Preclinical Evaluation of NHS-Activated Gold Nanoparticles Functionalized with Bombesin or Neurotensin-Like Peptides for Targeting Colon and Prostate Tumours

Chilug, Livia Elena; Niculae, Dana; Leonte, Radu A.; Nan, Alexandrina; Turcu, Rodica; Mustăciosu, Cosmin Cătălin; Serban, Radu M.; Lavric, Vasile; Manda, Gina

doi:10.3390/molecules25153363

Cited by 13 publications

(13 citation statements)

References 31 publications

(103 reference statements)

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“…These short peptide chains can also be further engineered to provide convenient means of condensation with nanoparticles [22][23][24], which will be discussed in more detail in the next subchapter. Frequently, the ligand is combined with poly(ethylene glycol) (PEG) to improve the pharmacokinetics of the construct and minimize the reticuloendothelial system uptake upon in vivo administration [25,26].…”

Section: Targeting Ligandsmentioning

confidence: 99%

“…This approach led to the successful targeting of GRPR-positive breast cancer and Ehrlich tumor cells [71][72][73]. [35] polymeric micelles glioma Coumarin-6 Camptothecin (CPT) [61] prostate cancer Monomethyl auristatin F (MMAF) [65] elastin-like micelles prostate cancer - [63] Docetaxel (DTX) [74] nanostructured lipid carriers lung cancer Doxorubicin (DOX) [17] solid lipid nanoparticles breast cancer Doxorubicin (DOX) [59] PLGA nanoparticles breast cancer Docetaxel (DTX) [14] prostate cancer Docetaxel (DTX) [75] gold nanoparticles cervical cancer RAF peptide analog (Ac-Cys-Ahx-RAF) [69] prostate cancer 99m Tc [24] 99m Tc, 177 Lu [31] - [76] Gallic acid (GA) [47] prostate cancer, colon cancer 68 Ga [25] gold nanorods breast cancer Photothermal therapy -use of NIR laser irradiation [39] prostate cancer Heat-labile cytotoxic free radical donor -AIPH [77] graphene oxide glioblastoma Magnetic targeting, doxorubicin (DOX), NIR laser irradiation…”

Section: Ligand Incorporationmentioning

confidence: 99%

“…Different AuNP-based nanocarriers were synthesized and examined in treating both prostate and colon cancers by Chilug et al They used engineered bombesin and neurotensin-like peptides and checked how these ligands bind to both types of tumors [25]. One of the targeting moieties was [ 68 Ga]Ga-DOTA-PEG(4)-BBN(7-14), which, together with its AuNPs counterpart, was subjected to in vitro and in vivo tests.…”

Section: Gold Nanomaterialsmentioning

confidence: 99%

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Nanostrategies for Therapeutic and Diagnostic Targeting of Gastrin-Releasing Peptide Receptor

Rurarz¹,

Bukowczyk²,

Gibka³

et al. 2023

Preprint

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Advances in nanomedicine bring the attention of researchers to the molecular targets which can play a major role in the development of novel therapeutic and diagnostic modalities for cancer management. The choice of a proper molecular target can decide on the efficacy of the treatment and endorse the personalized medicine approach. Gastrin-releasing peptide receptor (GRPR) is a G-protein-coupled membrane receptor, well known to be overexpressed in numerous malignancies including pancreatic, prostate, breast, lung, colon, cervical and gastrointestinal cancers. Therefore, many research groups express a deep interest in targeting GRPR with their nanoformulations. A broad spectrum of the GRPR ligands has been described in the literature, which allows tuning of the properties of the final formulation, particularly in the field of the ligand affinity to the receptor and internalization possibilities. Hereby the recent advances in the field of applications of various nanoplatforms which are able to reach the GRPR expressing cells are reviewed.

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Section: Targeting Ligandsmentioning

confidence: 99%

Section: Ligand Incorporationmentioning

confidence: 99%

Section: Gold Nanomaterialsmentioning

confidence: 99%

See 1 more Smart Citation

Nanostrategies for Therapeutic and Diagnostic Targeting of Gastrin-Releasing Peptide Receptor

Rurarz¹,

Bukowczyk²,

Gibka³

et al. 2023

Preprint

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“…This approach aims to find the molecule with high specificity for a tumour cell type, and then properly attach to it an imaging or a treatment radioisotope, according to its use. One molecule of this kind is the neurotensin (NT) for which it has been previously demonstrated to have the potential to target tumours such as: pancreatic cancer [ 1 , 2 , 3 ], colorectal cancer [ 4 , 5 , 6 ], lung cancer [ 6 ], prostate cancer [ 7 , 8 ] or breast cancer [ 9 ]. Neurotensin is a tridecapeptide (pGlu-Leu-Tyr-Glu-Asn-Lys-Pro-Arg-Arg-Pro-Tyr-Ile-Leu) that acts as a neurotransmitter or neuromodulator in the central nervous system (CNS).…”

