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Volume 17
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10.3390/pharmaceutics17020164
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This is an early access version, the complete PDF, HTML, and XML versions will be available soon.
Article

Development, Characterization, and Evaluation of Chi-Tn mAb-Functionalized DOTAP-PLGA Hybrid Nanoparticles Loaded with Docetaxel for Lung Cancer Therapy

by
Analía Castro
1,†,
Álvaro Pittini
2,3,†,
Nora Berois
2,
Ricardo Faccio
1,4,
Pablo Miranda
1,
Álvaro W. Mombrú
1,4,
Eduardo Osinaga
2,3 and
Helena Pardo
1,4,*
1
Centro NanoMat, Instituto Polo Tecnológico de Pando, Facultad de Química, Universidad de la República, Canelones 91000, Uruguay
2
Laboratorio de Glicobiología e Inmunología Tumoral, Institut Pasteur de Montevideo, Montevideo 11400, Uruguay
3
Departamento de Inmunobiología, Facultad de Medicina, Universidad de la República, Montevideo 11800, Uruguay
4
Cátedra de Física, Facultad de Química, DETEMA, Universidad de la República, Montevideo 11800, Uruguay
*
Author to whom correspondence should be addressed.
†
These authors contributed equally to this work.
Pharmaceutics 2025, 17(2), 164; https://doi.org/10.3390/pharmaceutics17020164
Submission received: 26 November 2024 / Revised: 13 January 2025 / Accepted: 21 January 2025 / Published: 25 January 2025
(This article belongs to the Section Nanomedicine and Nanotechnology)
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Abstract

Background/Objectives: The focus of this study was to prepare and characterize docetaxel (DCX)-loaded lipid/polymer hybrid nanoparticles (LPHNps) functionalized with the monoclonal antibody (mAb) Chi-Tn for a potential active targeting approach in lung cancer treatment. Methods: We synthesized DOTAP-PLGA hybrid nanoparticles loaded with DCX and functionalized them with Chi-Tn mAb through a biotin–avidin approach. The physicochemical characterization involved dynamic light scattering, transmission electron microscopy, Raman spectroscopy, and atomic force microscopy. The in vitro and in vivo evaluations encompassed uptake studies, cell viability tests, and the assessment of tumor growth control in a lung cancer model. Results: The nanoparticles featured a hydrophobic PLGA core with 99.9% DCX encapsulation efficiency, surrounded by a DOTAP lipid shell ensuring colloidal stability with a high positive surface charge. The incorporation of PEGylated lipids on their surface helps evade the immune system and facilitate Chi-Tn mAb attachment. The resulting nanoparticles exhibit a spherical shape with monodisperse particle sizes averaging 250 nm, and demonstrate sustained drug release. In vitro uptake studies and viability assays conducted in A549 cancer cells show that the Chi-Tn mAb enhances nanoparticle internalization and significantly reduces cell viability. In vivo studies demonstrate a notable reduction in tumor volume and an increased survival rate in the A549 tumor xenograft mice model when DCX was encapsulated in nanoparticles and targeted with Chi-Tn mAb in comparison to the free drug. Conclusions: Therefore, Chi-Tn-functionalized LPHNps hold promise as carriers for actively targeting DCX to Tn-expressing carcinomas.
Keywords: lipid polymer hybrid nanoparticles; active targeting; cancer treatment; Tn antigen; PLGA; DOTAP lipid polymer hybrid nanoparticles; active targeting; cancer treatment; Tn antigen; PLGA; DOTAP
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MDPI and ACS Style

Castro, A.; Pittini, Á.; Berois, N.; Faccio, R.; Miranda, P.; Mombrú, Á.W.; Osinaga, E.; Pardo, H. Development, Characterization, and Evaluation of Chi-Tn mAb-Functionalized DOTAP-PLGA Hybrid Nanoparticles Loaded with Docetaxel for Lung Cancer Therapy. Pharmaceutics 2025, 17, 164. https://doi.org/10.3390/pharmaceutics17020164

AMA Style

Castro A, Pittini Á, Berois N, Faccio R, Miranda P, Mombrú ÁW, Osinaga E, Pardo H. Development, Characterization, and Evaluation of Chi-Tn mAb-Functionalized DOTAP-PLGA Hybrid Nanoparticles Loaded with Docetaxel for Lung Cancer Therapy. Pharmaceutics. 2025; 17(2):164. https://doi.org/10.3390/pharmaceutics17020164

Chicago/Turabian Style

Castro, Analía, Álvaro Pittini, Nora Berois, Ricardo Faccio, Pablo Miranda, Álvaro W. Mombrú, Eduardo Osinaga, and Helena Pardo. 2025. "Development, Characterization, and Evaluation of Chi-Tn mAb-Functionalized DOTAP-PLGA Hybrid Nanoparticles Loaded with Docetaxel for Lung Cancer Therapy" Pharmaceutics 17, no. 2: 164. https://doi.org/10.3390/pharmaceutics17020164

APA Style

Castro, A., Pittini, Á., Berois, N., Faccio, R., Miranda, P., Mombrú, Á. W., Osinaga, E., & Pardo, H. (2025). Development, Characterization, and Evaluation of Chi-Tn mAb-Functionalized DOTAP-PLGA Hybrid Nanoparticles Loaded with Docetaxel for Lung Cancer Therapy. Pharmaceutics, 17(2), 164. https://doi.org/10.3390/pharmaceutics17020164

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