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Polymeric Nanoparticles for Biomedical Applications
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Polymeric Nanoparticles for Biomedical Applications

A special issue of Polymers (ISSN 2073-4360). This special issue belongs to the section "Polymer Applications".

Deadline for manuscript submissions: closed (25 November 2023) | Viewed by 58765

Printed Edition Available!
A printed edition of this Special Issue is available here.

Special Issue Editors

Dr. Stephanie Andrade

E-Mail Website
Guest Editor
1. ALiCE—Associate Laboratory in Chemical Engineering, Faculty of Engineering, University of Porto, Rua Dr. Roberto Frias, 4200-465 Porto, Portugal
2. LEPABE—Laboratory for Process Engineering, Environment, Biotechnology and Energy, Faculty of Engineering, University of Porto, Rua Dr. Roberto Frias, 4200-465 Porto, Portugal
Interests: nanotechnology; polymeric nanoparticles; lipid-based nanoparticles; drug delivery systems; targeted therapy; brain delivery; neurodegenerative disease therapy; effect of compounds on the aggregation and conformation of peptides and proteins; biophysical models; drug–membrane interactions; pharmaceutical and food applications
Special Issues, Collections and Topics in MDPI journals
Dr. Joana A. Loureiro

E-Mail Website1 Website2
Guest Editor
1. LEPABE—Laboratory for Process Engineering, Environment, Biotechnology and Energy, R. Dr. Roberto Frias, 4200-465 Porto, Portugal
2. ALiCE—Associate Laboratory in Chemical Engineering, Faculty of Engineering, University of Porto, Rua Dr. Roberto Frias, 4200-465 Porto, Portugal
Interests: nanotechnology and interfacial phenomena; effects of fluorinated systems and peptides on the aggregation of amyloid beta peptides; conformational studies of protein and peptide self-organized systems and polymer surfaces; design and production of inorganic and polymeric nanosystems for pharmaceutical and food applications
Special Issues, Collections and Topics in MDPI journals
Dr. Maria João Ramalho

E-Mail Website
Guest Editor
1. LEPABE—Laboratory for Process Engineering, Environment, Biotechnology and Energy, Faculty of Engineering, University of Porto, Rua Dr. Roberto Frias, 4200-465 Porto, Portugal
2. ALiCE—Associate Laboratory in Chemical Engineering, Faculty of Engineering, University of Porto, Rua Dr. Roberto Frias, 4200-465 Porto, Portugal
Interests: drug delivery; targeted therapy; brain delivery; brain cancer; glioblastoma; cancer therapy; neurodegenerative disease therapy; biophysical models; drug–membrane interactions
Special Issues, Collections and Topics in MDPI journals

Special Issue Information

Dear Colleagues,

Recently, the use of polymeric nanoparticles has attracted significant attention in biomedical applications. Due to their advantageous properties, including biodegradability, biocompatibility, and non-toxicity, natural and synthetic polymers are versatile materials that offer several advantages for the therapy and diagnosis of a huge range of diseases and health conditions. Encapsulating therapeutic agents in polymeric nanoparticles allows for a sustained drug release, which is beneficial to improve drug efficacy and safety, to reduce unwanted side effects, and to enhance the acceptance and compliance of patients. Polymeric nanoparticles are now established as an important part of the nanotechnology field.

This Special Issue focuses on the recent advances in polymeric nanoparticles and their current applications in healthcare, including the prevention, diagnosis, and treatment of diseases. Authors are welcome to submit their latest findings in the form of original papers and reviews.

Dr. Stéphanie Andrade
Dr. Joana A. Loureiro
Dr. Maria João Ramalho
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. Polymers 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 2700 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
  • polymer-based nanoparticles
  • drug delivery systems
  • surface functionalization
  • targeted delivery
  • nanocarriers
  • nanomedicine
  • biomedical application
  • therapeutic application
  • therapy
  • healthcare
  • early diagnosis
  • theranostics

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Published Papers (15 papers)

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Editorial

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4 pages, 200 KiB  
Editorial
Polymeric Nanoparticles for Biomedical Applications
by Stéphanie Andrade, Maria J. Ramalho and Joana A. Loureiro
Polymers 2024, 16(2), 249; https://doi.org/10.3390/polym16020249 - 15 Jan 2024
Cited by 1 | Viewed by 2610
Abstract
Polymeric nanoparticles (NPs), utilized extensively in biomedical applications, have received increasing interest in the preceding years and today represent an established part of the nanotechnology field [...] Full article
(This article belongs to the Special Issue Polymeric Nanoparticles for Biomedical Applications)

