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Pharmaceutics
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Application of PLGA Nanoparticles in Cancer Therapy
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Application of PLGA Nanoparticles in Cancer Therapy

A special issue of Pharmaceutics (ISSN 1999-4923). This special issue belongs to the section "Nanomedicine and Nanotechnology".

Deadline for manuscript submissions: closed (31 December 2025) | Viewed by 3160

Special Issue Editor

Dr. Daniele Rubert Nogueira-Librelotto

E-Mail Website
Guest Editor
Department of Industrial Pharmacy, Federal University of Santa Maria, Santa Maria, RS, Brazil
Interests: nanotechnology; pH-responsive drug delivery system; in vitro methods; cell culture; antitumor activity; drug targeting; drug quality control; liquid chromatography; toxicology
Special Issues, Collections and Topics in MDPI journals

Special Issue Information

Dear Colleagues,

Pharmaceutics is excited to present a Special Issue focused on the “Application of PLGA Nanoparticles in Cancer Therapy”.

Poly(lactic-co-glycolic acid) (PLGA) nanoparticles are at the forefront of cancer treatment innovations due to their biocompatibility, biodegradability, and ability to encapsulate a wide range of therapeutic agents. These nanoparticles enhance the targeted delivery and controlled release of anticancer drugs, reducing side effects and improving treatment efficacy. The scientific background highlights PLGA's versatility in overcoming biological barriers and enhancing drug solubility. This Special Issue aims to explore the latest advancements in PLGA nanoparticle research, focusing on formulation strategies, targeting mechanisms, and clinical applications. Researchers are invited to contribute studies on novel PLGA-based therapies, characterization techniques, and the integration of imaging for theranostic applications. By gathering cutting-edge research, this Special Issue seeks to provide a comprehensive overview of the potential and future directions of PLGA nanoparticles in cancer therapy.

In this Special Issue, original research articles and reviews are welcome to be submitted. We look forward to receiving your contributions.

Dr. Daniele Rubert Nogueira-Librelotto
Guest Editor

Manuscript Submission Information

Manuscripts should be submitted online at www.mdpi.com by registering and logging in to this website. Once you are registered, click here to go to the submission form. Manuscripts can be submitted until the deadline. All submissions that pass pre-check are peer-reviewed. Accepted papers will be published continuously in the journal (as soon as accepted) and will be listed together on the special issue website. Research articles, review articles as well as short communications are invited. For planned papers, a title and short abstract (about 250 words) can be sent to the Editorial Office for assessment.

Submitted manuscripts should not have been published previously, nor be under consideration for publication elsewhere (except conference proceedings papers). All manuscripts are thoroughly refereed through a single-blind peer-review process. A guide for authors and other relevant information for submission of manuscripts is available on the Instructions for Authors page. Pharmaceutics is an international peer-reviewed open access monthly journal published by MDPI.

Please visit the Instructions for Authors page before submitting a manuscript. The Article Processing Charge (APC) for publication in this open access journal is 2900 CHF (Swiss Francs). Submitted papers should be well formatted and use good English. Authors may use MDPI's English editing service prior to publication or during author revisions.

Keywords

  • PLGA nanoparticles
  • cancer therapy
  • drug delivery
  • biocompatibility
  • controlled release
  • targeted therapy
  • theranostics
  • formulation strategies

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Published Papers (3 papers)

