Nanoparticle-Mediated Targeted 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 3638

Special Issue Editors


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Guest Editor
Laboratoire d’Imagerie Biomédicale Multimodale, BIOMAPS, Université Paris-Saclay, CEA, CNRS, Inserm, Service Hospitalier Frédéric Joliot, 4 Place du Général Leclerc, 91401 Orsay, France
Interests: blood-brain barrier; organic anion transporters; breast cancer resistance protein; vanadate-sensitive ATPase; multiple drug resistance
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Tashima Laboratories of Arts and Sciences, 1239-5 Toriyama-cho, Kohoku-ku, Yokohama 222-0035, Japan
Interests: drug design; drug discovery; pharmacophore; drug delivery; organic synthesis; drug cell-membrane permeability; pharmaceutical sciences; medicinal chemistry; chemical biology
Special Issues, Collections and Topics in MDPI journals

Special Issue Information

Dear Colleagues,

We will be serving as Guest Editors for this very interesting Special Issue on “Nanoparticle-Mediated Targeted Drug Delivery Systems”. In drug research and development, delivering drugs to the target sites is crucial to avoid serious off-target side effects and ensure effective medical treatment. Specifically, certain anti-cancer drugs exhibit their activity not only on cancer cells but also on normal cells, causing side effects such as nausea, skin disorders, or hair loss. Central nervous system drug candidates face challenges in penetrating the brain due to the blood–brain barrier. Furthermore, incorrect drug distribution can often lead to adverse events in terms of other diseases. Therefore, precision drug delivery should be enhanced and eventually established. The modification of nanoparticles is relatively straightforward. Consequently, a variety of useful nanoparticles can be produced for drug-controlled release, barrier permeation, including cell membranes, and/or targeting. Additionally, nanoparticles protect their cargos from degradation by enzymes and inhibit their unsuitable activity expression, reducing the risk of off-target side effects. Multiple strategies can be integrated into nanoparticles. Currently, pharmaceutical researchers and healthcare workers are increasingly interested in nanoparticle-mediated targeted drug delivery systems. Drug-loaded nanoparticles are employed differently based on the purpose and target area. Drug delivery systems utilizing nanoparticles as carriers represent promising strategies for achieving intelligent drug distribution. This Special Issue aims to disseminate recent progress and trends in this field. We welcome submissions of all types of original articles related to nanoparticles used for medical treatments.

Topics include, but are not limited to, the strategies outlined below.

˗ As a constituent, nanoparticles are mainly composed of the following:

  • Biodegradable artificial polymers;
  • Natural polymers (chitosan, PLGA, PGA, etc.);
  • Lipids (liposomes, micelles, exosomes, etc.);
  • Inorganic materials (Au, Si, Fe3O4, etc.);
  • Organic materials (albumin, monoclonal antibodies, virosome, etc.);
  • Emulsions;
  • Other components.

˗ Practically, functionalized or engineered nanoparticles demonstrate the following:

  • Passive targeting feature based on the enhanced permeability and retention effect particularly in solid cancers;
  • Active targeting feature based on ligand–receptor interactions inducing receptor-mediated endocytosis;
  • Magnetic feature;
  • pH-sensitive feature;
  • Thermosensitive feature;
  • Enteric feature in case of oral administration;
  • Other useful features.

˗ As drug therapy, nanoparticles are used for the treatment of the following:

  • Cancers;
  • Central nervous system diseases (Alzheimer's disease, Parkinson's disease, ischemic stroke, glioma, etc.);
  • Infectious diseases (influenza, cytomegalovirus, COVID-19, etc.);
  • Cardiovascular diseases;
  • Lung diseases;
  • Eye diseases;
  • Other diseases.

˗ As cargo, nanoparticles load or encapsulate the following:

  • Low-molecular-weight compounds;
  • Peptides;
  • Nucleic acids;
  • Other compounds.

˗ Other relevant topics.

