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Pharmaceutics
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Application of Polymeric Nanoparticles in Pulmonary Drug Delivery
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Application of Polymeric Nanoparticles in Pulmonary Drug Delivery

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

Deadline for manuscript submissions: 30 September 2024 | Viewed by 7130

Special Issue Editor

Dr. Ivana D'Angelo

E-Mail Website
Guest Editor
Department of Environmental, Biological and Pharmaceutical Sciences and Technologies, University of Campania “Luigi Vanvitelli”, 81100 Caserta, Italy
Interests: drug delivery; pharmaceutical technology; polymeric micro/nanoparticles; micro- and nanoemulsions; transmucosal and pulmonary drug delivery; antimicrobial delivery

Special Issue Information

Dear Colleagues,

Drug delivery to the lung through polymeric nanoparticles is considered a promising approach that may offer new opportunities to boost the research and marketing of inhaled products as well as enhance clinical responses in both local and systemic treatments. Due to the efficiency of lung clearance mechanisms and the multiple barriers imposed by the lungs, control of nanoparticle physicochemical properties, such as size, shape, surface and aerodynamic properties, is mandatory for improving stability of the drug in lungs and promote its transport across extracellular and cellular barriers. To achieve effective drug pulmonary delivery, optimized polymeric nanoparticles can be obtained by merging the appropriate materials and production techniques. Recent advances in nanotechnology have provided promising solutions in this field; nevertheless, there are still important issues to address and clarify, such as nanoparticle stability, mucociliary and phagocytic clearance, immunogenicity, toxicity and lung accumulation after inhalation.

This Special Issue aims to highlight current research advances in the design and development of inhalable polymeric nanoparticles, with a special focus on novel technological strategies capable of improving the compatibility of nanoparticles with the lung milieu and, thus, their safety and effectiveness.

Dr. Ivana D'Angelo
Guest Editor

Manuscript Submission Information

Manuscripts should be submitted online at www.mdpi.com by registering and logging in to this website. Once you are registered, click here to go to the submission form. Manuscripts can be submitted until the deadline. All submissions that pass pre-check are peer-reviewed. Accepted papers will be published continuously in the journal (as soon as accepted) and will be listed together on the special issue website. Research articles, review articles as well as short communications are invited. For planned papers, a title and short abstract (about 100 words) can be sent to the Editorial Office for announcement on this website.

Submitted manuscripts should not have been published previously, nor be under consideration for publication elsewhere (except conference proceedings papers). All manuscripts are thoroughly refereed through a single-blind peer-review process. A guide for authors and other relevant information for submission of manuscripts is available on the Instructions for Authors page. Pharmaceutics is an international peer-reviewed open access monthly journal published by MDPI.

Please visit the Instructions for Authors page before submitting a manuscript. The Article Processing Charge (APC) for publication in this open access journal is 2900 CHF (Swiss Francs). Submitted papers should be well formatted and use good English. Authors may use MDPI's English editing service prior to publication or during author revisions.

Keywords

  • polymeric nanoparticles
  • lung delivery
  • inhalable formulations
  • nanoparticle properties
  • aerosolization
  • nanoparticle/mucus interactions

Published Papers (4 papers)