Research

Jump to: Editorial, Review

23 pages, 9637 KiB  
Article
New Physico-Chemical Analysis of Magnesium-Doped Hydroxyapatite in Dextran Matrix Nanocomposites
by Daniela Predoi, Steluta Carmen Ciobanu, Simona Liliana Iconaru, Ştefan Ţălu, Liliana Ghegoiu, Robert Saraiva Matos, Henrique Duarte da Fonseca Filho and Roxana Trusca
Polymers 2024, 16(1), 125; https://doi.org/10.3390/polym16010125 - 29 Dec 2023
Cited by 3 | Viewed by 1526
Abstract
The new magnesium-doped hydroxyapatite in dextran matrix (10MgHApD) nanocomposites were synthesized using coprecipitation technique. A spherical morphology was observed by scanning electron microscopy (SEM). The X-ray diffraction (XRD) characterization results show hydroxyapatite hexagonal phase formation. The element map scanning during the EDS analysis [...] Read more.
The new magnesium-doped hydroxyapatite in dextran matrix (10MgHApD) nanocomposites were synthesized using coprecipitation technique. A spherical morphology was observed by scanning electron microscopy (SEM). The X-ray diffraction (XRD) characterization results show hydroxyapatite hexagonal phase formation. The element map scanning during the EDS analysis revealed homogenous distribution of constituent elements of calcium, phosphor, oxygen and magnesium. The presence of dextran in the sample was revealed by Fourier transform infrared (FTIR) spectroscopy. The antimicrobial activity of the 10MgHAPD nanocomposites was assessed by in vitro assays using Staphylococcus aureus ATCC 25923, Pseudomonas aeruginosa ATCC 27853, Streptococcus mutans ATCC 25175, Porphyromonas gingivalis ATCC 33277 and Candida albicans ATCC 10231 microbial strains. The results of the antimicrobial assays highlighted that the 10MgHApD nanocomposites presented excellent antimicrobial activity against all the tested microorganisms and for all the tested time intervals. Furthermore, the biocompatibility assays determined that the 10MgHApD nanocomposites did not exhibit any toxicity towards Human gingival fibroblast (HGF-1) cells. Full article
(This article belongs to the Special Issue Polymeric Nanoparticles for Biomedical Applications)
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20 pages, 10549 KiB  
Article
Copolymer-Green-Synthesized Copper Oxide Nanoparticles Enhance Folate-Targeting in Cervical Cancer Cells In Vitro
by Keelan Jagaran and Moganavelli Singh
Polymers 2023, 15(10), 2393; https://doi.org/10.3390/polym15102393 - 20 May 2023
Cited by 11 | Viewed by 2592
Abstract
Cervical cancer is fast becoming a global health crisis, accounting for most female deaths in low- and middle-income countries. It is the fourth most frequent cancer affecting women, and due to its complexity, conventional treatment options are limited. Nanomedicine has found a niche [...] Read more.
Cervical cancer is fast becoming a global health crisis, accounting for most female deaths in low- and middle-income countries. It is the fourth most frequent cancer affecting women, and due to its complexity, conventional treatment options are limited. Nanomedicine has found a niche in gene therapy, with inorganic nanoparticles becoming attractive tools for gene delivery strategies. Of the many metallic nanoparticles (NPs) available, copper oxide NPs (CuONPs) have been the least investigated in gene delivery. In this study, CuONPs were biologically synthesized using Melia azedarach leaf extract, functionalized with chitosan and polyethylene glycol (PEG), and conjugated to the targeting ligand folate. A peak at 568 nm from UV-visible spectroscopy and the characteristic bands for the functional groups using Fourier-transform infrared (FTIR) spectroscopy confirmed the successful synthesis and modification of the CuONPs. Spherical NPs within the nanometer range were evident from transmission electron microscopy (TEM) and nanoparticle tracking analysis (NTA). The NPs portrayed exceptional binding and protection of the reporter gene, pCMV-Luc-DNA. In vitro cytotoxicity studies revealed cell viability >70% in human embryonic kidney (HEK293), breast adenocarcinoma (MCF-7), and cervical cancer (HeLa) cells, with significant transgene expression, obtained using the luciferase reporter gene assay. Overall, these NPs showed favorable properties and efficient gene delivery, suggesting their potential role in gene therapy. Full article
(This article belongs to the Special Issue Polymeric Nanoparticles for Biomedical Applications)
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12 pages, 3016 KiB  
Article
Development of Crosslinker-Free Polysaccharide-Lysozyme Microspheres for Treatment Enteric Infection
by Shuo Li, Li Shi, Ting Ye, Biao Huang, Yuan Qin, Yongkang Xie, Xiaoyuan Ren and Xueqin Zhao
