Applications of Dendrimers in Biomedicine

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

Deadline for manuscript submissions: closed (30 June 2023) | Viewed by 31743

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Preclinical Department, Faculty of Medicine, “Lucian Blaga” University of Sibiu, 2A Lucian Blaga St., 550169 Sibiu, Romania
Interests: natural products; antioxidants; dendrimers; drug delivery; analytical methods; biochemistry; laboratory tests; pharmacovigilance
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Department of Toxicology, Faculty of Pharmacy, “Iuliu Hațieganu” University of Medicine and Pharmacy, 6 L. Pasteur Street, 400349 Cluj-Napoca, Romania
Interests: safety evaluation; nanotoxicity; oxidative stress biomarkers; toxicokinetics; analysis of toxicants
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E-Mail Website
Guest Editor
Preclinical Department, Faculty of Medicine, “Lucian Blaga” University of Sibiu, 2A Lucian Blaga St., 550169 Sibiu, Romania
Interests: safety and effectiveness of health products; pharmacotherapy; pharmacovigilance; nutrivigilance
Special Issues, Collections and Topics in MDPI journals

E-Mail Website
Guest Editor
Preclinical Department, Faculty of Medicine, “Lucian Blaga” University of Sibiu, 2A Lucian Blaga St., 550169 Sibiu, Romania
Interests: dendrimers; drug delivery; nanocosmetics; cosmetic formulation; safety and efficacy of cosmetics; natural products; cosmetovigilance; nutrivigilance
Special Issues, Collections and Topics in MDPI journals
Preclinical Department, Faculty of Medicine, “Lucian Blaga” University of Sibiu, 2A Lucian Blaga St., 550169 Sibiu, Romania
Interests: phytochemical analyses; antioxidants; polyphenols; environmental sciences; natural products; nutrivigilance; dendrimers; drug delivery
Special Issues, Collections and Topics in MDPI journals

E-Mail Website
Guest Editor
Preclinical Department, Faculty of Medicine, “Lucian Blaga” University of Sibiu, 2A Lucian Blaga St., 550169 Sibiu, Romania
Interests: natural products; antioxidants; phytochemicals; nutrivigilance; toxicology; dendrimers; drug delivery
Special Issues, Collections and Topics in MDPI journals

Special Issue Information

Dear Colleagues,

Dendrimers are synthetic polymers characterized by branched repeating units that emerge from a focal point and possess a large number of exposed anionic, neutral or cationic terminal functionalities on the surface. They are nanometric molecules that are radially symmetric, globular, mono-dispersed, and homogenous.

The term “dendrimer” is a combination of two Greek words, “dendron” and “meros” translated as tree and parts, thus explaining their branched structure. In 1941 Flory published the original concept of branched molecules. The first dendrimers were synthesized by Vögtle et al., in 1978. Initially, dendrimers were obtained based on divergent synthesis methods, and later convergent methods for obtaining dendritic structures were used.

Biomedicine represents one of the main study areas for dendrimers, which have proven valuable both in diagnostics and therapy, due to their capacity of improving solubility, absorption, bioavailability, and targeted distribution.

Many studies were performed in order to demonstrate the dendrimers’ wide potential as drug carriers in different pathologies such as cancer, diabetes, infections, inflammation, Alzheimer’s disease, cardiovascular conditions, etc. On the other hand, dendrimers are studied in regenerative medicine (e.g., wound healing, tissue and cartilage reconstruction, bone remineralization, etc.) or cosmetics. Furthermore, dendrimers have applications in diagnosis resulting in improved imaging agents.

In the present Special Issue, manuscripts covering aspects from the entire field such as synthesis, characterization methods, molecular simulations, regulatory, biological or clinical studies, potential applications in biomedicine, pharmacokinetics improvement, toxicity reduction, etc. are encouraged. 