Dr. Nicolas Tournier
Dr. Toshihiko Tashima
Guest Editors

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Keywords

  • drug delivery system
  • nanodelivery system
  • nanoparticle
  • receptor-mediated endocytosis/transcytosis
  • enhanced permeability and retention effect (EPR effect)
  • cancer therapy
  • central nervous system disease therapy
  • liposomes
  • exosomes
  • RNA delivery

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Published Papers (3 papers)

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Research

13 pages, 2136 KiB  
Article
Development of a Water-Soluble Nanomicellar Formulation Loaded with Trans-Resveratrol Using Polyethylene Glycol Monostearate for the Treatment of Intracerebral Hemorrhage
by Kengo Banshoya, Aoi Machida, Saki Kawamura, Tetsuhiro Yamada, Riko Okada, Yui Kawamoto, Hikaru Kimura, Sachi Shibata, Yuhzo Hieda, Yoshiharu Kaneo, Tetsuro Tanaka and Masatoshi Ohnishi
Pharmaceutics 2024, 16(11), 1462; https://doi.org/10.3390/pharmaceutics16111462 - 15 Nov 2024
Viewed by 353
Abstract
Background/Objectives: Trans-resveratrol (Res) has been reported to possess many biological activities, including neuroprotective effects, owing to its anti-inflammatory and antioxidant properties. However, Res has very low water solubility, which limits its therapeutic application. In this work, we formulated water-soluble micellar formulations incorporating Res [...] Read more.
Background/Objectives: Trans-resveratrol (Res) has been reported to possess many biological activities, including neuroprotective effects, owing to its anti-inflammatory and antioxidant properties. However, Res has very low water solubility, which limits its therapeutic application. In this work, we formulated water-soluble micellar formulations incorporating Res using polyethylene glycol monostearate (stPEG). Methods: These formulations (stPEG/Res) were developed using five types of stPEG containing 10, 25, 40, 55 and 140 PEG repeat units. The formulations were characterized for Res content, water solubility, particle size, zeta potential, precipitation, biodistribution, and efficacy against neuronal and motor dysfunction in intracerebral hemorrhage (ICH). Results: Intravenous administration of stPEG40/Res, which demonstrated particle size, water solubility, and biodistribution properties suitable for intravenous administration, suppressed neurological and motor dysfunction following in a collagenase-induced ICH mouse model. These effects were inhibited by zinc protoporphyrin-9, an inhibitor of the antioxidant enzyme heme oxygenase-1, suggesting that Res contributes to antioxidant enzyme expression and anti-inflammatory activity. Conclusions: The stPEG/Res micellar formulation developed in this study may offer a promising therapeutic approach for ICH treatment. Full article
(This article belongs to the Special Issue Nanoparticle-Mediated Targeted Drug Delivery Systems)
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16 pages, 4197 KiB  
Article
Peptide Functionalization of Emulsion-Based Nanocarrier to Improve Uptake across Blood–Brain Barrier
by Alberta De Capua, Raffaele Vecchione, Cinzia Sgambato, Marco Chino, Elena Lagreca, Angela Lombardi and Paolo Antonio Netti
Pharmaceutics 2024, 16(8), 1010; https://doi.org/10.3390/pharmaceutics16081010 - 30 Jul 2024
Viewed by 964
Abstract
New strategies for enhancing drug delivery to the blood–brain barrier (BBB) represent a major challenge in treating cerebral diseases. Nanoemulsion-based nanocarriers represent an ideal candidate to improve drug delivery thanks to their versatility in functionalization and cargo protection. In this work, a paclitaxel-loaded [...] Read more.