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Research

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21 pages, 4509 KiB  
Article
Sustained-Release Powders Based on Polymer Particles for Pulmonary Delivery of Beclomethasone Dipropionate in the Treatment of Lung Inflammation
by Emanuela Fabiola Craparo, Salvatore Emanuele Drago, Gabriella Costabile, Maria Ferraro, Elisabetta Pace, Roberto Scaffaro, Francesca Ungaro and Gennara Cavallaro
Pharmaceutics 2023, 15(4), 1248; https://doi.org/10.3390/pharmaceutics15041248 - 14 Apr 2023
Cited by 3 | Viewed by 1345
Abstract
Inhaled corticosteroids are the mainstay in the management of lung inflammation associated to chronic lung diseases, such as asthma and chronic obstructive pulmonary disease (COPD). Nonetheless, available inhalation products are mostly short-acting formulations that require frequent administrations and do not always produce the [...] Read more.
Inhaled corticosteroids are the mainstay in the management of lung inflammation associated to chronic lung diseases, such as asthma and chronic obstructive pulmonary disease (COPD). Nonetheless, available inhalation products are mostly short-acting formulations that require frequent administrations and do not always produce the desired anti-inflammatory effects. In this work, the production of inhalable beclomethasone dipropionate (BDP) dry powders based on polymeric particles was attempted. As starting material, the PHEA-g-RhB-g-PLA-g-PEG copolymer was chosen, obtained by grafting 0.6, 2.4 and 3.0 mol%, respectively, of rhodamine (RhB), polylactic acid (PLA) and polyethylene glycol 5000 (PEG) on alpha,beta-poly(N-2-hydroxyethyl)DL-aspartamide (PHEA). The drug was loaded into the polymeric particles (MP) as an inclusion complex (CI) with hydroxypropyl–cyclodextrin (HP-β-Cyd) (at a stoichiometric ratio of 1:1) or as free form. The spray-drying (SD) process to produce MPs was optimized by keeping the polymer concentration (0.6 wt/vol%) constant in the liquid feed and by varying other parameters such as the drug concentration. The theoretical aerodynamic diameter (daer) values among the MPs are comparable and potentially suitable for inhalation, as confirmed also through evaluation of the experimental mass median aerodynamic diameter (MMADexp). BDP shows a controlled release profile from MPs that is significantly higher (more than tripled) than from Clenil®. In vitro tests on bronchial epithelial cells (16HBE) and adenocarcinomic human alveolar basal epithelial cells (A549) showed that all the MP samples (empty or drug-loaded) were highly biocompatible. None of the systems used induced apoptosis or necrosis. Moreover, the BDP loaded into the particles (BDP-Micro and CI-Micro) was more efficient than free BDP to counteract the effects of cigarette smoke and LPS on release of IL-6 and IL-8. Full article
(This article belongs to the Special Issue Application of Polymeric Nanoparticles in Pulmonary Drug Delivery)
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14 pages, 2591 KiB  
Article
Quality by Design as a Tool in the Optimisation of Nanoparticle Preparation—A Case Study of PLGA Nanoparticles
by Anna-Maria Struzek and Regina Scherließ
Pharmaceutics 2023, 15(2), 617; https://doi.org/10.3390/pharmaceutics15020617 - 12 Feb 2023
Cited by 1 | Viewed by 2014
Abstract
Nanoparticles can be used as drug carriers in various applications (e.g., in pulmonary drug delivery and mucosal vaccination). For further investigations, such as drug release studies, as well as for cell and tissue targeting, particles with defined properties are needed. The purpose of [...] Read more.
Nanoparticles can be used as drug carriers in various applications (e.g., in pulmonary drug delivery and mucosal vaccination). For further investigations, such as drug release studies, as well as for cell and tissue targeting, particles with defined properties are needed. The purpose of the study was to show a multi-step systematic method utilising quality by design to ensure the quality of ovalbumin loaded polylactic-co-glycolic acid nanoparticles (OVA-PLGA-NP), which can be delivered to the lung, and to gain knowledge of the preparation method (double-emulsion solvent evaporation method) in an early development process. Within a definitive screening design, several process parameters (OVA, PLGA and stabiliser concentrations, stirring time and stirring speed of inner emulsion and stirring time and stirring speed of double emulsion) were varied to analyse their impact on resulting properties (z-average, PDI, loading efficiency and loading capacity). The results showed that the preparation of the inner emulsion mainly influenced the drug loading, while the parameters of the second emulsifying step controlled the size. Then a central composite response surface design was used to achieve a predictable OVA-PLGA-NP with an average particle size of 700 nm and high drug-loading. This also enabled the demonstration of curvature and interaction of the stabiliser and the PLGA concentration. Full article
(This article belongs to the Special Issue Application of Polymeric Nanoparticles in Pulmonary Drug Delivery)
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20 pages, 33126 KiB  
Article
Inhalable Polymeric Nanoparticles for Pulmonary Delivery of Antimicrobial Peptide SET-M33: Antibacterial Activity and Toxicity In Vitro and In Vivo
by Laura Cresti, Gemma Conte, Giovanni Cappello, Jlenia Brunetti, Chiara Falciani, Luisa Bracci, Fabiana Quaglia, Francesca Ungaro, Ivana d’Angelo and Alessandro Pini
Pharmaceutics 2023, 15(1), 3; https://doi.org/10.3390/pharmaceutics15010003 - 20 Dec 2022
Cited by 5 | Viewed by 2148
Abstract
Development of inhalable formulations for delivering peptides to the conductive airways and shielding their interactions with airway barriers, thus enhancing peptide/bacteria interactions, is an important part of peptide-based drug development for lung applications. Here, we report the construction of a biocompatible nanosystem where [...] Read more.
Development of inhalable formulations for delivering peptides to the conductive airways and shielding their interactions with airway barriers, thus enhancing peptide/bacteria interactions, is an important part of peptide-based drug development for lung applications. Here, we report the construction of a biocompatible nanosystem where the antimicrobial peptide SET-M33 is encapsulated within polymeric nanoparticles of poly(lactide-co-glycolide) (PLGA) conjugated with polyethylene glycol (PEG). This system was conceived for better delivery of the peptide to the lungs by aerosol. The encapsulated peptide showed prolonged antibacterial activity, due to its controlled release, and much lower toxicity than the free molecule. The peptide-based nanosystem killed Pseudomonas aeruginosa in planktonic and sessile forms in a dose-dependent manner, remaining active up to 72 h after application. The encapsulated peptide showed no cytotoxicity when incubated with human bronchial epithelial cells from healthy individuals and from cystic fibrosis patients, unlike the free peptide, which showed an EC50 of about 22 µM. In vivo acute toxicity studies in experimental animals showed that the peptide nanosystem did not cause any appreciable side effects, and confirmed its ability to mitigate the toxic and lethal effects of free SET-M33. Full article
(This article belongs to the Special Issue Application of Polymeric Nanoparticles in Pulmonary Drug Delivery)
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Review

