其在不同的生理条件下可调节的Ce 3+ / Ce 4+比例，纳米氧化铈被认为是一种有前途的调节其抗氧化和抗氧化活性的材料。在本研究中，我们探讨了CeO 2 NPs作为前药和载药媒介物对受体介导的阿霉素（DOX）向MCF-7癌细胞靶向递送的可行性。负载CeO 2的DOX-纳米共轭物的表面工程化，尺寸较小（3-4 nm）的粒子在水中的分散性极好，表面电荷范围为+17.03至-7.68 mV。功能化的纳米氧化铈表现出准可逆的Ce 3+ / Ce 4+氧化还原对的氧化还原电势要低得多，而纳米氧化铈上负载的DOX量在2.3–12％的范围内。CeO 2 NPs的DNA结合和裂解活性表明它们与诱导DNA损伤的磷酸酯键的有益结合。未包被和聚乙二醇化的CeO 2 NP对MCF-7具有显着的抗癌活性，由于MCF-7对活性氧（ROS）诱导的细胞氧化还原反应的干扰，在2.5μgmL -1下表现出更好的活性。此外，纳米氧化铈与DOX的协同缀合导致这些纳米缀合物以极低的浓度（57.5 ng mL -1）对MCF-7细胞具有优异的细胞毒性。）。此特征可归因于叶酸（FA）经由叶酸受体促进的纳米氧化铈的吸收增强以及DOX纳米缀合物的位点靶向。因此，可以得出结论，纳米氧化铈以双重方式既充当前药又作为用于在特定部位递送DOX的有效纳米载体。
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