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Keywords = theranostic liposomes

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29 pages, 2060 KiB  
Review
Revitalizing Colchicine: Novel Delivery Platforms and Derivatives to Expand Its Therapeutic Potential
by Natallia V. Dubashynskaya, Anton N. Bokatyi, Mikhail M. Galagudza and Yury A. Skorik
Int. J. Mol. Sci. 2025, 26(15), 7591; https://doi.org/10.3390/ijms26157591 - 6 Aug 2025
Abstract
Colchicine is a potent alkaloid with well-established anti-inflammatory properties. It shows significant promise in treating classic immune-mediated inflammatory diseases, as well as associated cardiovascular diseases, including atherosclerosis. However, its clinical use is limited by a narrow therapeutic window, dose-limiting systemic toxicity, variable bioavailability, [...] Read more.
Colchicine is a potent alkaloid with well-established anti-inflammatory properties. It shows significant promise in treating classic immune-mediated inflammatory diseases, as well as associated cardiovascular diseases, including atherosclerosis. However, its clinical use is limited by a narrow therapeutic window, dose-limiting systemic toxicity, variable bioavailability, and clinically significant drug–drug interactions, partly mediated by modulation of P-glycoprotein and cytochrome P450 3A4 metabolism. This review explores advanced delivery strategies designed to overcome these limitations. We critically evaluate lipid-based systems, such as solid lipid nanoparticles, liposomes, transferosomes, ethosomes, and cubosomes; polymer-based nanoparticles; microneedles; and implants, including drug-eluting stents. These systems ensure targeted delivery, improve pharmacokinetics, and reduce toxicity. Additionally, we discuss chemical derivatization approaches, such as prodrugs, codrugs, and strategic ring modifications (A-, B-, and C-rings), aimed at optimizing both the efficacy and safety profile of colchicine. Combinatorial nanoformulations that enable the co-delivery of colchicine with synergistic agents, such as glucocorticoids and statins, as well as theranostic platforms that integrate therapeutic and diagnostic functions, are also considered. These innovative delivery systems and derivatives have the potential to transform colchicine therapy by broadening its clinical applications while minimizing adverse effects. Future challenges include scalable manufacturing, long-term safety validation, and the translation of research into clinical practice. Full article
(This article belongs to the Section Macromolecules)
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21 pages, 3471 KiB  
Review
Nanomedicine: The Effective Role of Nanomaterials in Healthcare from Diagnosis to Therapy
by Raisa Nazir Ahmed Kazi, Ibrahim W. Hasani, Doaa S. R. Khafaga, Samer Kabba, Mohd Farhan, Mohammad Aatif, Ghazala Muteeb and Yosri A. Fahim
Pharmaceutics 2025, 17(8), 987; https://doi.org/10.3390/pharmaceutics17080987 - 30 Jul 2025
Viewed by 236
Abstract
Nanotechnology is revolutionizing medicine by enabling highly precise diagnostics, targeted therapies, and personalized healthcare solutions. This review explores the multifaceted applications of nanotechnology across medical fields such as oncology and infectious disease control. Engineered nanoparticles (NPs), such as liposomes, polymeric carriers, and carbon-based [...] Read more.
Nanotechnology is revolutionizing medicine by enabling highly precise diagnostics, targeted therapies, and personalized healthcare solutions. This review explores the multifaceted applications of nanotechnology across medical fields such as oncology and infectious disease control. Engineered nanoparticles (NPs), such as liposomes, polymeric carriers, and carbon-based nanomaterials, enhance drug solubility, protect therapeutic agents from degradation, and enable site-specific delivery, thereby reducing toxicity to healthy tissues. In diagnostics, nanosensors and contrast agents provide ultra-sensitive detection of biomarkers, supporting early diagnosis and real-time monitoring. Nanotechnology also contributes to regenerative medicine, antimicrobial therapies, wearable devices, and theranostics, which integrate treatment and diagnosis into unified systems. Advanced innovations such as nanobots and smart nanosystems further extend these capabilities, enabling responsive drug delivery and minimally invasive interventions. Despite its immense potential, nanomedicine faces challenges, including biocompatibility, environmental safety, manufacturing scalability, and regulatory oversight. Addressing these issues is essential for clinical translation and public acceptance. In summary, nanotechnology offers transformative tools that are reshaping medical diagnostics, therapeutics, and disease prevention. Through continued research and interdisciplinary collaboration, it holds the potential to significantly enhance treatment outcomes, reduce healthcare costs, and usher in a new era of precise and personalized medicine. Full article
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19 pages, 2357 KiB  
Article
Chimeric Element-Regulated MRI Reporter System for Mediation of Glioma Theranostics
by Qian Hu, Jie Huang, Xiangmin Zhang, Haoru Wang, Xiaoying Ni, Huiru Zhu and Jinhua Cai
Cancers 2025, 17(14), 2349; https://doi.org/10.3390/cancers17142349 - 15 Jul 2025
Viewed by 320
Abstract
Background and Purpose: Glioblastoma remains a therapeutic challenge with a poor prognosis despite multimodal treatments. Reporter-based magnetic resonance imaging (MRI) offers a promising approach for tumor visualization, but its efficacy depends on sufficient reporter gene expression. This study aimed to develop a [...] Read more.
