Stimuli-responsive release of drugs from a nanocarrier in spatial-, temporal-, and dosage-controlled fashions is of great interest in the pharmaceutical industry. Paclitaxel is one of the most effective and popular chemotherapeutic drugs against a number of cancers such as metastatic or nonmetastatic breast cancer, non–small cell lung cancer, refractory ovarian cancer, AIDS-related Kaposi’s sarcoma, and head and neck cancers. Here, by taking the advantage of RNA nanotechnology in biomedical and material science, we developed a three-dimensional pyramid-shaped RNA nanocage for a photocontrolled release of cargo, using paclitaxel as a model drug. The light-triggered release of paclitaxel or fluorophore Cy5 was achieved by incorporation of photocleavable spacers into the RNA nanoparticles. Upon irradiation with ultraviolet light, cargos were rapidly released (within 5 min). In vitro treatment of breast cancer cells with the RNA nanoparticles harboring photocleavable paclitaxel showed higher cytotoxicity as compared to RNA nanoparticles without the photocleavable spacer. The methodology provides proof of concept for the application of the light-triggered controlled release of drugs from RNA nanocages.

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从纳米载体以空间，时间和剂量控制的方式刺激响应释放药物在制药工业中引起了极大的兴趣。紫杉醇是针对多种癌症（例如转移性或非转移性乳腺癌，非小细胞肺癌，难治性卵巢癌，艾滋病相关的卡波西氏肉瘤和头颈癌）的最有效和最受欢迎的化学治疗药物之一。在这里，通过利用生物医学和材料科学中RNA纳米技术的优势，我们开发了三维金字塔形RNA纳米笼，用于以紫杉醇为模型药物对货物进行光控释放。紫杉醇或荧光团Cy5的光触发释放是通过将可光裂解的间隔基掺入RNA纳米颗粒中来实现的。在紫外线照射下，与不具有光可裂解间隔物的RNA纳米颗粒相比，具有光可裂解紫杉醇的RNA纳米颗粒对乳腺癌细胞的体外治疗显示出更高的细胞毒性。该方法为从RNA纳米笼中光触发药物的控释应用提供了概念验证。

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