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As a highly invasive and highly metastatic tumor, glioma is considered to be one of
the most aggressive malignant brain tumors due to its challenges such as poor prognosis, high mortality and high recurrence rate.
Although surgical resection, radiotherapy, chemotherapy and other methods have been used clinically to treat glioma, its prognosis is still poor, and the median overall survival is only 14-17 months
.
Due to the limitation of the blood-brain barrier (BBB), most of the currently developed anti-tumor drugs are difficult to cross the BBB to reach the tumor site, and the treatment effect on glioma is not good; In addition, because these drugs lack tumor specificity, they are prone to serious toxic side effects and drug resistance
.
Improving the delivery and efficacy of antitumor drugs in gliomas and achieving on-demand and efficient treatment of gliomas in situ remains challenging
.
the most aggressive malignant brain tumors due to its challenges such as poor prognosis, high mortality and high recurrence rate.
Although surgical resection, radiotherapy, chemotherapy and other methods have been used clinically to treat glioma, its prognosis is still poor, and the median overall survival is only 14-17 months
.
Due to the limitation of the blood-brain barrier (BBB), most of the currently developed anti-tumor drugs are difficult to cross the BBB to reach the tumor site, and the treatment effect on glioma is not good; In addition, because these drugs lack tumor specificity, they are prone to serious toxic side effects and drug resistance
.
Improving the delivery and efficacy of antitumor drugs in gliomas and achieving on-demand and efficient treatment of gliomas in situ remains challenging
.
Recently, Professor Liu Hong of the Shanghai Institute of Materia Medica, Chinese Academy of Sciences and Professor Ye Deju of Nanjing University have cooperated to make the latest research progress
in the research of targeted activated organic co-assembled nanodiagnostic and therapeutic probes for near-infrared fluorescence-magnetic resonance dual-modal imaging and chemotherapy-photodynamic combination therapy for brain gliomas in situ.
The relevant results were published in the internationally renowned academic journal ACS Nano on December 12, 2022 under the title "Controlling Disassembly of Paramagnetic Prodrug and Photosensitizer Nanoassemblies for On-Demand Orthotopic Glioma Theranostics" on
.
in the research of targeted activated organic co-assembled nanodiagnostic and therapeutic probes for near-infrared fluorescence-magnetic resonance dual-modal imaging and chemotherapy-photodynamic combination therapy for brain gliomas in situ.
The relevant results were published in the internationally renowned academic journal ACS Nano on December 12, 2022 under the title "Controlling Disassembly of Paramagnetic Prodrug and Photosensitizer Nanoassemblies for On-Demand Orthotopic Glioma Theranostics" on
.
Based on the molecular co-assembly and controlled deassembly strategies, the research team synthesized αvβ3 integrin-targeted and glutathione-responsive paramagnetic near-infrared photosensitive probes (PPa-RGD) and camptothecin prodrugs (CPT-RGD), respectively.
By optimizing the co-assembly ratio of these two molecules, a co-assembled nanodiagnostic and therapeutic probe (Co-NP-RGD) with both physiological stability and synergistic therapy was prepared.
Figure 1).
After intravenous administration, Co-NP-RGD can effectively prolong blood circulation time compared with small molecule drugs, and with the help of a large number of cRGD targeting groups present on the surface, cross the blood-brain barrier (BBB), and target delivery to glioma cells in situ (U87MG and U251), on the one hand, an enhanced MRI contrast signal is generated for locating glioma in situ in the brain; On the other hand, under the action of high concentrations of glutathione in glioma cells, rapid disassembly occurs, and camptothecin original drug (CPT) and near-infrared photosensitizer (PPa) are released at the same time, thereby restoring photodynamic therapeutic function and generating enhanced near-infrared fluorescence signals for monitoring drug release and accumulation
。 In addition, the released small molecule porphyrin photosensitizer further binds to albumin in tumor cells, which can prolong the accumulation of photosensitizer molecules in tumor cells, while the camptothecin released at the same time can simultaneously inhibit the hypoxia-inducible factor HIF-1α, thereby improving the hypoxic environment in glioma tissue, thereby enhancing the photodynamic therapeutic effect
of deep glioma in situ 。 Under the guidance of dual-modal imaging signals, the in-situ glioma of mice was irradiated with a low-dose 690 nm laser (0.