Prof. Dr. Felicia Gabriela Gligor
Prof. Dr. Felicia Loghin
Dr. Claudiu Morgovan
Dr. Anca Maria Juncan
Dr. Adina Frum
Dr. Carmen Maximiliana Dobrea
Guest Editors

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Keywords

  • dendrimers
  • dendritic polymers
  • nanostructures
  • carriers
  • synthesis
  • characterization
  • imaging agents
  • regenerative medicine
  • nanomedicine
  • cosmetics
  • drug delivery
  • biological properties
  • drug therapy

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Published Papers (11 papers)

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Research

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13 pages, 3962 KiB  
Article
Interaction of Graphene Oxide Particles and Dendrimers with Human Breast Cancer Cells by Real-Time Microscopy
by Beatriz Fumelli Monti Ribeiro, Julyane Batista Chaves, Marcelo Medina De Souza, Artur Franz Keppler, Devaney Ribeiro Do Carmo and Gláucia M. Machado-Santelli
Pharmaceutics 2023, 15(12), 2655; https://doi.org/10.3390/pharmaceutics15122655 - 22 Nov 2023
Viewed by 1602
Abstract
Graphene oxide (GOX) has become attractive due to its unique physicochemical properties. This nanomaterial can associate with other dendrimers, making them more soluble and allowing better interaction with biomacromolecules. The present study aimed to investigate, by real-time microscopy, the behavior of human breast [...] Read more.
Graphene oxide (GOX) has become attractive due to its unique physicochemical properties. This nanomaterial can associate with other dendrimers, making them more soluble and allowing better interaction with biomacromolecules. The present study aimed to investigate, by real-time microscopy, the behavior of human breast cancer cells exposed to particles of materials based on graphene oxide. The MCF-7 cell line was exposed to GOX, GOX associated with Polypropylenimine hexadecaamine Dendrimer, Generation 3.0—DAB-AM-16 (GOXD) and GOX associated with polypropyleneimine—PAMAM (GOXP) in the presence or absence of fetal bovine serum (FBS). GOX, GOXD and GOXP were taken up by the cells in clusters and then the clusters were fragmented into smaller ones inside the cells. Real-time microscopy showed that the presence of FBS in the culture medium could allow a more efficient internalization of graphene materials. After internalizing the materials, cells can redistribute the clumps to their daughter cells. In conclusion, the present study showed that the particles can adhere to the cell surface, favoring their internalization. The presence of FBS contributed to the formation of smaller aggregates of particles, avoiding the formation of large ones, and thus transmitted a more efficient internalization of the materials through the interaction of the particles with the cell membrane. Full article
(This article belongs to the Special Issue Applications of Dendrimers in Biomedicine)
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17 pages, 4563 KiB  
Article
Microglial-Targeted nSMase2 Inhibitor Fails to Reduce Tau Propagation in PS19 Mice
by Meixiang Huang, Carolyn Tallon, Xiaolei Zhu, Kaitlyn D. J. Huizar, Silvia Picciolini, Ajit G. Thomas, Lukas Tenora, Wathsala Liyanage, Francesca Rodà, Alice Gualerzi, Rangaramanujam M. Kannan, Marzia Bedoni, Rana Rais and Barbara S. Slusher
Pharmaceutics 2023, 15(9), 2364; https://doi.org/10.3390/pharmaceutics15092364 - 21 Sep 2023
Cited by 1 | Viewed by 1932
Abstract
The progression of Alzheimer’s disease (AD) correlates with the propagation of hyperphosphorylated tau (pTau) from the entorhinal cortex to the hippocampus and neocortex. Neutral sphingomyelinase2 (nSMase2) is critical in the biosynthesis of extracellular vesicles (EVs), which play a role in pTau propagation. We [...] Read more.
