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Pharmaceutics
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Next Generation of PLGA-Based Nanoparticles as Drug Delivery Systems for...
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Next Generation of PLGA-Based Nanoparticles as Drug Delivery Systems for Biomedical Applications

A special issue of Pharmaceutics (ISSN 1999-4923). This special issue belongs to the section "Drug Delivery and Controlled Release".

Deadline for manuscript submissions: 10 May 2024 | Viewed by 4358

Special Issue Editors

Prof. Dr. Piera Di Martino

E-Mail Website
Guest Editor
Department of Pharmacy, University G. D’Annunzio Chieti-Pescara, 66100 Chieti, Italy
Interests: nanomedicines; hydrogels; nanoparticles; nanohydrogels; drug delivery systems
Special Issues, Collections and Topics in MDPI journals
Dr. Maria Rosa Gigliobianco

E-Mail Website
Guest Editor
School of Pharmacy, University of Camerino, 62032 Camerino, Italy
Interests: drug delivery formulations; polymeric nanoparticles; functionalization of biocompatible polymers; nanotechnology

Special Issue Information

Dear Colleagues,

This Special Issue is dedicated to advanced PLGA-based nanotechnology research on biomedical applications.

The development of novel and cutting-edge treatments for disease is a relevant health matter on a global scale. As a result, we are constantly researching safe therapies and medications that can precisely target the site of diseases with the optimal duration of action, minimal side effects, and an ideal pharmacokinetic profile. Over the last few decades, polymeric nanoparticles used in the drug delivery field have successfully addressed most of these therapeutic objectives. Poly (lactic-co-glycolic acid) (PLGA) is a type of medical polymer that is most commonly used due to its excellent biocompatibility and tunable degradation and release properties. It is also a versatile vehicle for transporting different types of drugs, including those that are hydrophobic or hydrophilic, small molecules or macromolecules, and protects them from degradation and uncontrolled release. In addition, PLGA-based nanoparticles can have their surface characteristics modified to enhance interactions with biological substrates. Moreover, they may be conjugated with target molecules to reach particular organs, tissues, or cells. They have been used for various medical applications, from vaccinations to therapies for cancer, neurological problems, inflammation, and other illnesses. There are several biomedical applications for PLGA-based nanoparticles, and the number of these is expected to rise as technology progresses.

Here, we focus on the latest advanced PLGA-based nanoparticles used in the biomedical field. This issue will include contributions of research applications on the technologies available for producing and analyzing PLGA nanoparticles, with a focus on novel biomedical applications and the most up-to-date scalability PLGA-based nanoparticle formulation methods.

In this Special Issue, original research articles and reviews are welcome. Research areas may include (but are not limited to) the following:

  • PLGA nanocarriers for cancer targeting;
  • PLGA nanocarriers for immunomodulation and vaccine formulations;
  • PLGA nanocarriers for inflammatory disorders;
  • Scalable fabrication techniques for polymeric nanoparticles;
  • Antibiotic resistance;
  • Theranostic applications.

I look forward to receiving your contributions.

Prof. Dr. Piera Di Martino
Dr. Maria Rosa Gigliobianco
Guest Editors

Manuscript Submission Information

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

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

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

Keywords

  • nanoparticles
  • drug delivery systems
  • PLGA
  • targeting
  • formulation techniques
  • encapsulation
  • polymer

Published Papers (4 papers)