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Research

29 pages, 4588 KB  
Article
Polymeric PLGA Nanoparticles Loaded with Acalypha monostachya Leaf Hexane Extract: A Novel Strategy for Antineoplastic Activity
by Gloria A. Guillén-Meléndez, Carlos R. Montes-de-Oca-Saucedo, Raymundo A. Pérez-Hernández, Priscila Sepúlveda, Flavio F. Contreras-Torres, Rocío Castro-Ríos, Uziel Castillo-Velázquez, María de Jesús Loera-Arias, Humberto Rodríguez-Rocha, Joel H. Elizondo-Luevano, Magdalena Escobar-Saucedo, Juan C. Arellano-Barrientos, Odila Saucedo-Cárdenas, Abelardo Chávez-Montes and Adolfo Soto-Domínguez
Pharmaceutics 2026, 18(2), 274; https://doi.org/10.3390/pharmaceutics18020274 - 23 Feb 2026
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Abstract
Background/Objectives: Acalypha monostachya is used in rural communities in Mexico as a traditional remedy for cancer, and we previously observed cytotoxic activity of its extracts against MDA-MB-231 and HeLa cells. Methods: Because lipophilic plant fractions disperse poorly in water, we encapsulated [...] Read more.
Background/Objectives: Acalypha monostachya is used in rural communities in Mexico as a traditional remedy for cancer, and we previously observed cytotoxic activity of its extracts against MDA-MB-231 and HeLa cells. Methods: Because lipophilic plant fractions disperse poorly in water, we encapsulated the hexane leaf extract (LHE) of A. monostachya in poly (lactic-co-glycolic acid) (PLGA) nanoparticles prepared by nanoprecipitation, characterized them physicochemically, and evaluated their in vitro cytotoxicity. Results: The selected extract/polymer ratio (5/50, w/w) produced nanoparticles with a mean diameter of 131.4 ± 0.5 nm and a PDI of 0.122 ± 0.028, with an encapsulation efficiency of 92.03% and a loading of 8.43%. We next evaluated cytotoxicity by MTT after 24 h in HeLa and MDA-MB-231 cells and compared the response with non-tumorigenic HaCaT keratinocytes. Encapsulation increased potency relative to free LHE, yielding IC50 values of 30 µg/mL (HeLa), 60 µg/mL (MDA-MB-231), and 95 µg/mL (HaCaT). These values corresponded to selectivity indices of 3.2 (HaCaT/HeLa) and 1.6 (HaCaT/MDA-MB-231). Conclusions: Overall, encapsulation of LHE in PLGA nanoparticles yields an aqueous PLGA nanoparticle suspension and is associated with improved in vitro potency while maintaining measurable selectivity against cancer cells. Full article
(This article belongs to the Special Issue Application of PLGA Nanoparticles in Cancer Therapy)
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26 pages, 3111 KB  
Article
Preclinical Investigation of PLGA Nanocapsules and Nanostructured Lipid Carriers for Organoselenium Delivery: Comparative In Vitro Toxicological Profile and Anticancer Insights
by Bianca Costa Maia-do-Amaral, Taís Baldissera Pieta, Luisa Fantoni Zanon, Gabriele Cogo Carneosso, Laísa Pes Nascimento, Nayra Salazar Rocha, Bruna Fracari do Nascimento, Letícia Bueno Macedo, Tielle Moraes de Almeida, Oscar Endrigo Dorneles Rodrigues, Scheila Rezende Schaffazick, Clarice Madalena Bueno Rolim and Daniele Rubert Nogueira-Librelotto
Pharmaceutics 2026, 18(1), 57; https://doi.org/10.3390/pharmaceutics18010057 - 31 Dec 2025
Viewed by 930
Abstract
Background/Objectives: Cancer is a major health concern involving abnormal cell growth. Combining anticancer agents can enhance efficacy and overcome resistance by targeting multiple pathways and creating synergistic effects. Methods: This study used in silico approaches to evaluate the physicochemical and pharmacokinetic profiles of [...] Read more.
Background/Objectives: Cancer is a major health concern involving abnormal cell growth. Combining anticancer agents can enhance efficacy and overcome resistance by targeting multiple pathways and creating synergistic effects. Methods: This study used in silico approaches to evaluate the physicochemical and pharmacokinetic profiles of the innovative organoselenium nucleoside analog Di3a, followed by the design of two nanocarriers. Di3a-loaded PLGA nanocapsules and nanostructured lipid carriers based on compritol were prepared and evaluated alone and combined with doxorubicin (DOX) and docetaxel (DTX) for a synergistic effect. Results: Di3a subtly violated some of Lipinski’s rules, but still showed suitable pharmacokinetic properties. Both nanoparticles presented nanometric size, negative zeta potential and polydispersity index values < 0.20. Hemolysis assay suggested a pH-dependent pattern conferred by the surfactant 77KL, and evidenced the biocompatibility of the formulations, aligning with the results observed in the nontumor L929 cell line. The lack of drug release studies under varying pH conditions constitutes a limitation and warrants further investigation to validate the pH-responsive properties of the nanocarriers. MTT assay revealed that both formulations exhibited significant cytotoxic effects in the A549 cell line. However, neither formulation exhibited marked toxicity toward NCI/ADR-RES, a resistant tumor cell line. Conversely, when combined with DOX or DTX, the treatments were able to sensitize these resistant cells, achieving expressive synergistic antitumor activity. Conclusions: Despite the limitations in the in silico studies, the study highlights the potential of combining the proposed nanocarriers with conventional antitumor drugs to sensitize multidrug-resistant cancer cells and emphasizes the safety of the developed nanoformulations. Full article
(This article belongs to the Special Issue Application of PLGA Nanoparticles in Cancer Therapy)
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12 pages, 1573 KB  
Article
Enhancing the Solubility and Antibacterial Efficacy of Sulfamethoxazole by Incorporating Functionalized PLGA and Graphene Oxide Nanoparticles into the Crystal Structure
by Mohammad Saiful Islam, Indrani Gupta, Edgardo T. Farinas and Somenath Mitra
Pharmaceutics 2025, 17(11), 1460; https://doi.org/10.3390/pharmaceutics17111460 - 12 Nov 2025
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Abstract
Background/Objectives: The widespread use of sulfamethoxazole (SMX) has led to increasing antibiotic resistance, and there is a need for improved formulations to enhance its therapeutic effectiveness. In this study, we investigated the biocidal potential of SMX composite crystals incorporated with functionalized poly(lactic-co-glycolic [...] Read more.
Background/Objectives: The widespread use of sulfamethoxazole (SMX) has led to increasing antibiotic resistance, and there is a need for improved formulations to enhance its therapeutic effectiveness. In this study, we investigated the biocidal potential of SMX composite crystals incorporated with functionalized poly(lactic-co-glycolic acid) (nfPLGA) and nano-graphene oxide (nGO). Methods: The composites, namely SMX-nfPLGA and SMX-nGO, were synthesized via antisolvent precipitation and evaluated using Kirby–Bauer disk diffusion assays. Results: Incorporation of nfPLGA and nGO significantly improved SMX solubility, increasing it from 0.029 mg/mL to 0.058 mg/mL and 0.063 mg/mL, respectively. Additionally, the log partition coefficient (log P or Kw) also improved from 1.4 to 0.86 for nGO and 0.92 for nfPLGA composites. Both formulations exhibited improved antibacterial activity with distinct time-dependent bactericidal effects. Compared to pure SMX, the SMX-nfPLGA showed 60% and 53% greater bacterial inhibition at concentrations of 50 mg/mL and 100 mg/mL, respectively. Although SMX-nGO was slightly less potent, it still surpassed pure SMX, with 50% and 33% higher inhibition at the same concentrations. Conclusions: Importantly, neither nfPLGA nor nGO showed any biocidal effects, confirming that the observed enhancement was due to improved SMX solubility caused by their incorporation. These findings suggest that embedding solubility-enhancing nanoparticles into the existing crystal structure of the antibiotic is a promising strategy for enhancing the effectiveness. Full article
(This article belongs to the Special Issue Application of PLGA Nanoparticles in Cancer Therapy)
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