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Pharmaceutics
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Advanced Nanopharmaceuticals for Anticancer Therapy
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Advanced Nanopharmaceuticals for Anticancer Therapy

A special issue of Pharmaceutics (ISSN 1999-4923). This special issue belongs to the section "Drug Targeting and Design".

Deadline for manuscript submissions: closed (28 February 2025) | Viewed by 10790

Special Issue Editors

Dr. David Větvička

E-Mail Website
Guest Editor
Institute of Biophysics and Informatics, First Faculty of Medicine, Charles University, Salmovska 1, 120 00 Prague 2, Czech Republic
Interests: cancer immunotherapy; drug delivery; gene therapy; cancer immunology
Dr. Martin Studenovský

E-Mail Website
Guest Editor
Department of Biomedical Polymers, Institute of Macromolecular Chemistry CAS , Heyrovského nám. 2, 162 00 Prague 6, Czech Republic
Interests: nanotherapeutics; drug delivery; cancer; tumor

Special Issue Information

Dear Colleagues,

Over several decades, nanomedicines have achieved great advances in medical applications, especially in cancer therapy. Nano-sized drug delivery systems based on polymers, proteins, and lipids provide a flexible platform for binding therapeutic and/or diagnostic agents and delivering them to the target tissue. The smart design of these nanocarriers improves the delivery efficiency and site-specific controlled release of therapeutic agents. Recently, many studies have focused on (besides chemotherapy delivery) delivering cancer vaccines and immunotherapy and/or utilizing nanocarriers for diagnostic purposes such as delivering contrast agents for SPECT, PET, and MRI imaging or developing theranostic probes for image-guided resection.

Authors are kindly invited to submit original papers, reviews, and communications regarding recent advances in nanocarriers designed for anticancer drug delivery applications, diagnosis, their characterization, as well as in vitro, in vivo, clinical, or in silico testing to be published in this Special Issue of Pharmaceutics.

Dr. David Větvička
Dr. Martin Studenovský
Guest Editors

Manuscript Submission Information

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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

  • nanomaterials 
  • drug delivery systems 
  • cancer therapy 
  • polymer carriers 
  • liposomes 
  • theranostics 
  • imaging 
  • tumor targeting 
  • biomaterials

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Published Papers (6 papers)

