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Applied Sciences
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Polymeric Nanoparticles in Drug Delivery
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Polymeric Nanoparticles in Drug Delivery

A special issue of Applied Sciences (ISSN 2076-3417). This special issue belongs to the section "Nanotechnology and Applied Nanosciences".

Deadline for manuscript submissions: closed (20 August 2022) | Viewed by 25278

Special Issue Editors

Dr. Gianpiero Calabrese

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Guest Editor
Department of Pharmacy, Kingston University, London KT1 2EE, UK
Interests: drug delivery; polymeric nanoparticles; liposomes and carbon nanotubes for the targeting of the central nervous system; design; synthesis and formulation of boron-containing compounds for selective mitochondrial targeting in the boron neutron capture therapy of brain cancers; electronic cigarettes; analysis of content; public health issues related to pharmacy practice; pharmacology/toxicology; formulation
Special Issues, Collections and Topics in MDPI journals
Prof. Dr. Manuela Pintado

E-Mail Website
Guest Editor
Escola Superior de Biotecnologia, Universidade Católica Portuguesa, 4169-005 Porto, Portugal
Interests: biotechnology and biochemistry
Special Issues, Collections and Topics in MDPI journals

Special Issue Information

Dear Colleagues,

Polymeric nanoparticles are versatile systems employed to address various aspects of drug delivery: from improving oral bioavailability of drugs and facilitating the delivery of vaccines and antimicrobials, to increasing therapeutical efficacy in cancer treatment and promoting drug penetration through biological membranes such as the blood–brain barrier. Polymeric nanoparticles have enjoyed increasing popularity because of their favourable features of biocompatibility, biodegradability, low immunogenicity and, especially, their ability to deliver therapeutics to target cells with high efficiency. Polymers of natural or synthetic origin can be selected and methods for nanoparticle fabrication may vary from simple solvent evaporation to more complex procedures. Their physicochemical characteristics can be fine-tuned to enhance infiltration, stability, release and targeting to site of action; their nano size is key to allowing them to circulate in the body and cross biological barriers to target the tissue of interest in a stimuli-responsive fashion.

In this Special Issue, we invite submissions exploring innovation and originality in design, methods and applications of polymeric nanoparticles in drug delivery. Contributions can focus on single polymer or composite formulations, advanced methodologies of preparation and characterization, novel targeting strategies or applications. Survey papers and reviews are also welcomed.

Dr. Gianpiero Calabrese
Prof. Dr. Manuela Pintado
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. Applied Sciences is an international peer-reviewed open access semimonthly 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 2400 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
  • increased bioavailability
  • targeting
  • stimuli-responsive
  • nanoparticle characterization
  • fabrication

Published Papers (7 papers)