Polymers 2023, 15(5), 1077; https://doi.org/10.3390/polym15051077 - 21 Feb 2023
Cited by 2 | Viewed by 1636
Abstract
Antibiotic abuse in the conventional treatment of microbial infections, such as inflammatory bowel disease, induces cumulative toxicity and antimicrobial resistance which requires the development of new antibiotics or novel strategies for infection control. Crosslinker-free polysaccharide-lysozyme microspheres were constructed via an electrostatic layer-by-layer self-assembly [...] Read more.
Antibiotic abuse in the conventional treatment of microbial infections, such as inflammatory bowel disease, induces cumulative toxicity and antimicrobial resistance which requires the development of new antibiotics or novel strategies for infection control. Crosslinker-free polysaccharide-lysozyme microspheres were constructed via an electrostatic layer-by-layer self-assembly technique by adjusting the assembly behaviors of carboxymethyl starch (CMS) on lysozyme and subsequently outer cationic chitosan (CS) deposition. The relative enzymatic activity and in vitro release profile of lysozyme under simulated gastric and intestinal fluids were investigated. The highest loading efficiency of the optimized CS/CMS-lysozyme micro-gels reached 84.9% by tailoring CMS/CS content. The mild particle preparation procedure retained relative activity of 107.4% compared with free lysozyme, and successfully enhanced the antibacterial activity against E. coli due to the superposition effect of CS and lysozyme. Additionally, the particle system showed no toxicity to human cells. In vitro digestibility testified that almost 70% was recorded in the simulated intestinal fluid within 6 h. Results demonstrated that the cross-linker-free CS/CMS-lysozyme microspheres could be a promising antibacterial additive for enteric infection treatment due to its highest effective dose (573.08 μg/mL) and fast release at the intestinal tract. Full article
(This article belongs to the Special Issue Polymeric Nanoparticles for Biomedical Applications)
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18 pages, 2134 KiB  
Article
Polyester Nanocapsules for Intravenous Delivery of Artemether: Formulation Development, Antimalarial Efficacy, and Cardioprotective Effects In Vivo
by Alessandra Teixeira Vidal-Diniz, Homero Nogueira Guimarães, Giani Martins Garcia, Érika Martins Braga, Sylvain Richard, Andrea Grabe-Guimarães and Vanessa Carla Furtado Mosqueira
Polymers 2022, 14(24), 5503; https://doi.org/10.3390/polym14245503 - 15 Dec 2022
Cited by 5 | Viewed by 1698
Abstract
Artemether (ATM) is an effective antimalarial drug that also has a short half-life in the blood. Furthermore, ATM is also cardiotoxic and is associated with pro-arrhythmogenic risks. We aimed to develop a delivery system enabling the prolonged release of ATM into the blood [...] Read more.
Artemether (ATM) is an effective antimalarial drug that also has a short half-life in the blood. Furthermore, ATM is also cardiotoxic and is associated with pro-arrhythmogenic risks. We aimed to develop a delivery system enabling the prolonged release of ATM into the blood coupled with reduced cardiotoxicity. To achieve this, we prepared polymeric nanocapsules (NCs) from different biodegradable polyesters, namely poly(D,L-lactide) (PLA), poly-ε-caprolactone (PCL), and surface-modified NCs, using a monomethoxi-polyethylene glycol-block-poly(D,L-lactide) (PEG5kDa-PLA45kDa) polymer. Using this approach, we were able to encapsulate high yields of ATM (>85%, 0–4 mg/mL) within the oily core of the NCs. The PCL-NCs exhibited the highest percentage of ATM loading as well as a slow release rate. Atomic force microscopy showed nanometric and spherical particles with a narrow size dispersion. We used the PCL NCs loaded with ATM for biological evaluation following IV administration. As with free-ATM, the ATM-PCL-NCs formulation exhibited potent antimalarial efficacy using either the “Four-day test” protocol (ATM total at the end of the 4 daily doses: 40 and 80 mg/kg) in Swiss mice infected with P. berghei or a single low dose (20 mg/kg) of ATM in mice with higher parasitemia (15%). In healthy rats, IV administration of single doses of free-ATM (40 or 80 mg/kg) prolonged cardiac QT and QTc intervals and induced both bradycardia and hypotension. Repeated IV administration of free-ATM (four IV doses at 20 mg/kg every 12 h for 48 h) also prolonged the QT and QTc intervals but, paradoxically, induced tachycardia and hypertension. Remarkably, the incorporation of ATM in ATM-PCL-NCs reduced all adverse effects. In conclusion, the encapsulation of ATM in biodegradable polyester NCs reduces its cardiovascular toxicity without affecting its antimalarial efficacy. Full article