Background and Purpose: Glioblastoma remains a therapeutic challenge with a poor prognosis despite multimodal treatments. Reporter-based magnetic resonance imaging (MRI) offers a promising approach for tumor visualization, but its efficacy depends on sufficient reporter gene expression. This study aimed to develop a chimeric element-regulated ferritin heavy chain 1 (FTH1) reporter system to enhance MRI-based glioma detection while enabling targeted therapy via transferrin receptor (TfR)-mediated drug delivery. Methods: Using gene cloning techniques, we constructed a chimeric FTH1 expression system comprising tumor-specific PEG3 promoter (transcriptional control), bFGF-2 5′UTR (translational enhancement), and WPRE (mRNA stabilization). Lentiviral vectors delivered constructs to U251 glioblastoma cells and xenografts. FTH1/TfR expression was validated by Western blot and immunofluorescence. Iron accumulation was assessed via Prussian blue staining and TEM. MRI evaluated T2 signal changes. Transferrin-modified doxorubicin liposomes (Tf-LPD) were characterized for size and drug loading and tested for cellular uptake and cytotoxicity in vitro. In vivo therapeutic efficacy was assessed in nude mouse models through tumor volume measurement, MR imaging, and histopathology. Results: The chimeric system increased FTH1 expression significantly over PEG3-only controls (p < 0.01), with an increase of nearly 1.5-fold compared to the negative and blank groups and approximately a two-fold increase relative to the single promoter group, with corresponding TfR upregulation. Enhanced iron accumulation reduced T2 relaxation times significantly (p < 0.01), improving MR contrast. Tf-LPD (115 nm, 70% encapsulation) showed TfR-dependent uptake, inducing obvious apoptosis in high-TfR cells compared with that in controls. In vivo, Tf-LPD reduced tumor growth markedly in chimeric-system xenografts versus controls, with concurrent MR signal attenuation. Conclusions: The chimeric regulatory strategy overcomes limitations of single-element systems, demonstrating significant potential for integrated glioma theranostics. Its modular design may be adaptable to other reporter genes and malignancies. Full article
(This article belongs to the Section Cancer Therapy)
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34 pages, 4581 KiB  
Review
Nanoradiopharmaceuticals: Design Principles, Radiolabeling Strategies, and Biomedicine Applications
by Andrés Núñez-Salinas, Cristian Parra-Garretón, Daniel Acuña, Sofía Peñaloza, Germán Günther, Soledad Bollo, Francisco Arriagada and Javier Morales
Pharmaceutics 2025, 17(7), 912; https://doi.org/10.3390/pharmaceutics17070912 - 14 Jul 2025
Viewed by 604
Abstract
Nanoradiopharmaceuticals integrate nanotechnology with nuclear medicine to enhance the precision and effectiveness of radiopharmaceuticals used in diagnostic imaging and targeted therapies. Nanomaterials offer improved targeting capabilities and greater stability, helping to overcome several limitations. This review presents a comprehensive overview of the fundamental [...] Read more.