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Research

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15 pages, 3111 KiB  
Article
Erythropoietin Nanobots: Their Feasibility for the Controlled Release of Erythropoietin and Their Neuroprotective Bioequivalence in Central Nervous System Injury
by Thi Huong Le, Chanh Trung Nguyen, Kyo-in Koo and Chang Ho Hwang
Appl. Sci. 2022, 12(7), 3351; https://doi.org/10.3390/app12073351 - 25 Mar 2022
Viewed by 1492
Abstract
Background: Erythropoietin (EPO) plays important roles in neuroprotection in central nervous system injury. Due to the limited therapeutic time window and coexistence of hematopoietic/extrahematopoietic receptors displaying heterogenic and phylogenetic differences, fast, targeted delivery agents, such as nanobots, are needed. To confirm the feasibility [...] Read more.
Background: Erythropoietin (EPO) plays important roles in neuroprotection in central nervous system injury. Due to the limited therapeutic time window and coexistence of hematopoietic/extrahematopoietic receptors displaying heterogenic and phylogenetic differences, fast, targeted delivery agents, such as nanobots, are needed. To confirm the feasibility of EPO-nanobots (ENBs) as therapeutic tools, the authors evaluated controlled EPO release from ENBs and compared the neuroprotective bioequivalence of these substances after preconditioning sonication. Methods: ENBs were manufactured by a nanospray drying technique with preconditioning sonication. SH-SY5Y neuronal cells were cotreated with thapsigargin and either EPO or ENBs before cell viability, EPO receptor activation, and endoplasmic reticulum stress-related pathway deactivation were determined over 24 h. Results: Preconditioning sonication (50–60 kHz) for 1 h increased the cumulative EPO release from the ENBs (84% versus 25% at 24 h). Between EPO and ENBs at 24 h, both neuronal cell viability (both > 65% versus 15% for thapsigargin alone) and the expression of the proapoptotic/apoptotic biomolecular markers JAK2, PDI, PERK, GRP78, ATF6, CHOP, TGF-β, and caspase-3 were nearly the same or similar. Conclusion: ENBs controlled EPO release in vitro after preconditioning sonication, leading to neuroprotection similar to that of EPO at 24 h. Full article
(This article belongs to the Special Issue Polymeric Nanoparticles in Drug Delivery)
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27 pages, 8358 KiB  
Article
Formulation of Boron Encapsulated Smart Nanocapsules for Targeted Drug Delivery to the Brain
by Anis Daou, Raid G. Alany and Gianpiero Calabrese
Appl. Sci. 2021, 11(22), 10738; https://doi.org/10.3390/app112210738 - 14 Nov 2021
Cited by 2 | Viewed by 2123
Abstract
Drug delivery through the Blood–Brain Barrier (BBB) represents a significant challenge. Despite the current strategies to circumvent the BBB, nanotechnology offers unprecedented opportunities for combining selective delivery, improved bioavailability, drug protection, and enhanced pharmacokinetics profiles. Chitosan nanocarriers allow for a more efficacious strategy [...] Read more.