(This article belongs to the Special Issue Polymeric Nanoparticles for Biomedical Applications)
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19 pages, 5200 KiB  
Article
Apigenin Loaded Lipoid–PLGA–TPGS Nanoparticles for Colon Cancer Therapy: Characterization, Sustained Release, Cytotoxicity, and Apoptosis Pathways
by Mohamed A. Alfaleh, Anwar M. Hashem, Turki S. Abujamel, Nabil A. Alhakamy, Mohd Abul Kalam, Yassine Riadi and Shadab Md
Polymers 2022, 14(17), 3577; https://doi.org/10.3390/polym14173577 - 30 Aug 2022
Cited by 13 | Viewed by 2208
Abstract
Colon cancer (CC) is one of major causes of mortality and affects the socio-economic status world-wide. Therefore, developing a novel and efficient delivery system is needed for CC management. Thus, in the present study, lipid polymer hybrid nanoparticles of apigenin (LPHyNPs) was prepared [...] Read more.
Colon cancer (CC) is one of major causes of mortality and affects the socio-economic status world-wide. Therefore, developing a novel and efficient delivery system is needed for CC management. Thus, in the present study, lipid polymer hybrid nanoparticles of apigenin (LPHyNPs) was prepared and characterized on various parameters such as particle size (234.80 ± 12.28 nm), PDI (0.11 ± 0.04), zeta potential (−5.15 ± 0.70 mV), EE (55.18 ± 3.61%), etc. Additionally, the DSC, XRD, and FT-IR analysis determined drug entrapment and affinity with the selected excipient, demonstrating a promising drug affinity with the lipid polymer. Morphological analysis via SEM and TEM exhibited spherical NPs with a dark color core, which indicated drug entrapment inside the core. In vitro release study showed significant (p < 0.05) sustained release of AGN from LPHyNPs than AGN suspension. Further, the therapeutic efficacy in terms of apoptosis and cell cycle arrest of developed LPHyNPs against CC was estimated by performing flow cytometry and comparing its effectiveness with blank LPHyNPs and AGN suspension, which exhibited remarkable outcomes in favor of LPHyNPs. Moreover, the mechanism behind the anticancer attribute was further explored by estimating gene expression of various signaling molecules such as Bcl-2, BAX, NF-κB, and mTOR that were involved in carcinogenic pathways, which indicated significant (p < 0.05) results for LPHyNPs. Moreover, to strengthen the anticancer potential of LPHyNPs against chemoresistance, the expression of JNK and MDR-1 genes was estimated. Outcomes showed that their expression level reduced appreciably when compared to blank LPHyNPs and AGN suspension. Hence, it can be concluded that developed LPHyNPs could be an efficient therapeutic system for managing CC. Full article
(This article belongs to the Special Issue Polymeric Nanoparticles for Biomedical Applications)
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15 pages, 3773 KiB  
Article
Boosting the Anticancer Activity of Sunitinib Malate in Breast Cancer through Lipid Polymer Hybrid Nanoparticles Approach
by Mohammed Muqtader Ahmed, Md. Khalid Anwer, Farhat Fatima, Mohammed F. Aldawsari, Ahmed Alalaiwe, Amer S. Alali, Abdulrahman I. Alharthi and Mohd Abul Kalam
Polymers 2022, 14(12), 2459; https://doi.org/10.3390/polym14122459 - 16 Jun 2022
Cited by 26 | Viewed by 2962
Abstract
In the current study, lipid-polymer hybrid nanoparticles (LPHNPs) fabricated with lipoid-90H and chitosan, sunitinib malate (SM), an anticancer drug was loaded using lecithin as a stabilizer by employing emulsion solvent evaporation technique. Four formulations (SLPN1–SLPN4) were developed by varying the concentration of chitosan [...] Read more.
In the current study, lipid-polymer hybrid nanoparticles (LPHNPs) fabricated with lipoid-90H and chitosan, sunitinib malate (SM), an anticancer drug was loaded using lecithin as a stabilizer by employing emulsion solvent evaporation technique. Four formulations (SLPN1–SLPN4) were developed by varying the concentration of chitosan polymer. Based on particle characterization, SLPN4 was optimized with size (439 ± 5.8 nm), PDI (0.269), ZP (+34 ± 5.3 mV), and EE (83.03 ± 4.9%). Further, the optimized formulation was characterized by FTIR, DSC, XRD, SEM, and in vitro release studies. In-vitro release of the drug from SPN4 was found to be 84.11 ± 2.54% as compared with pure drug SM 24.13 ± 2.67%; in 48 h, release kinetics followed the Korsmeyer–Peppas model with Fickian release mechanism. The SLPN4 exhibited a potent cytotoxicity against MCF-7 breast cancer, as evident by caspase 3, 9, and p53 activities. According to the findings, SM-loaded LPHNPs might be a promising therapy option for breast cancer. Full article
(This article belongs to the Special Issue Polymeric Nanoparticles for Biomedical Applications)
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Review