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Research

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12 pages, 4149 KiB  
Article
Dendrimer-Derived Mimics of Host Defense Peptides Selectively Disrupt Cancer Cell Membranes for Melanoma Therapy
by Yusheng Qian, Danjing Yang, Xiangyu Lin, Chenyun Shen, Jieping Zhang, Jin Xu, Yan Zhao, Ling Zhu, Haoran Kong, Mingyu Zhang, Yueqian Zhu, Chuncai Zhou and Jing He
Pharmaceutics 2025, 17(3), 361; https://doi.org/10.3390/pharmaceutics17030361 - 12 Mar 2025
Viewed by 506
Abstract
Background: Melanoma is one of the most common malignancies, posing a significant health threat to patients, particularly in advanced stages due to its high aggressiveness. Chemotherapy agents with biocompatibility and low susceptibility to induce resistance are required for systematic management. Methods: [...] Read more.
Background: Melanoma is one of the most common malignancies, posing a significant health threat to patients, particularly in advanced stages due to its high aggressiveness. Chemotherapy agents with biocompatibility and low susceptibility to induce resistance are required for systematic management. Methods: Dendrimer-derived mimics (DMs) of host defense peptides (HDPs), which were constructed by a dendrimer core and optimized ratios of the hydrophobic arm, were used to treat A375 cells and HaCaT cells as the control. Live/dead staining, flow cytometry, and scanning electron microscopy (SEM) were conducted to analyze the anticancer mechanism. Mice with subcutaneous tumors were used to test the antitumor activity and toxicity in vivo. Results: DMs exhibited enhanced activity against A375 cells with remarkable selectivity, which mimics the action of natural HDPs and can cause damage to cell membranes. DMs can effectively inhibit solid tumor growth with minimal systemic toxicity and no adverse effects on healthy tissues. Conclusion: All the findings highlight DMs as promising anticancer candidates with significant potential for systemic melanoma therapy. Full article
(This article belongs to the Special Issue Advanced Nanopharmaceuticals for Anticancer Therapy)
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19 pages, 3013 KiB  
Article
Preparing a Liposome-Aided Drug Delivery System: The Entrapment and Release Profiles of Doxorubicin and 9-(N-Piperazinyl)-5-methyl-12(H)-quino [3,4-b][1,4]benzothiazinium Chloride with Human Serum Albumin
by Danuta Pentak, Violetta Kozik, Andrzej Zieba, Marlena Paździor-Heiske, Aleksandra Szymczyk, Josef Jampilek and Andrzej Bak
Pharmaceutics 2025, 17(2), 202; https://doi.org/10.3390/pharmaceutics17020202 - 6 Feb 2025
Viewed by 792
Abstract
Background/Objectives: The principal aim of this work was to prepare a liposomal drug delivery system based on the commercial drug doxorubicin (DOX) and a budding agent with promising anticancer activity, 9-(N-piperazinyl)-5-methyl-12(H)-quino [3,4-b][1,4]benzothiazinium chloride (9-PBThACl). Methods: A spectrophotometric methodology [...] Read more.
Background/Objectives: The principal aim of this work was to prepare a liposomal drug delivery system based on the commercial drug doxorubicin (DOX) and a budding agent with promising anticancer activity, 9-(N-piperazinyl)-5-methyl-12(H)-quino [3,4-b][1,4]benzothiazinium chloride (9-PBThACl). Methods: A spectrophotometric methodology was used to meticulously investigate the drug entrapment and release characteristics of the new liposomal complexes (L) based on dipalmitoylphosphatidylcholine (DPPC) with human serum albumin (HSA) and its defeated analog (dHSA). Results: The impact of the operational parameters (temperature and pH) on the liposome/drug(s)/(d)HSA, namely [LDPPC/9-PBThACl/DOX ]:(d)HSA] systems, as well as the polarity of the phospholipid bilayer, was examined. In order to compare the experimental findings, mathematical models were employed to specify the analytical factors controlling the process of drug release/potential drug release from liposomes. The observed variations in the drug encapsulation and release profiles were due to the combination of liposomal conjugates with human plasma protein. Conclusions: It was proven that changes in the environmental pH directly affect the percentage of drug entrapment in liposomes and the medicine release efficiency. Moreover, the grouping tendency of the liposomal combinations was investigated using a principal component analysis (PCA) and a hierarchical clustering analysis (HCA). Finally, an analysis of variance (ANOVA) confirmed the statistical impact of pH buffering and changing temperature factors on the drug release characteristics of liposomal conjugates. Full article
(This article belongs to the Special Issue Advanced Nanopharmaceuticals for Anticancer Therapy)
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16 pages, 3591 KiB  
Article
High Manganese Content of Lipid NanoMn (LNM) by Microfluidic Technology for Enhancing Anti-Tumor Immunity
by Jiawei Sun, Jingjing Gong, Lidong Gong, Chuanda Zhu, Longhao Li-Yang, Jingya Wang, Yuanyuan Yang, Shiming Zhang, Silu Liu, Ji-Jun Fu and Pengcheng Xu
Pharmaceutics 2024, 16(4), 556; https://doi.org/10.3390/pharmaceutics16040556 - 19 Apr 2024
Viewed by 1757
Abstract
Immunotherapy is a clinically effective method for treating tumors. Manganese can activate the cGAS-STING signaling pathway and induce an anti-tumor immune response. However, its efficacy is hindered by non-specific distribution and low uptake rates. In this study, we employed microfluidic technology to design [...] Read more.
Immunotherapy is a clinically effective method for treating tumors. Manganese can activate the cGAS-STING signaling pathway and induce an anti-tumor immune response. However, its efficacy is hindered by non-specific distribution and low uptake rates. In this study, we employed microfluidic technology to design and develop an innovative preparation process, resulting in the creation of a novel manganese lipid nanoparticle (LNM). The lipid manganese nanoparticle produced in this process boasts a high manganese payload, excellent stability, the capacity for large-scale production, and high batch repeatability. LNM has effectively demonstrated the ability to activate the cGAS-STING signaling pathway, induce the production of pro-inflammatory cytokines, and inhibit tumor development. Notably, LNM does not require combination chemotherapy drugs or other immune activators. Therefore, LNM presents a safe, straightforward, and efficient strategy for anti-tumor immune activation, with the potential for scalable production. Full article
(This article belongs to the Special Issue Advanced Nanopharmaceuticals for Anticancer Therapy)
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18 pages, 3311 KiB  
Article
Temoporfin-Conjugated Upconversion Nanoparticles for NIR-Induced Photodynamic Therapy: Studies with Pancreatic Adenocarcinoma Cells In Vitro and In Vivo
by Oleksandr Shapoval, David Větvička, Vitalii Patsula, Hana Engstová, Olga Kočková, Magdalena Konefał, Martina Kabešová and Daniel Horák
Pharmaceutics 2023, 15(12), 2694; https://doi.org/10.3390/pharmaceutics15122694 - 28 Nov 2023
Cited by 6 | Viewed by 1994
Abstract
Upconverting nanoparticles are interesting materials that have the potential for use in many applications ranging from solar energy harvesting to biosensing, light-triggered drug delivery, and photodynamic therapy (PDT). One of the main requirements for the particles is their surface modification, in our case [...] Read more.
Upconverting nanoparticles are interesting materials that have the potential for use in many applications ranging from solar energy harvesting to biosensing, light-triggered drug delivery, and photodynamic therapy (PDT). One of the main requirements for the particles is their surface modification, in our case using poly(methyl vinyl ether-alt-maleic acid) (PMVEMA) and temoporfin (THPC) photosensitizer to ensure the colloidal and chemical stability of the particles in aqueous media and the formation of singlet oxygen after NIR irradiation, respectively. Codoping of Fe2+, Yb3+, and Er3+ ions in the NaYF4 host induced upconversion emission of particles in the red region, which is dominant for achieving direct excitation of THPC. Novel monodisperse PMVEMA-coated upconversion NaYF4:Yb3+,Er3+,Fe2+ nanoparticles (UCNPs) with chemically bonded THPC were found to efficiently transfer energy and generate singlet oxygen. The cytotoxicity of the UCNPs was determined in the human pancreatic adenocarcinoma cell lines Capan-2, PANC-01, and PA-TU-8902. In vitro data demonstrated enhanced uptake of UCNP@PMVEMA-THPC particles by rat INS-1E insulinoma cells, followed by significant cell destruction after excitation with a 980 nm laser. Intratumoral administration of these nanoconjugates into a mouse model of human pancreatic adenocarcinoma caused extensive necrosis at the tumor site, followed by tumor suppression after NIR-induced PDT. In vitro and in vivo results thus suggest that this nanoconjugate is a promising candidate for NIR-induced PDT of cancer. Full article
(This article belongs to the Special Issue Advanced Nanopharmaceuticals for Anticancer Therapy)
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Review

