Guangdong Provincial Key Laboratory of Construction and Detection in Tissue Engineering, Medical Imaging Center, Nanfang Hospital, School of Biomedical Engineering, Southern Medical University, 1023 Sha-Tai South Road, Guangzhou, Guangdong 510515, China.
State Key Laboratory of Natural Medicines and Jiangsu Key Laboratory of Drug Discovery for Metabolic Diseases, Center of Advanced Pharmaceuticals and Biomaterials, China Pharmaceutical University, Nanjing, 210009, China.
Nano Lett. 2021 Nov 24;21(22):9551-9559. doi: 10.1021/acs.nanolett.1c03130. Epub 2021 Nov 5.
Hollow mesoporous organosilica nanoparticles (HMONs) are widely considered as a promising drug nanocarrier, but the loaded drugs can easily leak from HMONs, resulting in the considerably decreased drug loading capacity and increased biosafety risk. This study reports the smart use of core/shell FeO/GdO (FG) hybrid nanoparticles as a gatekeeper to block the pores of HMONs, which can yield an unreported large loading content (up to 20.4%) of DOX. The conjugation of RGD dimer (R2) onto the DOX-loaded HMON with FG capping (D@HMON@FG@R2) allowed for active tumor-targeted delivery. The aggregated FG in D@HMON@FG@R2 could darken the normal tissue surrounding the tumor due to the high value (253.7 mM s) and high / ratio (19.13), and the intratumorally released FG as a result of reducibility-triggered HMON degradation could brighten the tumor because of the high value (20.1 mM s) and low / ratio (7.01), which contributed to high contrast magnetic resonance imaging (MRI) for guiding highly efficient tumor-specific DOX release and chemotherapy.
中空介孔有机硅纳米粒子（HMONs）被广泛认为是一种很有前途的药物纳米载体，但负载的药物很容易从 HMONs 中泄漏出来，导致药物装载能力大大降低和生物安全性风险增加。本研究报告了智能使用核/壳 FeO/GdO（FG）杂化纳米粒子作为守门员来阻挡 HMONs 的孔，从而可以产生未报道的高载药量（高达 20.4%）的 DOX。将 RGD 二聚体（R2）接枝到用 FG 封端的 DOX 负载的 HMON 上（D@HMON@FG@R2），允许主动肿瘤靶向递药。由于高 r 值（253.7mM s）和高 r/值（19.13），聚集的 FG 会使肿瘤周围的正常组织变暗，并且由于还原触发的 HMON 降解而在肿瘤内释放的 FG 会使肿瘤变亮，这是因为 r 值高（20.1mM s），r/值低（7.01），有助于高对比度磁共振成像（MRI）指导高效的肿瘤特异性 DOX 释放和化疗。
