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Pharmaceutics
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Lipid-Based Nanoparticles for Drug Delivery in Cancer
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Lipid-Based Nanoparticles for Drug Delivery in Cancer

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 2024) | Viewed by 12483

Special Issue Editors

Dr. Daniela Chirio

E-Mail Website
Guest Editor
Department of Drug Science and Technology, University of Turin, 10125 Turin, Italy
Interests: drug delivery systems; solid lipid nanoparticles microemulsions; nanoemulsions; nanostructured lipid carriers; targeting
Dr. Elena Peira

E-Mail Website
Guest Editor
Department of Drug Science and Technology, University of Turin, 10125 Turin, Italy
Interests: drug delivery systems; solid lipid nanoparticles microemulsions; nanoemulsions; nanostructured lipid carriers; targeting

Special Issue Information

Dear Colleagues,

We are planning to publish a Special Issue based on “Lipid-Based Nanoparticles for Drug Delivery in Cancer” in the journal Pharmaceutics.

Often, cancer chemotherapy encounters several obstacles such as severe side effects, low specificity and stability, and a high incidence of drug-resistant tumor cells. Recently, the attention of researchers has mainly been focused on overcoming multidrug resistance, considered the main cause of chemotherapy failure. The use of nanotechnology and, in particular, of lipid-based nanoparticles as a drug delivery system is promising for avoiding these problems in many tumor types.

Authors are kindly invited to submit original papers, communications, and reviews regarding the potential applications of lipid-based nanocarriers as drug delivery systems for cancer therapy to be published in this Special Issue of Pharmaceutics. We look forward to receiving your contributions.

Dr. Daniela Chirio
Dr. Elena Peira
Guest Editors

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

  • lipid nanoparticles
  • nanocarriers
  • drug delivery systems
  • cancer
  • chemotherapy

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Published Papers (6 papers)

