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Pharmaceutics
Special Issues
Anti-Cancer Drug Delivery Systems
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Anti-Cancer Drug Delivery Systems

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

Deadline for manuscript submissions: 20 February 2025 | Viewed by 10113

Special Issue Editor

Dr. Karolina Kędra

E-Mail Website
Guest Editor
Institute of Physical Chemistry, Polish Academy of Sciences, 44/52 Kasprzaka St., 01-224 Warsaw, Poland
Interests: microcalorimetry of biological macromolecules; differential scanning calorimetry; biomolecule structure, stability and interactions; physico-chemical properties of dispersed systems; drug delivery systems

Special Issue Information

Dear Colleagues,

We are pleased to invite you to this Special Issue of Pharmaceutics, dedicated to anti-cancer drug delivery systems. Cancer diseases are still one of the main problems of modern medicine and pharmacy. Therefore, one of the most important areas of the science as well as technology of pharmaceutics and biopharmaceutics is the development of innovative anti-cancer DDS. The systems mentioned above allow for a higher effectiveness of therapy and reduce the likelihood of side effects. It is known that, by developing a variety of DDSs, it is now possible to better control the pharmacokinetics, pharmacodynamics, toxicity, immunogenicity, and efficacy of drugs.

This Special Issue aims at polymeric, inorganic, and macromolecular anti-cancer drug carriers, such as nano- and micro-particles, transdermal, implantable, and macromolecular conjugates of drugs, etc.

In this Special Issue, original research articles and reviews are welcome. Research areas may include (but not limited to) aspects of anti-cancer DDS, i.e., the synthesis, physicochemical, and biological properties.

I look forward to receiving your contributions.

Dr. Karolina Kędra
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 100 words) can be sent to the Editorial Office for announcement on this website.

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

  • anti-cancer drugs
  • drug carriers
  • drug delivery systems
  • polymeric biomaterials
  • ceramic biomaterials
  • carbon biomaterials
  • composite biomaterials
  • implantation drug delivery systems
  • transdermal drug delivery systems

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Published Papers (5 papers)