Section: Introductionmentioning

confidence: 99%

“…Furthermore, 68 Ga and 177 Lu are two radioisotopes which can be chelated with good results to a variety of biomolecules; this allowing to approach more diseases than e.g., 99m Tc. Therefore, 68 Ga has gained increasing importance in clinical research in the last 25 years [ 13 ] as a PET imaging agent, exhibiting more suitable characteristics than other PET radioisotopes in terms of higher detection resolution and sensitivity (T 1/2 = 67.83 min, E β+ = 1.899 MeV) [ 8 , 14 ], a lower or comparative effective dose to that of 18 F or 99m Tc (2.3 mSv for [ 68 Ga]Ga-DOTA-TOC per PET scan, compared to 5.6 mSv for [ 18 F]FDG [ 15 ]) and fast data acquisition. It decays by β + emission (88.88%) and electronic capture (11.11%) to stable 68 Zn [ 14 ].…”

Section: Introductionmentioning

confidence: 99%

Preparation and Preliminary Evaluation of Neurotensin Radiolabelled with 68Ga and 177Lu as Potential Theranostic Agent for Colon Cancer

et al. 2021

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The neurotensin is a tridecapeptide involved in the proliferation of colon cancer, the overexpression of neurotensin receptors occurring at an early stage development of many tumours. Targeting neurotensin receptors by using the same biological active molecule is an effective approach for both imaging quantification and treatment. The present work aimed to demonstrate the ability of radiolabelled neurotensin to specifically target colon cancer cells, and substantiate its usefulness in targeted imaging and radiotherapy, depending on the emission of the coupled radioisotope. Syntheses of 68Ga–DOTA–NT and 177Lu–DOTA–NT were developed to obtain a level of quality suitable for preclinical use with consistent high synthesis yields. Radiochemical purity meets the pharmaceutical requirements, and it is maintained 4 h for 68Ga–DOTA–NT and 48 h for 177Lu–DOTA–NT. Extensive in vitro studies were conducted to assess the uptake and retention of 68Ga–DOTA–NT, the amount of non-specific binding of neurotensin and the effect of 177Lu–DOTA–NT on HT–29 cells. In vivo biodistribution of 68Ga–DOTA–NT revealed significant uptake at the tumour site, along with fast clearance evidenced by decreasing activity in kidneys and blood after 60 min p.i. 177Lu–DOTA–NT exhibited similar uptake in the tumour, but also a significant uptake at 14 days p.i. in the bone marrow was reported. These results successfully demonstrated the potential of neurotensin to deliver imaging/therapeutic 68Ga/177Lu radioisotopes pair, but also the need for further evaluation of the possible radiotoxicity effects on the liver, kidneys or bone marrow.

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Assessment of chromatography separation parameters in the quality control of copper-64-labeled neurotensin-like peptides

Tudoroiu-Cornoiu,

Chilug,

Cocioabă

et al. 2024

J Radioanal Nucl Chem

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In recent years, research on the Cu-64 effects on malignant tumours has increased, leading to the development of radiopharmaceuticals with higher selectivity, aiming to target tumour cells while preserving healthy body cells. This work aims to assess the quality of two DOTA-derivatized neuropeptides, NMN and NT (8-13) radiolabelled with Cu-64. An improved analytical radio-HPLC method was developed to evaluate the radiochemical purity and stability. The radiochemical purity is > 99.95% for both 64Cu-DOTA-NMN and 64Cu-DOTA-NT (8-13), the radiolabelled molecules being stable for 72 h after synthesis.

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Preclinical Evaluation of NHS-Activated Gold Nanoparticles Functionalized with Bombesin or Neurotensin-Like Peptides for Targeting Colon and Prostate Tumours

Cited by 13 publications

References 31 publications

Nanostrategies for Therapeutic and Diagnostic Targeting of Gastrin-Releasing Peptide Receptor

Nanostrategies for Therapeutic and Diagnostic Targeting of Gastrin-Releasing Peptide Receptor

Preparation and Preliminary Evaluation of Neurotensin Radiolabelled with 68Ga and 177Lu as Potential Theranostic Agent for Colon Cancer

Assessment of chromatography separation parameters in the quality control of copper-64-labeled neurotensin-like peptides

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