Synthesis and biological assessment of folate-accepted developer 99mTc-DTPA-folate-polymer

Chen, Fei; Shao, Kejing; Zhu, Bao Li; Mengjun, Jiang

doi:10.1016/j.bmcl.2016.03.084

Cited by 3 publications

(2 citation statements)

References 26 publications

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“…There is an increasing number of studies on FA-enabled targeted delivery of radionuclides, fluorescent dyes, chemotherapeutics, liposomes, and gene vectors. Vintafolide was one of the most promising folate-conjugated low-molecular-weight chemotherapeutics, in which the potent microtubule-destabilizing agent vinca alkaloid desacetylvinblastine monohydrazide is conjugated with FA to target cancer cells via FR-α-mediated endocytosis. − Early clinical evidence suggested good tolerance and enhanced antitumor effect of vintafolide in combination with PEGylated doxorubicin liposomes in women with advanced ovarian cancer (clinical trials NCT00722592 and NCT00507741). , However, the subsequent phase III trial did not meet the prespecified criteria for required progression-free survival (PFS) improvement, and resistance against vintafolide occurred (clinical trial NCT01170650). , Most of the clinical studies of FA-enabled targeting failed with the exception of some FA-fluorescent dyes (clinical trials NCT01996072 and NCT01994369) and FA-radionuclide conjugates (clinical trials NCT00003763, NCT01999738, and NCT00722592) still active for imaging. − …”

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confidence: 99%

Interrogation of Folic Acid-Functionalized Nanomedicines: The Regulatory Roles of Plasma Proteins Reexamined

et al. 2020

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Folic acid (FA) has been extensively exploited to facilitate targeted delivery of nanomedicines by recognizing the folate receptor-α (FR-α) overexpressed in many human cancers. Unfortunately, none have been approved for clinical use yet. Here we reveal that FA functionalization induces heavy natural IgM absorption on the liposomal surface, depriving FA of receptor recognition and accelerating complement activation in vivo. FA functionalization does not enhance distribution of liposomes in FR-α-overexpressed tumors in comparison to plain liposomes (without FA), but leads to aggravated capture of liposomes by macrophages in the tumor, liver, and spleen. In addition, FA-functionalized polymeric nanoparticles are also vulnerable to natural IgM absorption. This work highlights the pivotal roles of natural IgM in regulating in vivo delivery of FA-functionalized nanomedicines. Due to the prevalent association of immune disorders and varying levels of immunoglobulins with cancer patients, extraordinary cautiousness is urged for clinical translation of FA-enabled targeted delivery systems.

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confidence: 99%

Interrogation of Folic Acid-Functionalized Nanomedicines: The Regulatory Roles of Plasma Proteins Reexamined

et al. 2020

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“…Therefore, 99m Tc complexes are often used in the clinical diagnosis of some diseases, accounting for more than 85% of nuclear medicine SPECT images [ 8 , 9 ]. Recently, a number of 99m Tc-labeled folate-based conjugates have been developed as potential folate receptor imaging agents [ 10 , 11 , 12 , 13 , 14 ]. Although these complexes have shown high tumor uptake, most of the reported radiopharmaceuticals targeting folate receptor require purification by high-performance liquid chromatography (HPLC), thus limiting their application in clinical practice.…”

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confidence: 99%

Preparation and Evaluation of Novel Folate Isonitrile 99mTc Complexes as Potential Tumor Imaging Agents to Target Folate Receptors

et al. 2021

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In order to seek novel technetium-99m folate receptor-targeting agents, two folate derivatives (CN5FA and CNPFA) were synthesized and radiolabeled to obtain [99mTc]Tc-CN5FA and [99mTc]Tc-CNPFA complexes, which exhibited high radiochemical purity (>95%) without purification, hydrophilicity, and good stability in vitro. The KB cell competitive binding experiments indicated that [99mTc]Tc-CN5FA and [99mTc]Tc-CNPFA had specificity to folate receptor. Biodistribution studies in KB tumor-bearing mice illustrated that [99mTc]Tc-CN5FA and [99mTc]Tc-CNPFA had specific tumor uptake. Compared with [99mTc]Tc-CN5FA, the tumor/muscle ratios of [99mTc]Tc-CNPFA were higher, resulting in a better SPECT/CT imaging background. According to the results, the two 99mTc complexes have potential as tumor imaging agents to target folate receptors.

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Imaging, biodistribution and in vitro study of smart 99mTc-PAMAM G4 dendrimer as novel nano-complex

Narmani

Yavari

Mohammadnejad

2017

Colloids and Surfaces B: Biointerfaces

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Synthesis and biological assessment of folate-accepted developer 99mTc-DTPA-folate-polymer

Cited by 3 publications

References 26 publications

Interrogation of Folic Acid-Functionalized Nanomedicines: The Regulatory Roles of Plasma Proteins Reexamined

Interrogation of Folic Acid-Functionalized Nanomedicines: The Regulatory Roles of Plasma Proteins Reexamined

Preparation and Evaluation of Novel Folate Isonitrile 99mTc Complexes as Potential Tumor Imaging Agents to Target Folate Receptors

Imaging, biodistribution and in vitro study of smart 99mTc-PAMAM G4 dendrimer as novel nano-complex

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