Nanoradiopharmaceuticals integrate nanotechnology with nuclear medicine to enhance the precision and effectiveness of radiopharmaceuticals used in diagnostic imaging and targeted therapies. Nanomaterials offer improved targeting capabilities and greater stability, helping to overcome several limitations. This review presents a comprehensive overview of the fundamental design principles, radiolabeling techniques, and biomedical applications of nanoradiopharmaceuticals, with a particular focus on their expanding role in precision oncology. It explores key areas, including single- and multi-modal imaging modalities (SPECT, PET), radionuclide therapies involving beta, alpha, and Auger emitters, and integrated theranostic systems. A diverse array of nanocarriers is examined, including liposomes, micelles, albumin nanoparticles, PLGA, dendrimers, and gold, iron oxide, and silica-based platforms, with an assessment of both preclinical and clinical research outcomes. Theranostic nanoplatforms, which integrate diagnostic and therapeutic functions within a single system, enable real-time monitoring and personalized dose optimization. Although some of these systems have progressed to clinical trials, several obstacles remain, including formulation stability, scalable manufacturing, regulatory compliance, and long-term safety considerations. In summary, nanoradiopharmaceuticals represent a promising frontier in personalized medicine, particularly in oncology. By combining diagnostic and therapeutic capabilities within a single nanosystem, they facilitate more individualized and adaptive treatment approaches. Continued innovation in formulation, radiochemistry, and regulatory harmonization will be crucial to their successful routine clinical use. Full article
(This article belongs to the Special Issue Nanosystems for Advanced Diagnostics and Therapy)
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20 pages, 1490 KiB  
Review
Liposome-Based Drug Delivery Systems: From Laboratory Research to Industrial Production—Instruments and Challenges
by Suman Basak and Tushar Kanti Das
ChemEngineering 2025, 9(3), 56; https://doi.org/10.3390/chemengineering9030056 - 27 May 2025
Cited by 3 | Viewed by 2779
Abstract
Liposome-based drug delivery systems have revolutionized modern pharmaceutics, offering unparalleled versatility and precision in therapeutic delivery. These lipid vesicles, capable of encapsulating hydrophilic, hydrophobic, and amphiphilic drugs, have demonstrated significant potential in addressing pharmacokinetic challenges such as poor solubility, systemic toxicity, and rapid [...] Read more.
Liposome-based drug delivery systems have revolutionized modern pharmaceutics, offering unparalleled versatility and precision in therapeutic delivery. These lipid vesicles, capable of encapsulating hydrophilic, hydrophobic, and amphiphilic drugs, have demonstrated significant potential in addressing pharmacokinetic challenges such as poor solubility, systemic toxicity, and rapid clearance. This review provides a comprehensive exploration of the evolution of liposomes from laboratory models to clinically approved therapeutics, highlighting their structural adaptability, functional tunability, and transformative impact on modern medicine. We discuss pivotal laboratory-scale preparation techniques, including thin-film hydration, ethanol injection, and reverse-phase evaporation, along with their inherent advantages and limitations. The challenges of transitioning to industrial-scale production are examined, with emphasis on achieving batch-to-batch consistency, scalability, regulatory compliance, and cost-effectiveness. Innovative strategies, such as the incorporation of microfluidic systems and advanced process optimization, are explored to address these hurdles. The clinical success of Food and Drug Administration (FDA)-approved liposomal formulations such as Doxil® and AmBisome® underscores their efficacy in treating conditions ranging from cancer to fungal infections. Furthermore, this review delves into emerging trends, including stimuli-responsive and hybrid liposomes, as well as their integration with nanotechnology for enhanced therapeutic precision. As liposomes continue to expand their role in gene therapy, theranostics, and personalized medicine, this review highlights their potential to redefine pharmaceutical applications. Despite existing challenges, ongoing advancements in formulation techniques and scalability underscore the bright future of liposome-based therapeutics in addressing unmet medical needs. Full article
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26 pages, 3748 KiB  
Review
Mechanical Properties of Medical Microbubbles and Echogenic Liposomes—A Review
by Hussain Alsadiq and Zahra Alhay
Micromachines 2025, 16(5), 588; https://doi.org/10.3390/mi16050588 - 17 May 2025
Viewed by 784
Abstract
Lipid-shelled microbubbles (MBs) and echogenic liposomes (ELIPs) have been proposed as acoustofluidic theranostic agents after having been proven to be efficient in diagnostics as ultrasonic contrast agents. Their mechanical properties—such as shell stiffness, friction, and resonance frequency—are critical to their performance, stability, oscillatory [...] Read more.