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44 pages, 3546 KiB  
Review
Recent Advances in Micro- and Nano-Drug Delivery Systems Based on Natural and Synthetic Biomaterials
by Md. Harun-Or-Rashid, Most. Nazmin Aktar, Md. Sabbir Hossain, Nadia Sarkar, Md. Rezaul Islam, Md. Easin Arafat, Shukanta Bhowmik and Shin-ichi Yusa
Polymers 2023, 15(23), 4563; https://doi.org/10.3390/polym15234563 - 28 Nov 2023
Cited by 12 | Viewed by 5215
Abstract
Polymeric drug delivery technology, which allows for medicinal ingredients to enter a cell more easily, has advanced considerably in recent decades. Innovative medication delivery strategies use biodegradable and bio-reducible polymers, and progress in the field has been accelerated by future possible research applications. [...] Read more.
Polymeric drug delivery technology, which allows for medicinal ingredients to enter a cell more easily, has advanced considerably in recent decades. Innovative medication delivery strategies use biodegradable and bio-reducible polymers, and progress in the field has been accelerated by future possible research applications. Natural polymers utilized in polymeric drug delivery systems include arginine, chitosan, dextrin, polysaccharides, poly(glycolic acid), poly(lactic acid), and hyaluronic acid. Additionally, poly(2-hydroxyethyl methacrylate), poly(N-isopropyl acrylamide), poly(ethylenimine), dendritic polymers, biodegradable polymers, and bioabsorbable polymers as well as biomimetic and bio-related polymeric systems and drug-free macromolecular therapies have been employed in polymeric drug delivery. Different synthetic and natural biomaterials are in the clinical phase to mitigate different diseases. Drug delivery methods using natural and synthetic polymers are becoming increasingly common in the pharmaceutical industry, with biocompatible and bio-related copolymers and dendrimers having helped cure cancer as drug delivery systems. This review discusses all the above components and how, by combining synthetic and biological approaches, micro- and nano-drug delivery systems can result in revolutionary polymeric drug and gene delivery devices. Full article
(This article belongs to the Special Issue Polymeric Nanoparticles for Biomedical Applications)
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38 pages, 1511 KiB  
Review
Biofunctionalization and Applications of Polymeric Nanofibers in Tissue Engineering and Regenerative Medicine
by Prasanna Phutane, Darshan Telange, Surendra Agrawal, Mahendra Gunde, Kunal Kotkar and Anil Pethe
Polymers 2023, 15(5), 1202; https://doi.org/10.3390/polym15051202 - 27 Feb 2023
Cited by 31 | Viewed by 3767
Abstract
The limited ability of most human tissues to regenerate has necessitated the interventions namely autograft and allograft, both of which carry the limitations of its own. An alternative to such interventions could be the capability to regenerate the tissue in vivo.Regeneration of tissue [...] Read more.
The limited ability of most human tissues to regenerate has necessitated the interventions namely autograft and allograft, both of which carry the limitations of its own. An alternative to such interventions could be the capability to regenerate the tissue in vivo.Regeneration of tissue using the innate capacity of the cells to regenerate is studied under the discipline of tissue engineering and regenerative medicine (TERM). Besides the cells and growth-controlling bioactives, scaffolds play the central role in TERM which is analogous to the role performed by extracellular matrix (ECM) in the vivo. Mimicking the structure of ECM at the nanoscale is one of the critical attributes demonstrated by nanofibers. This unique feature and its customizable structure to befit different types of tissues make nanofibers a competent candidate for tissue engineering. This review discusses broad range of natural and synthetic biodegradable polymers employed to construct nanofibers as well as biofunctionalization of polymers to improve cellular interaction and tissue integration. Amongst the diverse ways to fabricate nanofibers, electrospinning has been discussed in detail along with advances in this technique. Review also presents a discourse on application of nanofibers for a range of tissues, namely neural, vascular, cartilage, bone, dermal and cardiac. Full article