The progression of Alzheimer’s disease (AD) correlates with the propagation of hyperphosphorylated tau (pTau) from the entorhinal cortex to the hippocampus and neocortex. Neutral sphingomyelinase2 (nSMase2) is critical in the biosynthesis of extracellular vesicles (EVs), which play a role in pTau propagation. We recently conjugated DPTIP, a potent nSMase2 inhibitor, to hydroxyl-PAMAM-dendrimer nanoparticles that can improve brain delivery. We showed that dendrimer-conjugated DPTIP (D–DPTIP) robustly inhibited the spread of pTau in an AAV-pTau propagation model. To further evaluate its efficacy, we tested D-DPTIP in the PS19 transgenic mouse model. Unexpectantly, D-DPTIP showed no beneficial effect. To understand this discrepancy, we assessed D-DPTIP’s brain localization. Using immunofluorescence and fluorescence-activated cell-sorting, D-DPTIP was found to be primarily internalized by microglia, where it selectively inhibited microglial nSMase2 activity with no effect on other cell types. Furthermore, D-DPTIP inhibited microglia-derived EV release into plasma without affecting other brain-derived EVs. We hypothesize that microglial targeting allowed D-DPTIP to inhibit tau propagation in the AAV-hTau model, where microglial EVs play a central role in propagation. However, in PS19 mice, where tau propagation is independent of microglial EVs, it had a limited effect. Our findings confirm microglial targeting with hydroxyl-PAMAM dendrimers and highlight the importance of understanding cell-specific mechanisms when designing targeted AD therapies. Full article
(This article belongs to the Special Issue Applications of Dendrimers in Biomedicine)
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14 pages, 2759 KiB  
Article
Lysine-Dendrimer, a New Non-Aggressive Solution to Rebalance the Microbiota of Acne-Prone Skin
by Julie Leignadier, Marie Drago, Olivier Lesouhaitier, Magalie Barreau, Albert Dashi, Oliver Worsley and Joan Attia-Vigneau
Pharmaceutics 2023, 15(8), 2083; https://doi.org/10.3390/pharmaceutics15082083 - 3 Aug 2023
Cited by 3 | Viewed by 2388
Abstract
Acne is a chronic inflammatory skin disease that affects the quality of life of patients. Several treatments exist for acne, but their effectiveness tends to decrease over time due to increasing resistance to treatment and associated side effects. To circumvent these issues, a [...] Read more.
Acne is a chronic inflammatory skin disease that affects the quality of life of patients. Several treatments exist for acne, but their effectiveness tends to decrease over time due to increasing resistance to treatment and associated side effects. To circumvent these issues, a new approach has emerged that involves combating the pathogen Cutibacterium acnes while maintaining the homeostasis of the skin microbiome. Recently, it was shown that the use of a G2 lysine dendrigraft (G2 dendrimer) could specifically decrease the C. acnes phylotype (IAI) involved in acne, compared to non-acne-causing C. acnes (phylotype II) bacteria. In the present study, we demonstrate that the efficacy of this technology is related to its 3D structure, which, in contrast to the linear form, significantly decreases the inflammation factor (IL-8) linked to acne. In addition, our in-vitro data confirm the specific activity of the G2 dendrimer: after treatment of bacterial cultures and biofilms, the G2 dendrimer affected neither non-acneic C. acnes nor commensal bacteria of the skin (Staphylococcus epidermidis, S. hominis, and Corynebacterium minutissimum). In parallel, comparative in-vitro and in-vivo studies with traditional over-the-counter molecules showed G2’s effects on the survival of commensal bacteria and the reduction of acne outbreaks. Finally, metagenomic analysis of the cutaneous microbiota of volunteers who applied a finished cosmetic product containing the G2 dendrimer confirmed the ability of G2 to rebalance cutaneous acne microbiota dysbiosis while maintaining commensal bacteria. These results confirm the value of using this G2 dendrimer to gently prevent the appearance of acne vulgaris while respecting the cutaneous microbiota. Full article
(This article belongs to the Special Issue Applications of Dendrimers in Biomedicine)
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29 pages, 7457 KiB  
Article
Effect of the Size and Shape of Dendronized Iron Oxide Nanoparticles Bearing a Targeting Ligand on MRI, Magnetic Hyperthermia, and Photothermia Properties—From Suspension to In Vitro Studies
by Barbara Freis, Maria De Los Angeles Ramirez, Céline Kiefer, Sébastien Harlepp, Cristian Iacovita, Céline Henoumont, Christine Affolter-Zbaraszczuk, Florent Meyer, Damien Mertz, Anne Boos, Mariana Tasso, Sonia Furgiuele, Fabrice Journe, Sven Saussez, Sylvie Bégin-Colin and Sophie Laurent
Pharmaceutics 2023, 15(4), 1104; https://doi.org/10.3390/pharmaceutics15041104 - 30 Mar 2023
Cited by 15 | Viewed by 2987
Abstract