Lipid-shelled microbubbles (MBs) and echogenic liposomes (ELIPs) have been proposed as acoustofluidic theranostic agents after having been proven to be efficient in diagnostics as ultrasonic contrast agents. Their mechanical properties—such as shell stiffness, friction, and resonance frequency—are critical to their performance, stability, oscillatory dynamics, and response to sonication. A precise characterization of these properties is essential for optimizing their biomedical applications, however the current methods vary significantly in their sensitivity and accuracy. This review examines the experimental and theoretical methodologies used to quantify the mechanical properties of MBs and ELIPs, discusses how each approach estimates shell stiffness and friction, and outlines the strengths and limitations inherent to each technique. Additionally, the effects of parameters such as temperature and lipid composition on MB and ELIP mechanical behavior are examined. Four characterization methods are analyzed, including frequency-dependent attenuation, optical observation, atomic force microscopy (AFM), and laser scattering, their advantages and limitations are critically assessed. Additionally, the factors that influence the mechanical properties of the MBs and ELIPs, such as temperature and lipid composition, are examined. Frequency-dependent attenuation was shown to provide reliable shell elasticity estimates but is influenced by nonlinear oscillations, AFM confirms that microbubble stiffness is size-dependent with smaller bubbles exhibiting higher shell stiffness, and theoretical models such as modified Rayleigh–Plesset equations increasingly incorporate viscoelastic shell properties to improve prediction accuracy. However, many of these models still assume radial symmetry and neglect inter-bubble interactions, which can lead to inaccurate elasticity values when applied to dense suspensions. In such cases, using modified frameworks like the Sarkar model, which incorporates damping and surface tension explicitly, may provide more reliable estimates under nonlinear conditions. Additionally, lipid composition and temperature significantly affect shell mechanics, with higher temperatures generally reducing stiffness. On the other hand, inconsistencies in experimental protocols hinder direct comparison across studies, highlighting the need for standardized characterization methods and improved computational modeling. Full article
(This article belongs to the Section B:Biology and Biomedicine)
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16 pages, 3216 KiB  
Article
Multifaceted Functional Liposomes: Theranostic Potential of Liposomal Indocyanine Green and Doxorubicin for Enhanced Anticancer Efficacy and Imaging
by Wei-Ting Liao, Dao-Ming Chang, Meng-Xian Lin, Te-Sen Chou, Yi-Chung Tung and Jong-Kai Hsiao
Pharmaceutics 2025, 17(3), 344; https://doi.org/10.3390/pharmaceutics17030344 - 7 Mar 2025
Viewed by 1004
Abstract
Background/Objectives: Liposomal drug formulations improve anticancer treatment efficacy and reduce toxicity by altering pharmacokinetics and biodistribution. Indocyanine Green (ICG), an FDA-approved near-infrared imaging agent, exhibits photosensitivity, photothermal effects, and potential ferroptosis induction, enhancing anticancer activity. Doxorubicin (DOX), widely used for treating breast, ovarian, [...] Read more.
Background/Objectives: Liposomal drug formulations improve anticancer treatment efficacy and reduce toxicity by altering pharmacokinetics and biodistribution. Indocyanine Green (ICG), an FDA-approved near-infrared imaging agent, exhibits photosensitivity, photothermal effects, and potential ferroptosis induction, enhancing anticancer activity. Doxorubicin (DOX), widely used for treating breast, ovarian, and liver cancers, is limited by cardiotoxicity, requiring dosage control. Incorporating ICG and DOX into liposomes enables medical imaging, controlled drug release, reduced administration frequency, and fewer side effects. This study aims to develop liposomes encapsulating both ICG and DOX and evaluate their theranostic potential in in vitro and in vivo lung adenocarcinoma models. Methods: Liposomes containing ICG and DOX (Lipo-ICG/DOX) were synthesized using an active loading method and characterized for size (~140 nm), lipid, and drug concentrations. In vitro studies using A549 lung cancer cells assessed liposome uptake via fluorescence microscopy, while in vivo xenograft models evaluated therapeutic efficacy. Results: Lipo-ICG/DOX showed uptake in A549 cells, with ICG localizing in lysosomes and DOX in nuclei. Treatment reduced cell viability significantly by day three. In vivo imaging demonstrated the retention of liposomes in tumor sites, with ICG signals observed in the liver and intestines, indicating metabolic routes. When combined with 780 nm light exposure, liposomes slowed tumor growth over 12 days. Mechanistic studies revealed combined ferroptosis and apoptosis induction. Conclusions: Lipo-ICG/DOX demonstrates strong theranostic potential, integrating imaging and therapy for lung adenocarcinoma. This multifunctional formulation offers a promising strategy for improving cancer treatment efficacy while minimizing side effects. Full article
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45 pages, 2056 KiB  
Review
Nanomedicine: Pioneering Advances in Neural Disease, Stroke and Spinal Cord Injury Treatment
by Borish Loushambam, Sangeeta Yanglem, Venkateswaran Krishnaswami, Munish Kumar and Sivakumar Vijayaraghavalu
Neuroglia 2025, 6(1), 9; https://doi.org/10.3390/neuroglia6010009 - 21 Feb 2025
Cited by 2 | Viewed by 1940
Abstract
Background: Neurological disorders such as Alzheimer’s disease (AD), Parkinson’s disease (PD), stroke, and spinal cord injury (SCI) are significant global health challenges due to their complex pathology and limited therapeutic options. Conventional treatments often fail to efficiently cross the blood–brain barrier (BBB), leading [...] Read more.