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Research

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21 pages, 3239 KiB  
Article
Darunavir Nanoformulation Suppresses HIV Pathogenesis in Macrophages and Improves Drug Delivery to the Brain in Mice
by Lina Zhou, Sandip Godse, Namita Sinha, Sunitha Kodidela, Udai Singh and Santosh Kumar
Pharmaceutics 2024, 16(4), 555; https://doi.org/10.3390/pharmaceutics16040555 - 19 Apr 2024
Viewed by 329
Abstract
Although antiretroviral therapy (ART) can suppress peripheral HIV, patients still suffer from neuroHIV due to insufficient levels of ART drugs in the brain. Hence, this study focuses on developing a poly lactic-co-glycolic acid (PLGA) nanoparticle-based ART drug delivery system for darunavir (DRV) using [...] Read more.
Although antiretroviral therapy (ART) can suppress peripheral HIV, patients still suffer from neuroHIV due to insufficient levels of ART drugs in the brain. Hence, this study focuses on developing a poly lactic-co-glycolic acid (PLGA) nanoparticle-based ART drug delivery system for darunavir (DRV) using an intranasal route that can overcome the limitation of drug metabolic stability and blood–brain barrier (BBB) permeability. The physicochemical properties of PLGA-DRV were characterized. The results indicated that PLGA-DRV formulation inhibits HIV replication in U1 macrophages directly and in the presence of the BBB without inducing cytotoxicity. However, the PLGA-DRV did not inhibit HIV replication more than DRV alone. Notably, the total antioxidant capacity remained unchanged upon treatment with both DRV or PLGA-DRV in U1 cells. Compared to DRV alone, PLGA-DRV further decreased reactive oxygen species, suggesting a decrease in oxidative stress by the formulation. Oxidative stress is generally increased by HIV infection, leading to increased inflammation. Although the PLGA-DRV formulation did not further reduce the inflammatory response, the formulation did not provoke an inflammatory response in HIV-infected U1 macrophages. As expected, in vitro experiments showed higher DRV permeability by PLGA-DRV than DRV alone to U1 macrophages. Importantly, in vivo experiments, especially using intranasal administration of PLGA-DRV in wild-type mice, demonstrated a significant increase in the brain-to-plasma ratio of DRV compared to the free DRV. Overall, findings from this study attest to the potential of the PLGA-DRV nanoformulation in reducing HIV pathogenesis in macrophages and enhancing drug delivery to the brain, offering a promising avenue for treating HIV-related neurological disorders. Full article
(This article belongs to the Special Issue Next Generation of PLGA-Based Nanoparticles as Drug Delivery Systems for Biomedical Applications)
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25 pages, 5051 KiB  
Article
PEG–Lipid–PLGA Hybrid Particles for Targeted Delivery of Anti-Inflammatory Drugs
by Jana Ismail, Lea C. Klepsch, Philipp Dahlke, Ekaterina Tsarenko, Antje Vollrath, David Pretzel, Paul M. Jordan, Kourosh Rezaei, Justyna A. Czaplewska, Steffi Stumpf, Baerbel Beringer-Siemers, Ivo Nischang, Stephanie Hoeppener, Oliver Werz and Ulrich S. Schubert
Pharmaceutics 2024, 16(2), 187; https://doi.org/10.3390/pharmaceutics16020187 - 28 Jan 2024
Viewed by 1429
Abstract
Hybrid nanoparticles (HNPs) were designed by combining a PLGA core with a lipid shell that incorporated PEG–Lipid conjugates with various functionalities (-RGD, -cRGD, -NH2, and -COOH) to create targeted drug delivery systems. Loaded with a neutral lipid orange dye, the HNPs [...] Read more.
Hybrid nanoparticles (HNPs) were designed by combining a PLGA core with a lipid shell that incorporated PEG–Lipid conjugates with various functionalities (-RGD, -cRGD, -NH2, and -COOH) to create targeted drug delivery systems. Loaded with a neutral lipid orange dye, the HNPs were extensively characterized using various techniques and investigated for their uptake in human monocyte-derived macrophages (MDMs) using FC and CLSM. Moreover, the best-performing HNPs (i.e., HNP-COOH and HNP-RGD as well as HNP-RGD/COOH mixed) were loaded with the anti-inflammatory drug BRP-201 and prepared in two size ranges (dH ~140 nm and dH ~250 nm). The HNPs were examined further for their stability, degradation, MDM uptake, and drug delivery efficiency by studying the inhibition of 5-lipoxygenase (5-LOX) product formation, whereby HNP-COOH and HNP-RGD both exhibited superior uptake, and the HNP-COOH/RGD (2:1) displayed the highest inhibition. Full article
(This article belongs to the Special Issue Next Generation of PLGA-Based Nanoparticles as Drug Delivery Systems for Biomedical Applications)
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18 pages, 4156 KiB  
Article
Polymeric Particle BAM15 Targeting Macrophages Attenuates the Severity of LPS-Induced Sepsis: A Proof of Concept for Specific Immune Cell-Targeted Therapy
by Kanyarat Udompornpitak, Thansita Bhunyakarnjanarat, Wilasinee Saisorn, Chonnavee Manipuntee, Kittawat Plengplang, Samarch Sittichaitaweekul, Panisa Jenphatanapong, Suwasin Udomkarnjananun, Warerat Kaewduangduen, Kasirapat Ariya-anandech, Amanee Samaeng, Numpon Insin, Patcharee Ritprajak and Asada Leelahavanichkul
Pharmaceutics 2023, 15(12), 2695; https://doi.org/10.3390/pharmaceutics15122695 - 28 Nov 2023
Viewed by 987
Abstract
Macrophage polarization requires different energy sources and metabolic processes. Therefore, cell energy interference to alter macrophage functions has been proposed as a treatment for severe inflammatory diseases, including sepsis. In this study, targeting cell energy using BAM15 (a mitochondrial uncoupling agent) in human [...] Read more.
Macrophage polarization requires different energy sources and metabolic processes. Therefore, cell energy interference to alter macrophage functions has been proposed as a treatment for severe inflammatory diseases, including sepsis. In this study, targeting cell energy using BAM15 (a mitochondrial uncoupling agent) in human THP-1 and mouse RAW264.7 macrophages prominently interfered with M1 but not M2 polarization. Free BAM15 (BAM15) and BAM15-loaded PLGA particles (BAM15 particles) reduced the inflammatory response of M1 macrophages and enhanced the expression of M2 signature genes with the restoration of mitochondrial activity (extracellular flux analysis) in RAW264.7 cells. Furthermore, BAM15 particles but not BAM15 showed specific effects on the inflammatory response of macrophages but not neutrophils, and the particles were actively captured by splenic and liver macrophages in vivo. Administration of BAM15 and BAM15 particles attenuated the severity of sepsis in LPS-induced sepsis mice. Interestingly, BAM15 particles but not BAM15 alleviated LPS-induced liver injury by reducing hepatic inflammation. Our findings substantiate the superior efficacy of macrophage-targeted therapy using a BAM15 particle-delivery system and provide further support for clinical development as a potential therapy for severe inflammatory diseases. Full article
(This article belongs to the Special Issue Next Generation of PLGA-Based Nanoparticles as Drug Delivery Systems for Biomedical Applications)
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Review