Drug delivery through the Blood–Brain Barrier (BBB) represents a significant challenge. Despite the current strategies to circumvent the BBB, nanotechnology offers unprecedented opportunities for combining selective delivery, improved bioavailability, drug protection, and enhanced pharmacokinetics profiles. Chitosan nanocarriers allow for a more efficacious strategy at the cellular and sub-cellular levels. Boron Neutron Capture Therapy (BNCT) is a targeted chemo-radiotherapeutic technique that allows the selective depletion of cancer cells by means of selective tagging of cancer cells with 10B, followed by irradiation with low-energy neutrons. Consequently, the combination of a polymer-based nanodelivery system enclosing an effective BNCT pharmacophore can potentially lead to the selective delivery of the load to cancer cells beyond the BBB. In this work, synthesized novel boronated agents based on carborane-functionalized Delocalized Lipophilic Cations (DLCs) are assessed for safety and selective targeting of tumour cells. The compounds are then encapsulated in nanocarriers constituted by chitosan to promote permeability through the BBB. Additionally, chitosan was used in combination with polypyrrole to form a smart composite nanocapsule, which is expected to release its drug load with variations in pH. Results indicate the achievement of more selective boron delivery to cells via carboranyl DLCs. Finally, preliminary cell studies indicate no toxicity was detected in chitosan nanocapsules, further enhancing its viability as a potential delivery vehicle in the BNCT of brain tumours. Full article
(This article belongs to the Special Issue Polymeric Nanoparticles in Drug Delivery)
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13 pages, 1220 KiB  
Article
Preparation, Characterization and Evaluation of Guar Films Impregnated with Relaxing Peptide Loaded into Chitosan Microparticles
by Patrícia Batista, Pedro M. Castro, Ana Raquel Madureira, Bruno Sarmento and Manuela Pintado
Appl. Sci. 2021, 11(21), 9849; https://doi.org/10.3390/app11219849 - 21 Oct 2021
Cited by 7 | Viewed by 1735
Abstract
Background: Biological molecules such as therapeutic proteins and peptides have provided ample opportunities for further improvements in health and wellbeing. However, such biomacromolecules face stability challenges regarding premature processing and digestion, whenever any enteric delivery route is considered. Hence, oral guar films entrapping [...] Read more.
Background: Biological molecules such as therapeutic proteins and peptides have provided ample opportunities for further improvements in health and wellbeing. However, such biomacromolecules face stability challenges regarding premature processing and digestion, whenever any enteric delivery route is considered. Hence, oral guar films entrapping peptide-containing chitosan microparticles have been developed as a new delivery system to carry and protect therapeutic relaxing peptides. Results: The composite films were characterized regarding physicochemical properties using FTIR as well as peptide encapsulation efficiency, cytotoxicity, and peptide permeability through buccal and intestinal cell-based models. The composite films with 0.18% (w/w) of peptide demonstrated ca. 0.63% of peptide loading efficiency into the chitosan microparticles and to be safe for buccal and intestinal epithelial cells up to 24 h of contact. The permeability assays through TR146 cells to mimic buccal mucosa epithelium and Caco-2/HT29-MTX to mimic duodenum conditions showed that the incorporation of peptide chitosan microparticles into guar-gum oral films offered a faster permeability, when compared with the free peptide and peptide-chitosan-microparticles-loaded chitosan. Conclusion: This study suggests that peptide-loaded chitosan microparticles into guar-gum oral films might be a promising carrier for enhancement of the buccal and intestinal absorption of a relaxing peptide. Full article
(This article belongs to the Special Issue Polymeric Nanoparticles in Drug Delivery)
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Review