Background: Neurological disorders such as Alzheimer’s disease (AD), Parkinson’s disease (PD), stroke, and spinal cord injury (SCI) are significant global health challenges due to their complex pathology and limited therapeutic options. Conventional treatments often fail to efficiently cross the blood–brain barrier (BBB), leading to poor bioavailability and systemic toxicity. This narrative review explores the potential of nanomedicine in addressing these limitations and advancing targeted therapies for neural disorders. Methods: This review examines recent studies on the use of engineered nanoparticles (NPs), including liposomes, dendrimers, micelles, and nanogels, for targeted drug delivery and multifunctional theranostics in neural diseases. It evaluates their role in promoting axon regeneration, reducing neuroinflammation, and repairing neural damage. Additionally, innovative applications in gene therapy and RNA-based treatments, such as CRISPR-Cas9 and RNA interference (RNAi), are discussed. Challenges related to toxicity, scalability, affordability, and regulatory barriers are highlighted, along with potential strategies to address these issues. Results: Nanoparticles have shown significant promise in crossing the BBB, delivering therapeutic agents to neural tissues, and minimizing off-target effects. Emerging applications in gene and RNA-based therapies demonstrate their versatility in addressing disease-specific challenges. However, unresolved issues such as long-term safety, manufacturing scalability, and cost continue to pose challenges. Conclusions: Nanomedicine offers a promising approach to overcoming current limitations in the treatment of neural disorders. This review emphasizes the need for continued interdisciplinary efforts to address translational barriers and highlights the potential for nanomedicine to improve the outcomes and quality of life for patients with neural disorders, stroke, and SCI. Full article
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29 pages, 9386 KiB  
Review
Nanostructured Formulations for a Local Treatment of Cancer: A Mini Review About Challenges and Possibilities
by Tatiane Roquete Amparo, Tamires Cunha Almeida, Lucas Resende Dutra Sousa, Viviane Flores Xavier, Glenda Nicioli da Silva, Geraldo Célio Brandão and Orlando David Henrique dos Santos
Pharmaceutics 2025, 17(2), 205; https://doi.org/10.3390/pharmaceutics17020205 - 6 Feb 2025
Cited by 2 | Viewed by 1473
Abstract
Cancer represents a significant societal, public health, and economic challenge. Conventional chemotherapy is based on systemic administration; however, it has current limitations, including poor bioavailability, high-dose requirements, adverse side effects, low therapeutic indices, and the development of multiple drug resistance. These factors underscore [...] Read more.
