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Open AccessArticle

Synthesis and Evaluation of 177Lu-DOTA-DN(PTX)-BN for Selective and Concomitant Radio and Drug—Therapeutic Effect on Breast Cancer Cells

Departamento de Materiales Radiactivos, Instituto Nacional de Investigaciones Nucleares, Carretera México-Toluca S/N, Ocoyoacac, Estado de México 52750, Mexico
Facultad de Química, Universidad Autónoma del Estado de México, Paseo Tollocan S/N, Toluca, Estado de México 50180, Mexico
Departamento de Bioprocesos, UPIBI-Instituto Politécnico Nacional, Ciudad de México 07340, Mexico
Author to whom correspondence should be addressed.
Polymers 2019, 11(10), 1572;
Received: 31 July 2019 / Revised: 1 September 2019 / Accepted: 7 September 2019 / Published: 27 September 2019
(This article belongs to the Special Issue Polymeric Colloidal Systems in Nanomedicine)
The peptide-receptor radionuclide therapy (PRRT) is a successful approach for selectively delivering radiation within tumor sites through specific recognition of radiolabeled peptides by overexpressed receptors on cancer cell surfaces. The efficacy of PRRT could be improved by using polymeric radio- and drug- therapy nanoparticles for a concomitant therapeutic effect on malignant cells. This research aimed to prepare and evaluate, a novel drug and radiation delivery nanosystem based on the 177Lu-labeled polyamidoamine (PAMAM) dendrimer (DN) loaded with paclitaxel (PTX) and functionalized on the surface with the Lys1Lys3(DOTA)-bombesin (BN) peptide for specific targeting to gastrin-releasing peptide receptors (GRPr) overexpressed on breast cancer cells. DN was first conjugated covalently to BN and DOTA (chemical moiety for lutetium-177 complexing) and subsequently loaded with PTX. The characterization by microscopic and spectroscopic techniques, in-vitro drug delivery tests as well as in in-vitro and in-vivo cellular uptake of 177Lu-DOTA-DN(PTX)-BN by T47D breast cancer cells (GRPr-positive), indicated the formation of an improved delivery nanosystem with target-specific recognition by GRPr. Results of the 177Lu-DOTA-DN(PTX)-BN effect on T47D cell viability (1.3%, compared with 10.9% of 177Lu-DOTA-DN-BN and 14.0% of DOTA-DN-(PTX)-BN) demonstrated the concomitant radiotherapeutic and chemotherapeutic properties of the polymeric nanosystem as a potential agent for the treatment of GRPr-positive tumors. View Full-Text
Keywords: polymeric nanosystems; dendrimers; radiotherapy; GRPr; paclitaxel; lutetium-177 polymeric nanosystems; dendrimers; radiotherapy; GRPr; paclitaxel; lutetium-177
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Gibbens-Bandala, B.; Morales-Avila, E.; Ferro-Flores, G.; Santos-Cuevas, C.; Luna-Gutiérrez, M.; Ramírez-Nava, G.; Ocampo-García, B. Synthesis and Evaluation of 177Lu-DOTA-DN(PTX)-BN for Selective and Concomitant Radio and Drug—Therapeutic Effect on Breast Cancer Cells. Polymers 2019, 11, 1572.

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