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Research

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16 pages, 3830 KiB  
Article
Synergetic Effect of β-Cyclodextrin and Its Simple Carbohydrate Substituents on Complexation of Folic Acid and Its Structural Analog Methotrexate
by Magdalena Ceborska, Aleksandra Siklitskaya, Aneta Aniela Kowalska and Karolina Kędra
Pharmaceutics 2024, 16(9), 1161; https://doi.org/10.3390/pharmaceutics16091161 - 3 Sep 2024
Viewed by 853
Abstract
Folic acid (FA) and its structural analog, anticancer medicine methotrexate (MTX), are known to form host/guest complexes with native cyclodextrins, of which the most stable are formed with the medium-sized β-cyclodextrin. Based on our research, proving that simple sugars (D-glucose, D-galactose, and D-mannose) [...] Read more.
Folic acid (FA) and its structural analog, anticancer medicine methotrexate (MTX), are known to form host/guest complexes with native cyclodextrins, of which the most stable are formed with the medium-sized β-cyclodextrin. Based on our research, proving that simple sugars (D-glucose, D-galactose, and D-mannose) can form adducts with folic acid, we envisioned that combining these two types of molecular receptors (cyclodextrin and simple carbohydrates) into one may be beneficial for the complexation of FA and MTX. We designed and obtained host/guest inclusion complexes of FA and MTX with two monoderivatives of β-cyclodextrin—substituted at position 6 with monosaccharide (glucose, G-β-CD) and disaccharide (maltose, Ma-β-CD). The complexation was proved by experimental (NMR, UV-vis, IR, TG, DSC) and theoretical methods. We proved that derivatization of β-cyclodextrin with glucose and maltose has a significant impact on the complexation with FA and MTX, as the addition of one glucose subunit to the structure of the receptor significantly increases the value of association constant for both FA/G-β-CD and MTX/G-β-CD, while further extending a pendant chain (incorporation of maltose subunit) results in no additional changes. Full article
(This article belongs to the Special Issue Anti-Cancer Drug Delivery Systems)
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19 pages, 8253 KiB  
Article
Nucleolin-Targeting AS1411 Aptamer-Conjugated Nanospheres for Targeted Treatment of Glioblastoma
by Kyeongjin Seo, Kihwan Hwang, Kyung Mi Nam, Min Ju Kim, Yoon-Kyu Song and Chae-Yong Kim
Pharmaceutics 2024, 16(4), 566; https://doi.org/10.3390/pharmaceutics16040566 - 21 Apr 2024
Cited by 2 | Viewed by 2827
Abstract
Post-operative chemotherapy is still required for the treatment of glioblastoma (GBM), for which nanocarrier-based drug delivery has been identified as one of the most effective methods. However, the blood-brain barrier (BBB) and non-specific delivery to non-tumor tissues can significantly limit drug accumulation in [...] Read more.
Post-operative chemotherapy is still required for the treatment of glioblastoma (GBM), for which nanocarrier-based drug delivery has been identified as one of the most effective methods. However, the blood-brain barrier (BBB) and non-specific delivery to non-tumor tissues can significantly limit drug accumulation in tumor tissues and cause damage to nearby normal tissues. This study describes a targeted cancer therapy approach that uses AS1411 aptamer-conjugated nanospheres (100–300 nm in size) loaded with doxorubicin (Dox) to selectively identify tumor cells overexpressing nucleolin (NCL) proteins. The study demonstrates that the active target model, which employs aptamer-mediated drug delivery, is more effective than non-specific enhanced permeability and maintenance (EPR)-mediated delivery and passive drug delivery in improving drug penetration and maintenance in tumor cells. Additionally, the study reveals the potential for anti-cancer effects through 3D spheroidal and in vivo GBM xenograft models. The DNA-protein hybrid nanospheres utilized in this study offer numerous benefits, such as efficient synthesis, structural stability, high drug loading, dye labeling, biocompatibility, and biodegradability. When combined with nanospheres, the 1411 aptamer has been shown to be an effective drug delivery carrier allowing for the precise targeting of tumors. This combination has the potential to produce anti-tumor effects in the active targeted therapy of GBM. Full article
(This article belongs to the Special Issue Anti-Cancer Drug Delivery Systems)
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14 pages, 7480 KiB  
Article
Size Tuning of Mesoporous Silica Adjuvant for One-Shot Vaccination with Long-Term Anti-Tumor Effect
by Xiupeng Wang, Yu Sogo and Xia Li
Pharmaceutics 2024, 16(4), 516; https://doi.org/10.3390/pharmaceutics16040516 - 8 Apr 2024
Viewed by 1750
Abstract
Despite recent clinical successes in cancer immunotherapy, it remains difficult to initiate a long-term anti-tumor effect. Therefore, repeated administrations of immune-activating agents are generally required in most cases. Herein, we propose an adjuvant particle size tuning strategy to initiate a long-term anti-tumor effect [...] Read more.
Despite recent clinical successes in cancer immunotherapy, it remains difficult to initiate a long-term anti-tumor effect. Therefore, repeated administrations of immune-activating agents are generally required in most cases. Herein, we propose an adjuvant particle size tuning strategy to initiate a long-term anti-tumor effect by one-shot vaccination. This strategy is based on the size-dependent immunostimulation mechanism of mesoporous silica particles. Hollow mesoporous silica (HMS) nanoparticles enhance the antigen uptake with dendritic cells around the immunization site in vivo. In contrast, hierarchically porous silica (HPS) microparticles prolong cancer antigen retention and release in vivo. The size tuning of the mesoporous silica adjuvant prepared by combining both nanoparticles and microparticles demonstrates the immunological properties of both components and has a long-term anti-tumor effect after one-shot vaccination. One-shot vaccination with HMS-HPS-ovalbumin (OVA)-Poly IC (PIC, a TLR3 agonist) increases CD4+ T cell, CD8+ T cell, and CD86+ cell populations in draining lymph nodes even 4 months after vaccination, as well as effector memory CD8+ T cell and tumor-specific tetramer+CD8+ T cell populations in splenocytes. The increases in the numbers of effector memory CD8+ T cells and tumor-specific tetramer+CD8+ T cells indicate that the one-shot vaccination with HMS-HPS-OVA-PIC achieved the longest survival time after a challenge with E.G7-OVA cells among all groups. The size tuning of the mesoporous silica adjuvant shows promise for one-shot vaccination that mimics multiple clinical vaccinations in future cancer immunoadjuvant development. This study may have important implications in the long-term vaccine design of one-shot vaccinations. Full article
(This article belongs to the Special Issue Anti-Cancer Drug Delivery Systems)
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14 pages, 14092 KiB  
Article
Polydopamine-Modified Copper Coordination Mesoporous Silica Nanoparticles Loaded with Disulfiram for Synergistic Chemo-Photothermal Therapy
by Junhong Ling, Yingying Cai, Haozhan Feng, Zhen Liu and Xiao-kun Ouyang
Pharmaceutics 2024, 16(4), 512; https://doi.org/10.3390/pharmaceutics16040512 - 7 Apr 2024
Cited by 2 | Viewed by 1995
Abstract
Disulfiram (DSF) degrades to diethyldithiocarbamate (DTC) in vivo and coordinates with copper ions to form CuET, which has higher antitumor activity. In this study, DSF@CuMSN-PDA nanoparticles were prepared using mesoporous silica with copper ions, DSF as a carrier, and polydopamine (PDA) as a [...] Read more.
Disulfiram (DSF) degrades to diethyldithiocarbamate (DTC) in vivo and coordinates with copper ions to form CuET, which has higher antitumor activity. In this study, DSF@CuMSN-PDA nanoparticles were prepared using mesoporous silica with copper ions, DSF as a carrier, and polydopamine (PDA) as a gate system. The nanoparticles selectively released CuET into tumor tissue by taking advantage of the tumor microenvironment, where PDA could be degraded. The release ratio reached 79.17% at pH 5.0, indicating pH-responsive drug release from the nanoparticles. The PDA-gated system provided the nanoparticles with unique photothermal conversion performance and significantly improved antitumor efficiency. In vivo, antitumor experiments showed that the designed DSF@CuMSN-PDA nanoparticles combined with near-infrared light (808 nm, 1 W/cm2) irradiation effectively inhibited tumor growth in HCT116 cells by harnessing the combined potential of chemotherapy and photothermal therapy; a synergistic effect was achieved. Taken together, these results suggest that the designed DSF@CuMSN-PDA construct can be employed as a promising candidate for combined chemo-photothermal therapy. Full article
(This article belongs to the Special Issue Anti-Cancer Drug Delivery Systems)
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Review