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31 pages, 1516 KiB  
Review
State-of-the-Art Review on Inhalable Lipid and Polymer Nanocarriers: Design and Development Perspectives
by Gabriella Costabile, Gemma Conte, Susy Brusco, Pouria Savadi, Agnese Miro, Fabiana Quaglia, Ivana d’Angelo and Francesca Ungaro
Pharmaceutics 2024, 16(3), 347; https://doi.org/10.3390/pharmaceutics16030347 - 01 Mar 2024
Viewed by 944
Abstract
Nowadays, the interest in research towards the local administration of drugs via the inhalation route is growing as it enables the direct targeting of the lung tissue, at the same time reducing systemic side effects. This is of great significance in the era [...] Read more.
Nowadays, the interest in research towards the local administration of drugs via the inhalation route is growing as it enables the direct targeting of the lung tissue, at the same time reducing systemic side effects. This is of great significance in the era of nucleic acid therapeutics and personalized medicine for the local treatment of severe lung diseases. However, the success of any inhalation therapy is driven by a delicate interplay of factors, such as the physiochemical profile of the payload, formulation, inhalation device, aerodynamic properties, and interaction with the lung fluids. The development of drug delivery systems tailored to the needs of this administration route is central to its success and to revolutionize the treatment of respiratory diseases. With this review, we aim to provide an up-to-date overview of advances in the development of nanoparticulate carriers for drug delivery to the lung tissue, with special regard concerning lipid and polymer-based nanocarriers (NCs). Starting from the biological barriers that the anatomical structure of the lung imposes, and that need to be overcome, the current strategies to achieve efficient lung delivery and the best support for the success of NCs for inhalation are highlighted. Full article
(This article belongs to the Special Issue Application of Polymeric Nanoparticles in Pulmonary Drug Delivery)
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