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20 pages, 2486 KiB  
Review
Natural Killer-Based Therapy: A Prospective Thought for Cancer Treatment Related to Diversified Drug Delivery Pathways
by Jing Zang, Yijun Mei, Shiguo Zhu, Shaoping Yin, Nianping Feng, Tianyuan Ci and Yaqi Lyu
Pharmaceutics 2024, 16(7), 939; https://doi.org/10.3390/pharmaceutics16070939 - 14 Jul 2024
Viewed by 1759
Abstract
Immunotherapy has been a research hotspot due to its low side effects, long-lasting efficacy, and wide anti-tumor spectrum. Recently, NK cell-based immunotherapy has gained broad attention for its unique immunological character of tumor identification and eradication and low risk of graft-versus-host disease and [...] Read more.
Immunotherapy has been a research hotspot due to its low side effects, long-lasting efficacy, and wide anti-tumor spectrum. Recently, NK cell-based immunotherapy has gained broad attention for its unique immunological character of tumor identification and eradication and low risk of graft-versus-host disease and cytokine storm. With the cooperation of a drug delivery system (DDS), NK cells activate tumoricidal activity by adjusting the balance of the activating and inhibitory signals on their surface after drug-loaded DDS administration. Moreover, NK cells or NK-derived exosomes can also be applied as drug carriers for distinct modification to promote NK activation and exert anti-tumor effects. In this review, we first introduce the source and classification of NK cells and describe the common activating and inhibitory receptors on their surface. Then, we summarize the strategies for activating NK cells in vivo through various DDSs. Finally, the application prospects of NK cells in tumor immunotherapy are also discussed. Full article
(This article belongs to the Special Issue Advanced Nanopharmaceuticals for Anticancer Therapy)
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22 pages, 5386 KiB  
Review
Recent Progress of Copper-Based Nanomaterials in Tumor-Targeted Photothermal Therapy/Photodynamic Therapy
by Xiqian Zhuo, Zhongshan Liu, Reyida Aishajiang, Tiejun Wang and Duo Yu
Pharmaceutics 2023, 15(9), 2293; https://doi.org/10.3390/pharmaceutics15092293 - 7 Sep 2023
Cited by 10 | Viewed by 2958
Abstract
Nanotechnology, an emerging and promising therapeutic tool, may improve the effectiveness of phototherapy (PT) in antitumor therapy because of the development of nanomaterials (NMs) with light-absorbing properties. The tumor-targeted PTs, such as photothermal therapy (PTT) and photodynamic therapy (PDT), transform light energy into [...] Read more.
Nanotechnology, an emerging and promising therapeutic tool, may improve the effectiveness of phototherapy (PT) in antitumor therapy because of the development of nanomaterials (NMs) with light-absorbing properties. The tumor-targeted PTs, such as photothermal therapy (PTT) and photodynamic therapy (PDT), transform light energy into heat and produce reactive oxygen species (ROS) that accumulate at the tumor site. The increase in ROS levels induces oxidative stress (OS) during carcinogenesis and disease development. Because of the localized surface plasmon resonance (LSPR) feature of copper (Cu), a vital trace element in the human body, Cu-based NMs can exhibit good near-infrared (NIR) absorption and excellent photothermal properties. In the tumor microenvironment (TME), Cu2+ combines with H2O2 to produce O2 that is reduced to Cu1+ by glutathione (GSH), causing a Fenton-like reaction that reduces tumor hypoxia and simultaneously generates ROS to eliminate tumor cells in conjunction with PTT/PDT. Compared with other therapeutic modalities, PTT/PDT can precisely target tumor location to kill tumor cells. Moreover, multiple treatment modalities can be combined with PTT/PDT to treat a tumor using Cu-based NMs. Herein, we reviewed and briefly summarized the mechanisms of actions of tumor-targeted PTT/PDT and the role of Cu, generated from Cu-based NMs, in PTs. Furthermore, we described the Cu-based NMs used in PTT/PDT applications. Full article
(This article belongs to the Special Issue Advanced Nanopharmaceuticals for Anticancer Therapy)
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