Functionalized iron oxide nanoparticles (IONPs) are increasingly being designed as a theranostic nanoplatform combining specific targeting, diagnosis by magnetic resonance imaging (MRI), and multimodal therapy by hyperthermia. The effect of the size and the shape of IONPs is of tremendous importance to develop [...] Read more.
Functionalized iron oxide nanoparticles (IONPs) are increasingly being designed as a theranostic nanoplatform combining specific targeting, diagnosis by magnetic resonance imaging (MRI), and multimodal therapy by hyperthermia. The effect of the size and the shape of IONPs is of tremendous importance to develop theranostic nanoobjects displaying efficient MRI contrast agents and hyperthermia agent via the combination of magnetic hyperthermia (MH) and/or photothermia (PTT). Another key parameter is that the amount of accumulation of IONPs in cancerous cells is sufficiently high, which often requires the grafting of specific targeting ligands (TLs). Herein, IONPs with nanoplate and nanocube shapes, which are promising to combine magnetic hyperthermia (MH) and photothermia (PTT), were synthesized by the thermal decomposition method and coated with a designed dendron molecule to ensure their biocompatibility and colloidal stability in suspension. Then, the efficiency of these dendronized IONPs as contrast agents (CAs) for MRI and their ability to heat via MH or PTT were investigated. The 22 nm nanospheres and the 19 nm nanocubes presented the most promising theranostic properties (respectively, r2 = 416 s−1·mM−1, SARMH = 580 W·g−1, SARPTT = 800 W·g−1; and r2 = 407 s−1·mM−1, SARMH = 899 W·g−1, SARPTT = 300 W·g−1). MH experiments have proven that the heating power mainly originates from Brownian relaxation and that SAR values can remain high if IONPs are prealigned with a magnet. This raises hope that heating will maintain efficient even in a confined environment, such as in cells or in tumors. Preliminary in vitro MH and PTT experiments have shown the promising effect of the cubic shaped IONPs, even though the experiments should be repeated with an improved set-up. Finally, the grafting of a specific peptide (P22) as a TL for head and neck cancers (HNCs) has shown the positive impact of the TL to enhance IONP accumulation in cells. Full article
(This article belongs to the Special Issue Applications of Dendrimers in Biomedicine)
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16 pages, 4862 KiB  
Article
Conjugation of Short Oligopeptides to a Second-Generation Polyamidoamine Dendrimer Shows Antibacterial Activity
by Namyoung Kang, Le Thi Thuy, Viet Dongquoc and Joon Sig Choi
Pharmaceutics 2023, 15(3), 1005; https://doi.org/10.3390/pharmaceutics15031005 - 21 Mar 2023
Viewed by 1821
Abstract
The growing evolution of bacterial resistance to antibiotics represents a global issue that not only impacts healthcare systems but also political and economic processes. This necessitates the development of novel antibacterial agents. Antimicrobial peptides have shown promise in this regard. Thus, in this [...] Read more.
The growing evolution of bacterial resistance to antibiotics represents a global issue that not only impacts healthcare systems but also political and economic processes. This necessitates the development of novel antibacterial agents. Antimicrobial peptides have shown promise in this regard. Thus, in this study, a new functional polymer was synthesized by joining a short oligopeptide sequence (Phe-Lys-Phe-Leu, FKFL) to the surface of a second-generation polyamidoamine (G2 PAMAM) dendrimer as an antibacterial component. This method of synthesis proved simple and resulted in a high conjugation yield of the product FKFL-G2. To determine its antibacterial potential, FKFL-G2 was subsequently analyzed via mass spectrometry, a cytotoxicity assay, bacterial growth assay, colony-forming unit assay, membrane permeabilization assay, transmission electron microscopy, and biofilm formation assay. FKFL-G2 was found to exhibit low toxicity to noncancerous NIH3T3 cells. Additionally, FKFL-G2 had an antibacterial effect on Escherichia coli and Staphylococcus aureus strains by interacting with and disrupting the bacterial cell membrane. Based on these findings, FKFL-G2 shows promise as a potential antibacterial agent. Full article
(This article belongs to the Special Issue Applications of Dendrimers in Biomedicine)
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21 pages, 2296 KiB  
Article
Biological Effects in Cancer Cells of Mono- and Bidentate Conjugation of Cisplatin on PAMAM Dendrimers: A Comparative Study