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Research

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22 pages, 8473 KiB  
Article
Bilosomal Co-Encapsulated Tamoxifen and Propranolol for Potentiated Anti-Breast Cancer Efficacy: In Vitro and In Vivo Investigation
by Toka T. Elebyary, Amal A. Sultan, Sally E. Abu-Risha, Gamal M. El Maghraby and Manna Amin
Pharmaceutics 2025, 17(1), 123; https://doi.org/10.3390/pharmaceutics17010123 - 17 Jan 2025
Viewed by 877
Abstract
Background/Objectives: Tamoxifen (TAM) is an anti-breast cancer drug suffering from acquired resistance development, prompting cancer relapse. Propranolol (PRO)’s repurposing for cancer therapy has gained interest. This work aimed to investigate combined TAM/PRO therapy for potentiating the anti-breast cancer activity of TAM. The [...] Read more.
Background/Objectives: Tamoxifen (TAM) is an anti-breast cancer drug suffering from acquired resistance development, prompting cancer relapse. Propranolol (PRO)’s repurposing for cancer therapy has gained interest. This work aimed to investigate combined TAM/PRO therapy for potentiating the anti-breast cancer activity of TAM. The work probed bilosomes versus standard noisome for simultaneous oral and intratumor delivery of TAM and PRO. Methods: Bilosomes comprising Span60, cholesterol, and increasing concentrations of bile salts were prepared together with bile salts containing free standard niosomes. The vesicular size and morphology were characterized. The entrapment and release efficiencies of TAM and PRO from the tailored vesicles were determined. The in vivo investigations of anti-tumor activity of TAM with or without PRO employed the solid Ehrlich carcinoma model. Results: The vesicles of all fabricated dispersions were spherical and negatively charged, with a size ranging from 104 to 182 nm. The entrapment efficiency depended on the nature of the drug, recording values ranging from 87.5% to 97.8% for TAM and from 31.0% to 46.8% for PRO. Incorporation of bile salts into vesicles increased TAM and PRO release compared to standard niosomes. Oral administration of combined TAM/PRO bilosomes showed a significant reduction in tumor growth volume compared to that recorded following naked drug administration. Histopathological investigations reflected a significant decline in tumor giant cells and mitotic figures, implying the in vivo capability of the TAM/PRO combination to interfere with cancer cell proliferation and persistence. Conclusions: The overall results demonstrated the impact of repurposed PRO to enhance the anti-breast cancer activity of TAM when both were co-encapsulated into bilosomes. Full article
(This article belongs to the Special Issue Lipid-Based Nanoparticles for Drug Delivery in Cancer)
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14 pages, 6040 KiB  
Article
Personalized SO2 Prodrug for pH-Triggered Gas Enhancement in Anti-Tumor Radio-Immunotherapy
by Zhiran Chen, Xiaoxiang Zhou, Bo Wu, Han Tang, Wei Wei, Daoming Zhu, Yi Ding and Longyun Chen
Pharmaceutics 2024, 16(6), 833; https://doi.org/10.3390/pharmaceutics16060833 - 19 Jun 2024
Viewed by 1461
Abstract
The inhibition of the immune response in the tumor microenvironment by therapy regimens can impede the eradication of tumors, potentially resulting in tumor metastasis. As a non-invasive therapeutic method, radiotherapy is utilized for tumor ablation. In this study, we aimed to improve the [...] Read more.
The inhibition of the immune response in the tumor microenvironment by therapy regimens can impede the eradication of tumors, potentially resulting in tumor metastasis. As a non-invasive therapeutic method, radiotherapy is utilized for tumor ablation. In this study, we aimed to improve the therapeutic impact of radiotherapy and trigger an immune response by formulating a benzothiazole sulfinate (BTS)-loaded fusion liposome (BFL) nanoplatform, which was then combined with radiotherapy for anti-cancer treatment. The platelet cell membrane, equipped with distinctive surface receptors, enables BFL to effectively target tumors while evading the immune system and adhering to tumor cells. This facilitates BFL’s engulfment by cancer cells, subsequently releasing BTS within them. Following the release, the BTS produces sulfur dioxide (SO2) for gas therapy, initiating the oxidation of intracellular glutathione (GSH). This process demonstrates efficacy in repairing damage post-radiotherapy, thereby achieving effective radiosensitization. It was revealed that an immune response was triggered following the enhanced radiosensitization facilitated by BFL. This approach facilitated the maturation of dendritic cell (DC) within lymph nodes, leading to an increase in the proportion of T cells in distant tumors. This resulted in significant eradication of primary tumors and inhibition of growth in distant tumors. In summary, the integration of personalized BFL with radiotherapy shows potential in enhancing both tumor immune response and the elimination of tumors, including metastasis. Full article
(This article belongs to the Special Issue Lipid-Based Nanoparticles for Drug Delivery in Cancer)
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18 pages, 6823 KiB  
Article
Combination of miR159 Mimics and Irinotecan Utilizing Lipid Nanoparticles for Enhanced Treatment of Colorectal Cancer
by Rulei Yang, Yiran Liu, Ning Yang, Tian Zhang, Jiazhen Hou, Zongyan He, Yutong Wang, Xujie Sun, Jingshan Shen, Hualiang Jiang, Yuanchao Xie and Tianqun Lang
Pharmaceutics 2024, 16(4), 570; https://doi.org/10.3390/pharmaceutics16040570 - 22 Apr 2024
Cited by 1 | Viewed by 2349
Abstract
Colorectal cancer (CRC) ranks as the third most prevalent global malignancy, marked by significant metastasis and post-surgical recurrence, posing formidable challenges to treatment efficacy. The integration of oligonucleotides with chemotherapeutic drugs emerges as a promising strategy for synergistic CRC therapy. The nanoformulation, lipid [...] Read more.
Colorectal cancer (CRC) ranks as the third most prevalent global malignancy, marked by significant metastasis and post-surgical recurrence, posing formidable challenges to treatment efficacy. The integration of oligonucleotides with chemotherapeutic drugs emerges as a promising strategy for synergistic CRC therapy. The nanoformulation, lipid nanoparticle (LNP), presents the capability to achieve co-delivery of oligonucleotides and chemotherapeutic drugs for cancer therapy. In this study, we constructed lipid nanoparticles, termed as LNP-I-V by microfluidics to co-deliver oligonucleotides miR159 mimics (VDX05001SI) and irinotecan (IRT), demonstrating effective treatment of CRC both in vitro and in vivo. The LNP-I-V exhibited a particle size of 118.67 ± 1.27 nm, ensuring excellent stability and targeting delivery to tumor tissues, where it was internalized and escaped from the endosome with a pH-sensitive profile. Ultimately, LNP-I-V significantly inhibited CRC growth, extended the survival of tumor-bearing mice, and displayed favorable safety profiles. Thus, LNP-I-V held promise as an innovative platform to combine gene therapy and chemotherapy for improving CRC treatment. Full article
(This article belongs to the Special Issue Lipid-Based Nanoparticles for Drug Delivery in Cancer)
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17 pages, 5859 KiB  
Article
Maleimide–Thiol Linkages Alter the Biodistribution of SN38 Therapeutic Microbubbles Compared to Biotin–Avidin While Preserving Parity in Tumoral Drug Delivery
by Nicola Ingram, Radwa H. Abou-Saleh, Amanda D. Race, Paul M. Loadman, Richard J. Bushby, Stephen D. Evans and P. Louise Coletta
Pharmaceutics 2024, 16(3), 434; https://doi.org/10.3390/pharmaceutics16030434 - 21 Mar 2024
Viewed by 2144
Abstract
Therapeutic microbubbles (thMBs) contain drug-filled liposomes linked to microbubbles and targeted to vascular proteins. Upon the application of a destructive ultrasound trigger, drug uptake to tumour is improved. However, the structure of thMBs currently uses powerful non-covalent bonding of biotin with avidin-based proteins [...] Read more.
Therapeutic microbubbles (thMBs) contain drug-filled liposomes linked to microbubbles and targeted to vascular proteins. Upon the application of a destructive ultrasound trigger, drug uptake to tumour is improved. However, the structure of thMBs currently uses powerful non-covalent bonding of biotin with avidin-based proteins to link both the liposome to the microbubble (MB) and to bind the targeting antibody to the liposome–MB complex. This linkage is not currently FDA-approved, and therefore, an alternative, maleimide–thiol linkage, that is currently used in antibody–drug conjugates was examined. In a systematic manner, vascular endothelial growth factor receptor 2 (VEGFR2)-targeted MBs and thMBs using both types of linkages were examined for their ability to specifically bind to VEGFR2 in vitro and for their ultrasound imaging properties in vivo. Both showed equivalence in the production of the thMB structure, in vitro specificity of binding and safety profiles. In vivo imaging showed subtle differences for thMBs where biotin thMBs had a faster wash-in rate than thiol thMBs, but thiol thMBs were longer-lived. The drug delivery to tumours was also equivalent, but interestingly, thiol thMBs altered the biodistribution of delivery away from the lungs and towards the liver compared to biotin thMBs, which is an improvement in biosafety. Full article
(This article belongs to the Special Issue Lipid-Based Nanoparticles for Drug Delivery in Cancer)
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14 pages, 2304 KiB  
Article
In Vitro and Preclinical Antitumor Evaluation of Doxorubicin Liposomes Coated with a Cholesterol-Based Trimeric β-D-Glucopyranosyltriazole
by Aline Teixeira Maciel e Silva, Ana Luiza Chaves Maia, Juliana de Oliveira Silva, Sued Eustáquio Mendes Miranda, Talia Silva Cantini, Andre Luis Branco de Barros, Daniel Crístian Ferreira Soares, Mariana Torquato Quezado de Magalhães, Ricardo José Alves and Gilson Andrade Ramaldes
Pharmaceutics 2023, 15(12), 2751; https://doi.org/10.3390/pharmaceutics15122751 - 11 Dec 2023
Cited by 1 | Viewed by 1657
Abstract
The coating of liposomes with polyethyleneglycol (PEG) has been extensively discussed over the years as a strategy for enhancing the in vivo and in vitro stability of nanostructures, including doxorubicin-loaded liposomes. However, studies have shown some important disadvantages of the PEG molecule as [...] Read more.
The coating of liposomes with polyethyleneglycol (PEG) has been extensively discussed over the years as a strategy for enhancing the in vivo and in vitro stability of nanostructures, including doxorubicin-loaded liposomes. However, studies have shown some important disadvantages of the PEG molecule as a long-circulation agent, including the immunogenic role of PEG, which limits its clinical use in repeated doses. In this context, hydrophilic molecules as carbohydrates have been proposed as an alternative to coating liposomes. Thus, this work studied the cytotoxicity and preclinical antitumor activity of liposomes coated with a glycosyl triazole glucose (GlcL-DOX) derivative as a potential strategy against breast cancer. The glucose-coating of liposomes enhanced the storage stability compared to PEG-coated liposomes, with the suitable retention of DOX encapsulation. The antitumor activity, using a 4T1 breast cancer mouse model, shows that GlcL-DOX controlled the tumor growth in 58.5% versus 35.3% for PEG-coated liposomes (PegL-DOX). Additionally, in the preliminary analysis of the GlcL-DOX systemic toxicity, the glucose-coating liposomes reduced the body weight loss and hepatotoxicity compared to other DOX-treated groups. Therefore, GlcL-DOX could be a promising alternative for treating breast tumors. Further studies are required to elucidate the complete GlcL-DOX safety profile. Full article
(This article belongs to the Special Issue Lipid-Based Nanoparticles for Drug Delivery in Cancer)
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Review