New strategies for enhancing drug delivery to the blood–brain barrier (BBB) represent a major challenge in treating cerebral diseases. Nanoemulsion-based nanocarriers represent an ideal candidate to improve drug delivery thanks to their versatility in functionalization and cargo protection. In this work, a paclitaxel-loaded nano-emulsion has been firstly functionalized and stabilized with two layers constituted of chitosan and hyaluronic acid, and, secondly, the latter has been conjugated to the CRT peptide. CRT is a bioactive peptide that selectively recognizes bEnd.3 cells, a model of the BBB, thanks to its interactions with transferrin (Tf) and its receptor (TfR). Cytotoxic results showed a 41.5% higher uptake of CRT functionalized nano-emulsion than the negative control, demonstrating the ability of this novel tool to be accumulated in brain endothelium tissue. Based upon these results, our approach can be fully generalizable to the design of multifunctional nanocarriers for delivery of therapeutic agents to the central nervous systems. Full article
(This article belongs to the Special Issue Nanoparticle-Mediated Targeted Drug Delivery Systems)
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14 pages, 2993 KiB  
Article
Evaluation of Novel Nasal Mucoadhesive Nanoformulations Containing Lipid-Soluble EGCG for Long COVID Treatment
by Nicolette Frank, Douglas Dickinson, Garrison Lovett, Yutao Liu, Hongfang Yu, Jingwen Cai, Bo Yao, Xiaocui Jiang and Stephen Hsu
Pharmaceutics 2024, 16(6), 791; https://doi.org/10.3390/pharmaceutics16060791 - 11 Jun 2024
Cited by 1 | Viewed by 1491
Abstract
Following recovery from the acute infection stage of the SARS-CoV-2 virus (COVID-19), survivors can experience a wide range of persistent Post-Acute Sequelae of COVID-19 (PASC), also referred to as long COVID. According to the US National Research Action Plan on Long COVID 2022, [...] Read more.
Following recovery from the acute infection stage of the SARS-CoV-2 virus (COVID-19), survivors can experience a wide range of persistent Post-Acute Sequelae of COVID-19 (PASC), also referred to as long COVID. According to the US National Research Action Plan on Long COVID 2022, up to 23.7 million Americans suffer from long COVID, and approximately one million workers may be out of the workforce each day due to these symptoms, leading to a USD 50 billion annual loss of salary. Neurological symptoms associated with long COVID result from persistent infection with SARS-CoV-2 in the nasal neuroepithelial cells, leading to inflammation in the central nervous system (CNS). As of today, there is no evidence that vaccines or medications can clear the persistent viral infection in olfactory mucosa. Recently published clinical data demonstrate that only 5% of long COVID anosmia patients have fully recovered during the past 2 years, and 10.4% of COVID patients are still symptomatic 18 months post-infection. Our group demonstrated that epigallocatechin-3-gallate-monopalmitate (EC16m) nanoformulations possess strong antiviral activity against human coronavirus, suggesting that this green-tea-derived compound in nanoparticle formulations could be developed as an intranasally delivered new drug targeting the persistent SARS-CoV-2 infection, as well as inflammation and oxidative stress in the CNS, leading to restoration of neurologic functions. The objective of the current study was to evaluate the mucociliary safety of the EC16m nasal nanoformulations and their efficacy against human coronavirus. Methods: Nanoparticle size and Zeta potential were measured using the ZetaView Nanoparticle Tracking Analysis system; mucociliary safety was determined using the MucilAir human nasal model; contact antiviral activity and post-infection inhibition against the OC43 viral strain were assessed by the TCID50 assay for cytopathic effect on MRC-5 cells. Results: The saline-based EC16 mucoadhesive nanoformulations containing 0.005 to 0.02% w/v EC16m have no significant difference compared to saline (0.9% NaCl) with respect to tissue integrity, cytotoxicity, and cilia beat frequency. A 5 min contact resulted in 99.9% inactivation of β-coronavirus OC43. OC43 viral replication was inhibited by >90% after infected MRC-5 cells were treated with the formulations. Conclusion: The saline-based novel EC16m mucoadhesive nasal nanoformulations rapidly inactivated human coronavirus with mucociliary safety properties comparable to saline, a solution widely used for nasal applications. Full article
(This article belongs to the Special Issue Nanoparticle-Mediated Targeted Drug Delivery Systems)
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