by Cláudia Camacho, Dina Maciel, Helena Tomás and João Rodrigues
Pharmaceutics 2023, 15(2), 689; https://doi.org/10.3390/pharmaceutics15020689 - 17 Feb 2023
Cited by 2 | Viewed by 2430
Abstract
Cisplatin (cis-diamminedichloroplatinum(II)) is a potent chemotherapeutic agent commonly used to treat cancer. However, its use also leads to serious side effects, such as nephrotoxicity, ototoxicity, and cardiotoxicity, which limit the dose that can be safely administered to patients. To minimize these [...] Read more.
Cisplatin (cis-diamminedichloroplatinum(II)) is a potent chemotherapeutic agent commonly used to treat cancer. However, its use also leads to serious side effects, such as nephrotoxicity, ototoxicity, and cardiotoxicity, which limit the dose that can be safely administered to patients. To minimize these problems, dendrimers may be used as carriers for cisplatin through the coordination of their terminal functional groups to platinum. Here, cisplatin was conjugated to half-generation anionic PAMAM dendrimers in mono- and bidentate forms, and their biological effects were assessed in vitro. After preparation and characterization of the metallodendrimers, their cytotoxicity was evaluated against several cancer cell lines (A2780, A2780cisR, MCF-7, and CACO-2 cells) and a non-cancer cell line (BJ cells). The results showed that all the metallodendrimers were cytotoxic and that the cytotoxicity level depended on the cell line and the type of coordination mode (mono- or bidentate). Although, in this study, a correlation between dendrimer generation (number of carried metallic fragments) and cytotoxicity could not be completely established, the monodentate coordination form of cisplatin resulted in lower IC50 values, thus revealing a more accessible cisplatin release from the dendritic scaffold. Moreover, most of the metallodendrimers were more potent than the cisplatin, especially for the A2780 and A2780cisR cell lines, which showed higher selectivity than for non-cancer cells (BJ cells). The monodentate G0.5COO(Pt(NH3)2Cl)8 and G2.5COO(Pt(NH3)2Cl)32 metallodendrimers, as well as the bidentate G2.5COO(Pt(NH3)2)16 metallodendrimer, were even more active towards the cisplatin-resistant cell line (A2780cisR cells) than the correspondent cisplatin-sensitive one (A2780 cells). Finally, the effect of the metallodendrimers on the hemolysis of human erythrocytes was neglectable, and metallodendrimers’ interaction with calf thymus DNA seemed to be stronger than that of free cisplatin. Full article
(This article belongs to the Special Issue Applications of Dendrimers in Biomedicine)
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15 pages, 1491 KiB  
Article
Synthesis of β-Cyclodextrin-Decorated Dendritic Compounds Based on EDTA Core: A New Class of PAMAM Dendrimer Analogs
by Israel González-Méndez, Esteban Loera-Loera, Kendra Sorroza-Martínez, Mireille Vonlanthen, Fabián Cuétara-Guadarrama, María Josefa Bernad-Bernad, Ernesto Rivera and Jesús Gracia-Mora
Pharmaceutics 2022, 14(11), 2363; https://doi.org/10.3390/pharmaceutics14112363 - 2 Nov 2022
Cited by 4 | Viewed by 2128
Abstract
In this work, two dendritic molecules containing an ethylenediaminetetraacetic acid (EDTA) core decorated with two and four β-cyclodextrin (βCD) units were synthesized and fully characterized. Copper(I)-catalyzed alkyne–azide cycloaddition (CuAAC) click chemistry under microwave irradiation was used to obtain the target compounds with yields [...] Read more.
In this work, two dendritic molecules containing an ethylenediaminetetraacetic acid (EDTA) core decorated with two and four β-cyclodextrin (βCD) units were synthesized and fully characterized. Copper(I)-catalyzed alkyne–azide cycloaddition (CuAAC) click chemistry under microwave irradiation was used to obtain the target compounds with yields up to 99%. The classical ethylenediamine (EDA) core present in PAMAM dendrimers was replaced by an EDTA core, obtaining platforms that increase the water solubility at least 80 times compared with native βCD. The synthetic methodology presented here represents a convenient alternative for the rapid and efficient construction of PAMAM analogs. These molecules are envisaged for future applications as drug carriers. Full article
(This article belongs to the Special Issue Applications of Dendrimers in Biomedicine)
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Review