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33 pages, 2123 KiB  
Review
Journey to the Market: The Evolution of Biodegradable Drug Delivery Systems
by Minze Zhu, Andrew K. Whittaker, Felicity Y. Han and Maree T. Smith
Appl. Sci. 2022, 12(2), 935; https://doi.org/10.3390/app12020935 - 17 Jan 2022
Cited by 17 | Viewed by 4278
Abstract
Biodegradable polymers have been used as carriers in drug delivery systems for more than four decades. Early work used crude natural materials for particle fabrication, whereas more recent work has utilized synthetic polymers. Applications include the macroscale, the microscale, and the nanoscale. Since [...] Read more.
Biodegradable polymers have been used as carriers in drug delivery systems for more than four decades. Early work used crude natural materials for particle fabrication, whereas more recent work has utilized synthetic polymers. Applications include the macroscale, the microscale, and the nanoscale. Since pioneering work in the 1960’s, an array of products that use biodegradable polymers to encapsulate the desired drug payload have been approved for human use by international regulatory agencies. The commercial success of these products has led to further research in the field aimed at bringing forward new formulation types for improved delivery of various small molecule and biologic drugs. Here, we review recent advances in the development of these materials and we provide insight on their drug delivery application. We also address payload encapsulation and drug release mechanisms from biodegradable formulations and their application in approved therapeutic products. Full article
(This article belongs to the Special Issue Polymeric Nanoparticles in Drug Delivery)
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34 pages, 8695 KiB  
Review
Application of Polymeric Nanocarriers for Enhancing the Bioavailability of Antibiotics at the Target Site and Overcoming Antimicrobial Resistance
by Hung Le, Carole Karakasyan, Thierry Jouenne, Didier Le Cerf and Emmanuelle Dé
Appl. Sci. 2021, 11(22), 10695; https://doi.org/10.3390/app112210695 - 12 Nov 2021
Cited by 17 | Viewed by 4909
Abstract
Antimicrobial resistance is one of the greatest threats to global health. Although the efforts in antibiotic drug discovery continue to play a pivotal role, this solution alone probably will not be enough to ensure the required level of infection control in the future. [...] Read more.
Antimicrobial resistance is one of the greatest threats to global health. Although the efforts in antibiotic drug discovery continue to play a pivotal role, this solution alone probably will not be enough to ensure the required level of infection control in the future. New strategies and innovative modes of action are desperately needed to preserve the effectiveness of antimicrobials. Accordingly, antibiotic delivery based on polymeric nanoparticles is one of the possible methods that has been recently explored to improve their pharmacokinetic profile. Through optimized access of antibiotics to their sites of action, nanocarriers can unlock the full potential of the antibiotic cargoes, extend the antimicrobial spectrum, and reduce the required dose of antibiotic while preserving efficacy. Additionally, the use of an antibiotic-loaded nanocarrier is also considered a steady solution as novel molecules can be continuously developed and incorporated into the delivery platform. This review describes the present state of polymeric nanocarriers in enhancing antibiotic treatment, including improved pharmacokinetic properties and restored antibiotic efficacy against drug-resistant bacteria. Additionally, the current challenges and the future direction of this field are discussed. Full article
(This article belongs to the Special Issue Polymeric Nanoparticles in Drug Delivery)
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19 pages, 2410 KiB  
Review
Stimuli-Responsive Polymeric Nanosystems for Controlled Drug Delivery
by Zhichu Xiang, Mouquan Liu and Jun Song
Appl. Sci. 2021, 11(20), 9541; https://doi.org/10.3390/app11209541 - 14 Oct 2021
Cited by 6 | Viewed by 2128
Abstract
Biocompatible nanosystems based on polymeric materials are promising drug delivery nanocarrier candidates for antitumor therapy. However, the efficacy is unsatisfying due to nonspecific accumulation and drug release of the nanoparticles in normal tissue. Recently, the nanosystems that can be triggered by tumor-specific stimuli [...] Read more.
Biocompatible nanosystems based on polymeric materials are promising drug delivery nanocarrier candidates for antitumor therapy. However, the efficacy is unsatisfying due to nonspecific accumulation and drug release of the nanoparticles in normal tissue. Recently, the nanosystems that can be triggered by tumor-specific stimuli have drawn great interest for drug delivery applications due to their controllable drug release properties. In this review, various polymers and external stimuli that can be employed to develop stimuli-responsive polymeric nanosystems are discussed, and finally, we delineate the challenges in designing this kind of Nanomedicine to improve the therapeutic efficacy. Full article
(This article belongs to the Special Issue Polymeric Nanoparticles in Drug Delivery)
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23 pages, 4202 KiB  
Review
Polysorbate-Based Drug Formulations for Brain-Targeted Drug Delivery and Anticancer Therapy
by Vasanthan Ravichandran, Minjong Lee, Thuy Giang Nguyen Cao and Min Suk Shim
Appl. Sci. 2021, 11(19), 9336; https://doi.org/10.3390/app11199336 - 08 Oct 2021
Cited by 21 | Viewed by 6415
Abstract
Polysorbates (PSs) are synthetic nonionic surfactants consisting of polyethoxy sorbitan fatty acid esters. PSs have been widely employed as emulsifiers and stabilizers in various drug formulations and food additives. Recently, various PS-based formulations have been developed for safe and efficient drug delivery. This [...] Read more.
Polysorbates (PSs) are synthetic nonionic surfactants consisting of polyethoxy sorbitan fatty acid esters. PSs have been widely employed as emulsifiers and stabilizers in various drug formulations and food additives. Recently, various PS-based formulations have been developed for safe and efficient drug delivery. This review introduces the general features of PSs and PS-based drug carriers, summarizes recent progress in the development of PS-based drug formulations, and discusses the physicochemical properties, biological safety, P-glycoprotein inhibitory properties, and therapeutic applications of PS-based drug formulations. Additionally, recent advances in brain-targeted drug delivery using PS-based drug formulations have been highlighted. This review will help researchers understand the potential of PSs as effective drug formulation agents. Full article
(This article belongs to the Special Issue Polymeric Nanoparticles in Drug Delivery)
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