2 W/cm2) to produce chemotherapy-photodynamic therapy synergistic therapy, which could effectively delay the growth of glioma in situ, prolong the survival of mice, and achieve efficient collaborative treatment of glioma in situ (Figure 2).
The molecular co-assembly and controlled deassembly strategies designed in this paper can be further applied to the construction of other tumor-targeted and activated nanodrugs to generate the combination therapeutic effect of cancer and promote the diagnosis and treatment
of cancer.
By optimizing the co-assembly ratio of these two molecules, a co-assembled nanodiagnostic and therapeutic probe (Co-NP-RGD) with both physiological stability and synergistic therapy was prepared.
Figure 1).
After intravenous administration, Co-NP-RGD can effectively prolong blood circulation time compared with small molecule drugs, and with the help of a large number of cRGD targeting groups present on the surface, cross the blood-brain barrier (BBB), and target delivery to glioma cells in situ (U87MG and U251), on the one hand, an enhanced MRI contrast signal is generated for locating glioma in situ in the brain; On the other hand, under the action of high concentrations of glutathione in glioma cells, rapid disassembly occurs, and camptothecin original drug (CPT) and near-infrared photosensitizer (PPa) are released at the same time, thereby restoring photodynamic therapeutic function and generating enhanced near-infrared fluorescence signals for monitoring drug release and accumulation
。 In addition, the released small molecule porphyrin photosensitizer further binds to albumin in tumor cells, which can prolong the accumulation of photosensitizer molecules in tumor cells, while the camptothecin released at the same time can simultaneously inhibit the hypoxia-inducible factor HIF-1α, thereby improving the hypoxic environment in glioma tissue, thereby enhancing the photodynamic therapeutic effect
of deep glioma in situ 。 Under the guidance of dual-modal imaging signals, the in-situ glioma of mice was irradiated with a low-dose 690 nm laser (0.
2 W/cm2) to produce chemotherapy-photodynamic therapy synergistic therapy, which could effectively delay the growth of glioma in situ, prolong the survival of mice, and achieve efficient collaborative treatment of glioma in situ (Figure 2).
The molecular co-assembly and controlled deassembly strategies designed in this paper can be further applied to the construction of other tumor-targeted and activated nanodrugs to generate the combination therapeutic effect of cancer and promote the diagnosis and treatment
of cancer.
Figure 1.
Structure and mechanism diagram of co-assembled nanodiagnostic and therapeutic probes
Structure and mechanism diagram of co-assembled nanodiagnostic and therapeutic probes
Figure 2.
Near-infrared fluorescence-MRI dual-modal imaging and chemotherapy-photodynamic combination therapy for in situ gliomas in mice
Near-infrared fluorescence-MRI dual-modal imaging and chemotherapy-photodynamic combination therapy for in situ gliomas in mice
An Ruibing, a postdoctoral fellow at Nanjing University and Liu Lingjun, a doctoral student jointly trained by China Pharmaceutical University, are the co-first authors of the paper, and Professor Ye Deju of Nanjing University and researcher Liu Hong of the Shanghai Institute of Materia Medica, Chinese Academy of Sciences are co-corresponding authors
.
This research has been supported
by the National Key Research and Development Program of China, the National Natural Science Foundation of China, the Natural Science Foundation of Jiangsu Province, the Excellence Program of Nanjing University, and the China Postdoctoral Science Foundation.
.
This research has been supported
by the National Key Research and Development Program of China, the National Natural Science Foundation of China, the Natural Science Foundation of Jiangsu Province, the Excellence Program of Nanjing University, and the China Postdoctoral Science Foundation.
Original link: https://pubs.
acs.
org/doi/10.
1021/acsnano.
2c07491
acs.
org/doi/10.
1021/acsnano.
2c07491
(Contributing department: Liu Hong Research Group; Contributor: Zhang Dan)