Jump to: Research

18 pages, 2885 KiB  
Review
Dendrimers in Corneal Drug Delivery: Recent Developments and Translational Opportunities
by Anubhav Dhull, Carson Yu, Alex Hunter Wilmoth, Minjie Chen, Anjali Sharma and Samuel Yiu
Pharmaceutics 2023, 15(6), 1591; https://doi.org/10.3390/pharmaceutics15061591 - 25 May 2023
Cited by 13 | Viewed by 2834
Abstract
Dendrimers are biocompatible organic nanomaterials with unique physicochemical properties, making them the focus of recent research in drug delivery. The cornea of the human eye presents a challenge for drug transit due to its inherently impenetrable nature, requiring nanocarrier-mediated targeted drug delivery. This [...] Read more.
Dendrimers are biocompatible organic nanomaterials with unique physicochemical properties, making them the focus of recent research in drug delivery. The cornea of the human eye presents a challenge for drug transit due to its inherently impenetrable nature, requiring nanocarrier-mediated targeted drug delivery. This review intends to examine recent advancements in the use of dendrimers for corneal drug delivery, including their properties and their potential for treating various ocular diseases. The review will also highlight the benefit of the novel technologies that have been developed and applied in the field, such as corneal targeting, drug release kinetics, treatments for dry eye disease, antibacterial drug delivery, corneal inflammation, and corneal tissue engineering. The review seeks to provide a comprehensive overview of the current state of research in this field, along with the translational developments in the field of dendrimer-based therapeutics and imaging agents and inspire the potential for future developments and translational opportunities in dendrimers based corneal drug delivery. Full article
(This article belongs to the Special Issue Applications of Dendrimers in Biomedicine)
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60 pages, 3218 KiB  
Review
Dendrimers and Derivatives as Multifunctional Nanotherapeutics for Alzheimer’s Disease
by Débora A. Moreira, Sofia D. Santos, Victoria Leiro and Ana P. Pêgo
Pharmaceutics 2023, 15(4), 1054; https://doi.org/10.3390/pharmaceutics15041054 - 24 Mar 2023
Cited by 10 | Viewed by 5242
Abstract
Alzheimer’s disease (AD) is the most prevalent form of dementia. It affects more than 30 million people worldwide and costs over US$ 1.3 trillion annually. AD is characterized by the brain accumulation of amyloid β peptide in fibrillar structures and the accumulation of [...] Read more.
Alzheimer’s disease (AD) is the most prevalent form of dementia. It affects more than 30 million people worldwide and costs over US$ 1.3 trillion annually. AD is characterized by the brain accumulation of amyloid β peptide in fibrillar structures and the accumulation of hyperphosphorylated tau aggregates in neurons, both leading to toxicity and neuronal death. At present, there are only seven drugs approved for the treatment of AD, of which only two can slow down cognitive decline. Moreover, their use is only recommended for the early stages of AD, meaning that the major portion of AD patients still have no disease-modifying treatment options. Therefore, there is an urgent need to develop efficient therapies for AD. In this context, nanobiomaterials, and dendrimers in particular, offer the possibility of developing multifunctional and multitargeted therapies. Due to their intrinsic characteristics, dendrimers are first-in-class macromolecules for drug delivery. They have a globular, well-defined, and hyperbranched structure, controllable nanosize and multivalency, which allows them to act as efficient and versatile nanocarriers of different therapeutic molecules. In addition, different types of dendrimers display antioxidant, anti-inflammatory, anti-bacterial, anti-viral, anti-prion, and most importantly for the AD field, anti-amyloidogenic properties. Therefore, dendrimers can not only be excellent nanocarriers, but also be used as drugs per se. Here, the outstanding properties of dendrimers and derivatives that make them excellent AD nanotherapeutics are reviewed and critically discussed. The biological properties of several dendritic structures (dendrimers, derivatives, and dendrimer-like polymers) that enable them to be used as drugs for AD treatment will be pointed out and the chemical and structural characteristics behind those properties will be analysed. The reported use of these nanomaterials as nanocarriers in AD preclinical research is also presented. Finally, future perspectives and challenges that need to be overcome to make their use in the clinic a reality are discussed. Full article