Cancer represents a significant societal, public health, and economic challenge. Conventional chemotherapy is based on systemic administration; however, it has current limitations, including poor bioavailability, high-dose requirements, adverse side effects, low therapeutic indices, and the development of multiple drug resistance. These factors underscore the need for innovative strategies to enhance drug delivery directly to tumours. However, local treatment also presents significant challenges, including the penetration of the drug through endothelial layers, tissue density in the tumour microenvironment, tumour interstitial fluid pressure, physiological conditions within the tumour, and permanence at the site of action. Nanotechnology represents a promising alternative for addressing these challenges. This narrative review elucidates the potential of nanostructured formulations for local cancer treatment, providing illustrative examples and an analysis of the advantages and challenges associated with this approach. Among the nanoformulations developed for the local treatment of breast, bladder, colorectal, oral, and melanoma cancer, polymeric nanoparticles, liposomes, lipid nanoparticles, and nanohydrogels have demonstrated particular efficacy. These systems permit mucoadhesion and enhanced tissue penetration, thereby increasing the drug concentration at the tumour site (bioavailability) and consequently improving anti-tumour efficacy and potentially reducing adverse effects. In addition to studies indicating chemotherapy, nanocarriers can be used as a theranostic approach and in combination with irradiation methods. Full article
(This article belongs to the Special Issue Nanoformulations for Local Treatment of Cancer, Infections and Wounds)
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36 pages, 1627 KiB  
Review
Current Non-Metal Nanoparticle-Based Therapeutic Approaches for Glioblastoma Treatment
by Agata M. Gawel, Anna Betkowska, Ewa Gajda, Marlena Godlewska and Damian Gawel
Biomedicines 2024, 12(8), 1822; https://doi.org/10.3390/biomedicines12081822 - 11 Aug 2024
Cited by 10 | Viewed by 2945
Abstract
The increase in the variety of nano-based tools offers new possibilities to approach the therapy of poorly treatable tumors, which includes glioblastoma multiforme (GBM; a primary brain tumor). The available nanocomplexes exhibit great potential as vehicles for the targeted delivery of anti-GBM compounds, [...] Read more.
The increase in the variety of nano-based tools offers new possibilities to approach the therapy of poorly treatable tumors, which includes glioblastoma multiforme (GBM; a primary brain tumor). The available nanocomplexes exhibit great potential as vehicles for the targeted delivery of anti-GBM compounds, including chemotherapeutics, nucleic acids, and inhibitors. The main advantages of nanoparticles (NPs) include improved drug stability, increased penetration of the blood–brain barrier, and better precision of tumor targeting. Importantly, alongside their drug-delivery ability, NPs may also present theranostic properties, including applications for targeted imaging or photothermal therapy of malignant brain cells. The available NPs can be classified into two categories according to their core, which can be metal or non-metal based. Among non-metal NPs, the most studied in regard to GBM treatment are exosomes, liposomes, cubosomes, polymeric NPs, micelles, dendrimers, nanogels, carbon nanotubes, and silica- and selenium-based NPs. They are characterized by satisfactory stability and biocompatibility, limited toxicity, and high accumulation in the targeted tumor tissue. Moreover, they can be easily functionalized for the improved delivery of their cargo to GBM cells. Therefore, the non-metal NPs discussed here, offer a promising approach to improving the treatment outcomes of aggressive GBM tumors. Full article
(This article belongs to the Special Issue Advances in Cancer Biology and Experimental Anticancer Therapies)
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15 pages, 3500 KiB  
Article
Magnet-Guided Temozolomide and Ferucarbotran Loaded Nanoparticles to Enhance Therapeutic Efficacy in Glioma Model
by Reju George Thomas, Subin Kim, Thi-Anh-Thuy Tran, Young Hee Kim, Raveena Nagareddy, Tae-Young Jung, Seul Kee Kim and Yong Yeon Jeong
Nanomaterials 2024, 14(11), 939; https://doi.org/10.3390/nano14110939 - 27 May 2024
Cited by 4 | Viewed by 1757
Abstract
Background. The aim of the study was to synthesize liposomal nanoparticles loaded with temozolomide and ferucarbotran (LTF) and to evaluate the theranostic effect of LTF in the glioma model. Methods. We synthesized an LTF that could pass through the Blood Brain Barrier (BBB) [...] Read more.
Background. The aim of the study was to synthesize liposomal nanoparticles loaded with temozolomide and ferucarbotran (LTF) and to evaluate the theranostic effect of LTF in the glioma model. Methods. We synthesized an LTF that could pass through the Blood Brain Barrier (BBB) and localize in brain tumor tissue with the help of magnet guidance. We examined the chemical characteristics. Cellular uptake and cytotoxicity studies were conducted in vitro. A biodistribution and tumor inhibition study was conduted using an in vivo glioma model. Results. The particle size and surface charge of LTF show 108 nm and −38 mV, respectively. Additionally, the presence of ferucarbotran significantly increased the contrast agent effect of glioma compared to the control group in MR imaging. Magnet-guided LTF significantly reduced the tumor size compared to control and other groups. Furthermore, compared to the control group, our results demonstrate a significant inhibition in brain tumor size and an increase in lifespan. Conclusions. These findings suggest that the LTF with magnetic guidance represents a novel approach to address current obstacles, such as BBB penetration of nanoparticles and drug resistance. Magnet-guided LTF is able to enhance therapeutic efficacy in mouse brain glioma. Full article
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32 pages, 4436 KiB  
Review
Galactose: A Versatile Vector Unveiling the Potentials in Drug Delivery, Diagnostics, and Theranostics
by Chiara Battisegola, Chiara Billi, Maria Cristina Molaro, Marica Erminia Schiano, Maria Nieddu, Mariacristina Failla, Elisabetta Marini, Stefania Albrizio, Federica Sodano and Maria Grazia Rimoli
Pharmaceuticals 2024, 17(3), 308; https://doi.org/10.3390/ph17030308 - 27 Feb 2024
Cited by 13 | Viewed by 5303
Abstract
D-galactose, a simple natural compound, has been investigated as a powerful scaffold for drug delivery, diagnostics, and theranostics due to its distinctive properties and interactions with specific cell receptors. In the field of drug delivery, galactose functions as a ligand to selectively target [...] Read more.