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29 pages, 13064 KiB  
Review
Application of Nanotechnology and Phytochemicals in Anticancer Therapy
by Jin Hee Kim, Boluwatife Olamide Dareowolabi, Rekha Thiruvengadam and Eun-Yi Moon
Pharmaceutics 2024, 16(9), 1169; https://doi.org/10.3390/pharmaceutics16091169 - 5 Sep 2024
Cited by 2 | Viewed by 1703
Abstract
Cancer is well recognized as a leading cause of mortality. Although surgery tends to be the primary treatment option for many solid cancers, cancer surgery is still a risk factor for metastatic diseases and recurrence. For this reason, a variety of medications has [...] Read more.
Cancer is well recognized as a leading cause of mortality. Although surgery tends to be the primary treatment option for many solid cancers, cancer surgery is still a risk factor for metastatic diseases and recurrence. For this reason, a variety of medications has been adopted for the postsurgical care of patients with cancer. However, conventional medicines have shown major challenges such as drug resistance, a high level of drug toxicity, and different drug responses, due to tumor heterogeneity. Nanotechnology-based therapeutic formulations could effectively overcome the challenges faced by conventional treatment methods. In particular, the combined use of nanomedicine with natural phytochemicals can enhance tumor targeting and increase the efficacy of anticancer agents with better solubility and bioavailability and reduced side effects. However, there is limited evidence in relation to the application of phytochemicals in cancer treatment, particularly focusing on nanotechnology. Therefore, in this review, first, we introduce the drug carriers used in advanced nanotechnology and their strengths and limitations. Second, we provide an update on well-studied nanotechnology-based anticancer therapies related to the carcinogenesis process, including signaling pathways related to transforming growth factor-β (TGF-β), mitogen-activated protein kinase (MAPK), phosphatidylinositol 3 kinase (PI3K), Wnt, poly(ADP-ribose) polymerase (PARP), Notch, and Hedgehog (HH). Third, we introduce approved nanomedicines currently available for anticancer therapy. Fourth, we discuss the potential roles of natural phytochemicals as anticancer drugs. Fifth, we also discuss the synergistic effect of nanocarriers and phytochemicals in anticancer therapy. Full article
(This article belongs to the Special Issue Anti-Cancer Drug Delivery Systems)
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