(This article belongs to the Special Issue Applications of Dendrimers in Biomedicine)
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29 pages, 3178 KiB  
Review
Properties and Bioapplications of Amphiphilic Janus Dendrimers: A Review
by Adina Căta, Ioana Maria Carmen Ienașcu, Mariana Nela Ştefănuț, Dan Roșu and Oana-Raluca Pop
Pharmaceutics 2023, 15(2), 589; https://doi.org/10.3390/pharmaceutics15020589 - 9 Feb 2023
Cited by 15 | Viewed by 3230
Abstract
Amphiphilic Janus dendrimers are arrangements containing both hydrophilic and hydrophobic units, capable of forming ordered aggregates by intermolecular noncovalent interactions between the dendrimer units. Compared to conventional dendrimers, these molecular self-assemblies possess particular and effective attributes i.e., the presence of different terminal groups, [...] Read more.
Amphiphilic Janus dendrimers are arrangements containing both hydrophilic and hydrophobic units, capable of forming ordered aggregates by intermolecular noncovalent interactions between the dendrimer units. Compared to conventional dendrimers, these molecular self-assemblies possess particular and effective attributes i.e., the presence of different terminal groups, essential to design new elaborated materials. The present review will focus on the pharmaceutical and biomedical application of amphiphilic Janus dendrimers. Important information for the development of novel optimized pharmaceutical formulations, such as structural classification, synthetic pathways, properties and applications, will offer the complete characterization of this type of Janus dendrimers. This work will constitute an up-to-date background for dendrimer specialists involved in designing amphiphilic Janus dendrimer-based nanomaterials for future innovations in this promising field. Full article
(This article belongs to the Special Issue Applications of Dendrimers in Biomedicine)
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21 pages, 2519 KiB  
Review
Dendrimers as Modifiers of Inorganic Nanoparticles for Therapeutic Delivery in Cancer
by Mkhuseli Zenze, Aliscia Daniels and Moganavelli Singh
Pharmaceutics 2023, 15(2), 398; https://doi.org/10.3390/pharmaceutics15020398 - 24 Jan 2023
Cited by 25 | Viewed by 3678
Abstract
The formulation of nanoscale systems with well-defined sizes and shapes is of great interest in applications such as drug and gene delivery, diagnostics and imaging. Dendrimers are polymers that have attracted interest due to their size, shape, branching length, amine density, and surface [...] Read more.
The formulation of nanoscale systems with well-defined sizes and shapes is of great interest in applications such as drug and gene delivery, diagnostics and imaging. Dendrimers are polymers that have attracted interest due to their size, shape, branching length, amine density, and surface functionalities. These unique characteristics of dendrimers set them apart from other polymers, their ability to modify nanoparticles (NPs) for biomedical applications. Dendrimers are spherical with multiple layers over their central core, each representing a generation. Their amphiphilic nature and hollow structure allow for the incorporation of multiple drugs or genes, in addition to enabling easy surface modification with cellular receptor-targeting moieties to ensure site-specific delivery of therapeutics. Dendrimers are employed in chemotherapeutic applications for the delivery of anticancer drugs. There are many inorganic NPs currently being investigated for cancer therapy, each with their own unique biological, chemical, and physical properties. To favor biomedical applications, inorganic NPs require suitable polymers to ensure stability, biodegradability and target specificity. The success of dendrimers is dependent on their unique structure, good bioavailability and stability. In this review, we describe the properties of dendrimers and their use as modifiers of inorganic NPs for enhanced therapeutic delivery. Herein, we review the significant developments in this area from 2015 to 2022. Databases including Web of Science, Scopus, Google Scholar, Science Direct, BioMed Central (BMC), and PubMed were searched for articles using dendrimers, inorganic nanoparticles and cancer as keywords. Full article
(This article belongs to the Special Issue Applications of Dendrimers in Biomedicine)
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