D-galactose, a simple natural compound, has been investigated as a powerful scaffold for drug delivery, diagnostics, and theranostics due to its distinctive properties and interactions with specific cell receptors. In the field of drug delivery, galactose functions as a ligand to selectively target cells expressing galactose receptors, such as hepatocytes, macrophages, and specific cancer cells. The direct attachment of galactose to the main drug or to drug-loaded nanoparticles or liposomes enhances cellular uptake, thereby improving drug delivery to the intended target cells. Galactose has also been found to be useful in diagnostics. Specifically, diagnostic tests based on galactose, such as the galactose elimination capacity test, are utilized to evaluate liver function and assess liver disease as well as hepatic functional reserve. Additionally, galactose-based theranostic agents can be designed by combining drug delivery and diagnostic capabilities. This review is an update of our previous review concerning the broad spectrum of possibilities for exploiting D-galactose as a vector for prodrug design and the synthetic strategies that allow its realization, jointly in diagnostics and theranostics, to highlight the versatility of this interesting vector. Full article
(This article belongs to the Special Issue Carbohydrate-Based Drugs 2023)
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17 pages, 5557 KiB  
Article
Development of PET Radioisotope Copper-64-Labeled Theranostic Immunoliposomes for EGFR Overexpressing Cancer-Targeted Therapy and Imaging
by Hwa Yeon Jeong, Seong Jae Kang, Min Woo Kim, In-ho Jeong, Moon Jung Choi, Cheulhee Jung, In Ho Song, Tae Sup Lee and Yong Serk Park
Int. J. Mol. Sci. 2024, 25(3), 1813; https://doi.org/10.3390/ijms25031813 - 2 Feb 2024
Cited by 4 | Viewed by 2476
Abstract
Combining standard surgical procedures with personalized chemotherapy and the continuous monitoring of cancer progression is necessary for effective NSCLC treatment. In this study, we developed liposomal nanoparticles as theranostic agents capable of simultaneous therapy for and imaging of target cancer cells. Copper-64 ( [...] Read more.
Combining standard surgical procedures with personalized chemotherapy and the continuous monitoring of cancer progression is necessary for effective NSCLC treatment. In this study, we developed liposomal nanoparticles as theranostic agents capable of simultaneous therapy for and imaging of target cancer cells. Copper-64 (64Cu), with a clinically practical half-life (t1/2 = 12.7 h) and decay properties, was selected as the radioisotope for molecular PET imaging. An anti-epidermal growth factor receptor (anti-EGFR) antibody was used to achieve target-specific delivery. Simultaneously, the chemotherapeutic agent doxorubicin (Dox) was encapsulated within the liposomes using a pH-gradient method. The conjugates of 64Cu-labeled and anti-EGFR antibody-conjugated micelles were inserted into the doxorubicin-encapsulating liposomes via a post-insertion procedure (64Cu-Dox-immunoliposomes). We evaluated the size and zeta-potential of the liposomes and analyzed target-specific cell binding and cytotoxicity in EGFR-positive cell lines. Then, we analyzed the specific therapeutic effect and PET imaging of the 64Cu-Dox-immunoliposomes with the A549 xenograft mouse model. In vivo therapeutic experiments on the mouse models demonstrated that the doxorubicin-containing 64Cu-immunoliposomes effectively inhibited tumor growth. Moreover, the 64Cu-immunoliposomes provided superior in vivo PET images of the tumors compared to the untargeted liposomes. We suggest that nanoparticles will be the potential platform for cancer treatment as a widely applicable theranostic system. Full article
(This article belongs to the Section Materials Science)
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30 pages, 5604 KiB  
Review
Liposomes for Cancer Theranostics
by Donald A. Fernandes
Pharmaceutics 2023, 15(10), 2448; https://doi.org/10.3390/pharmaceutics15102448 - 11 Oct 2023
Cited by 14 | Viewed by 4368
Abstract
Cancer is one of the most well-studied diseases and there have been significant advancements over the last few decades in understanding its molecular and cellular mechanisms. Although the current treatments (e.g., chemotherapy, radiotherapy, gene therapy and immunotherapy) have provided complete cancer remission for [...] Read more.