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35 pages, 4305 KiB  
Review
Biomimetic Cell-Derived Nanoparticles: Emerging Platforms for Cancer Immunotherapy
by Tingting Hu, Yuezhou Huang, Jing Liu, Chao Shen, Fengbo Wu and Zhiyao He
Pharmaceutics 2023, 15(7), 1821; https://doi.org/10.3390/pharmaceutics15071821 - 26 Jun 2023
Cited by 11 | Viewed by 2785
Abstract
Cancer immunotherapy can significantly prevent tumor growth and metastasis by activating the autoimmune system without destroying normal cells. Although cancer immunotherapy has made some achievements in clinical cancer treatment, it is still restricted by systemic immunotoxicity, immune cell dysfunction, cancer heterogeneity, and the [...] Read more.
Cancer immunotherapy can significantly prevent tumor growth and metastasis by activating the autoimmune system without destroying normal cells. Although cancer immunotherapy has made some achievements in clinical cancer treatment, it is still restricted by systemic immunotoxicity, immune cell dysfunction, cancer heterogeneity, and the immunosuppressive tumor microenvironment (ITME). Biomimetic cell-derived nanoparticles are attracting considerable interest due to their better biocompatibility and lower immunogenicity. Moreover, biomimetic cell-derived nanoparticles can achieve different preferred biological effects due to their inherent abundant source cell-relevant functions. This review summarizes the latest developments in biomimetic cell-derived nanoparticles for cancer immunotherapy, discusses the applications of each biomimetic system in cancer immunotherapy, and analyzes the challenges for clinical transformation. Full article
(This article belongs to the Special Issue Lipid-Based Nanoparticles for Drug Delivery in Cancer)
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