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31 pages, 3570 KiB  
Review
Harnessing the Potential of PLGA Nanoparticles for Enhanced Bone Regeneration
by Mozan Hassan, Hiba Atiyah Abdelnabi and Sahar Mohsin
Pharmaceutics 2024, 16(2), 273; https://doi.org/10.3390/pharmaceutics16020273 - 15 Feb 2024
Viewed by 979
Abstract
Recently, nanotechnologies have become increasingly prominent in the field of bone tissue engineering (BTE), offering substantial potential to advance the field forward. These advancements manifest in two primary ways: the localized application of nanoengineered materials to enhance bone regeneration and their use as [...] Read more.
Recently, nanotechnologies have become increasingly prominent in the field of bone tissue engineering (BTE), offering substantial potential to advance the field forward. These advancements manifest in two primary ways: the localized application of nanoengineered materials to enhance bone regeneration and their use as nanovehicles for delivering bioactive compounds. Despite significant progress in the development of bone substitutes over the past few decades, it is worth noting that the quest to identify the optimal biomaterial for bone regeneration remains a subject of intense debate. Ever since its initial discovery, poly(lactic-co-glycolic acid) (PLGA) has found widespread use in BTE due to its favorable biocompatibility and customizable biodegradability. This review provides an overview of contemporary advancements in the development of bone regeneration materials using PLGA polymers. The review covers some of the properties of PLGA, with a special focus on modifications of these properties towards bone regeneration. Furthermore, we delve into the techniques for synthesizing PLGA nanoparticles (NPs), the diverse forms in which these NPs can be fabricated, and the bioactive molecules that exhibit therapeutic potential for promoting bone regeneration. Additionally, we addressed some of the current concerns regarding the safety of PLGA NPs and PLGA-based products available on the market. Finally, we briefly discussed some of the current challenges and proposed some strategies to functionally enhance the fabrication of PLGA NPs towards BTE. We envisage that the utilization of PLGA NP holds significant potential as a potent tool in advancing therapies for intractable bone diseases. Full article
(This article belongs to the Special Issue Next Generation of PLGA-Based Nanoparticles as Drug Delivery Systems for Biomedical Applications)
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