Cancer is one of the most well-studied diseases and there have been significant advancements over the last few decades in understanding its molecular and cellular mechanisms. Although the current treatments (e.g., chemotherapy, radiotherapy, gene therapy and immunotherapy) have provided complete cancer remission for many patients, cancer still remains one of the most common causes of death in the world. The main reasons for the poor response rates for different cancers include the lack of drug specificity, drug resistance and toxic side effects (i.e., in healthy tissues). For addressing the limitations of conventional cancer treatments, nanotechnology has shown to be an important field for constructing different nanoparticles for destroying cancer cells. Due to their size (i.e., less than 1 μm), nanoparticles can deliver significant amounts of cancer drugs to tumors and are able to carry moieties (e.g., folate, peptides) for targeting specific types of cancer cells (i.e., through receptor-mediated endocytosis). Liposomes, composed of phospholipids and an interior aqueous core, can be used as specialized delivery vehicles as they can load different types of cancer therapy agents (e.g., drugs, photosensitizers, genetic material). In addition, the ability to load imaging agents (e.g., fluorophores, radioisotopes, MRI contrast media) enable these nanoparticles to be used for monitoring the progress of treatment. This review examines a wide variety of different liposomes for cancer theranostics, with the different available treatments (e.g., photothermal, photodynamic) and imaging modalities discussed for different cancers. Full article
(This article belongs to the Special Issue Multifunctional Nanoparticles for Cancer Therapy and Imaging)
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12 pages, 1898 KiB  
Article
Folate-Targeted Nanoliposomal Chemophototherapy
by Upendra Chitgupi, Yiru Qin, Sanjana Ghosh, Breandan Quinn, Kevin Carter, Xuedan He, Ulas Sunar and Jonathan F. Lovell
Pharmaceutics 2023, 15(10), 2385; https://doi.org/10.3390/pharmaceutics15102385 - 26 Sep 2023
Cited by 4 | Viewed by 2259
Abstract
Light-responsive liposomes have been developed for the on-demand release of drugs. However, efficient delivery of chemotherapeutic drugs to tumor for cancer theranostics remains a challenge. Herein, folic acid (FA), an established ligand for targeted drug delivery, was used to decorate light-sensitive porphyrin-phospholipid (PoP) [...] Read more.
Light-responsive liposomes have been developed for the on-demand release of drugs. However, efficient delivery of chemotherapeutic drugs to tumor for cancer theranostics remains a challenge. Herein, folic acid (FA), an established ligand for targeted drug delivery, was used to decorate light-sensitive porphyrin-phospholipid (PoP) liposomes, which were assessed for FA-targeted chemophototherapy (CPT). PoP liposomes and FA-conjugated PoP liposomes were loaded with Doxorubicin (Dox), and physical properties were characterized. In vitro, FA-PoP liposomes that were incubated with FA receptor-overexpressing human KB cancer cells showed increased uptake compared to non-targeted PoP liposomes. Dox and PoP contributed towards chemophototherapy (CPT) in vitro, and PoP and FA-PoP liposomes induced cell killing. In vivo, mice bearing subcutaneous KB tumors treated with PoP or FA-PoP liposomes loaded with Dox, followed by 665 nm laser treatment, had delayed tumor growth and improved survival. Dox delivery to tumors increased following laser irradiation for both PoP and FA-PoP liposomes. Thus, while Dox-FA-PoP liposomes were effective following systemic administration and local light irradiation in this tumor model, the FA targeting moiety did not appear essential for anti-tumor responses. Full article
(This article belongs to the Special Issue Designing Nanomaterials for Drug Delivery and Cancer-Targeted Therapy)
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