(This article belongs to the Special Issue Polymeric Nanoparticles for Biomedical Applications)
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19 pages, 2158 KiB  
Review
Nanoparticles for Biomedical Application and Their Synthesis
by Iva Rezić
Polymers 2022, 14(22), 4961; https://doi.org/10.3390/polym14224961 - 16 Nov 2022
Cited by 29 | Viewed by 4176
Abstract
Tremendous developments in nanotechnology have revolutionized the impact of nanoparticles (NPs) in the scientific community and, more recently, in society. Nanomaterials are by their definition materials that have at least one dimension in range of 1 to 100 nm. Nanoparticles are found in [...] Read more.
Tremendous developments in nanotechnology have revolutionized the impact of nanoparticles (NPs) in the scientific community and, more recently, in society. Nanomaterials are by their definition materials that have at least one dimension in range of 1 to 100 nm. Nanoparticles are found in many types of different technological and scientific applications and innovations, from delicate electronics to state-of-the-art medical treatments. Medicine has recognized the importance of polymer materials coated with NPs and utilizes them widely thanks to their excellent physical, chemical, antibacterial, antimicrobial, and protective properties. Emphasis is given to their biomedical application, as the nanoscale structures are in the range of many biological molecules. Through this, they can achieve many important features such as targeted drug delivery, imaging, photo thermal therapy, and sensors. Moreover, by manipulating in a “nano-scale” range, their characteristic can be modified in order to obtain the desired properties needed in particular biomedical fields, such as electronic, optical, surface plasmon resonance, and physic-chemical features. Full article
(This article belongs to the Special Issue Polymeric Nanoparticles for Biomedical Applications)
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26 pages, 1733 KiB  
Review
Polymeric Nanoparticles in Brain Cancer Therapy: A Review of Current Approaches
by Chad A. Caraway, Hallie Gaitsch, Elizabeth E. Wicks, Anita Kalluri, Navya Kunadi and Betty M. Tyler
Polymers 2022, 14(14), 2963; https://doi.org/10.3390/polym14142963 - 21 Jul 2022
Cited by 42 | Viewed by 4965
Abstract
Translation of novel therapies for brain cancer into clinical practice is of the utmost importance as primary brain tumors are responsible for more than 200,000 deaths worldwide each year. While many research efforts have been aimed at improving survival rates over the years, [...] Read more.
Translation of novel therapies for brain cancer into clinical practice is of the utmost importance as primary brain tumors are responsible for more than 200,000 deaths worldwide each year. While many research efforts have been aimed at improving survival rates over the years, prognosis for patients with glioblastoma and other primary brain tumors remains poor. Safely delivering chemotherapeutic drugs and other anti-cancer compounds across the blood–brain barrier and directly to tumor cells is perhaps the greatest challenge in treating brain cancer. Polymeric nanoparticles (NPs) are powerful, highly tunable carrier systems that may be able to overcome those obstacles. Several studies have shown appropriately-constructed polymeric NPs cross the blood–brain barrier, increase drug bioavailability, reduce systemic toxicity, and selectively target central nervous system cancer cells. While no studies relating to their use in treating brain cancer are in clinical trials, there is mounting preclinical evidence that polymeric NPs could be beneficial for brain tumor therapy. This review includes a variety of polymeric NPs and how their associated composition, surface modifications, and method of delivery impact their capacity to improve brain tumor therapy. Full article
(This article belongs to the Special Issue Polymeric Nanoparticles for Biomedical Applications)
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31 pages, 3809 KiB  
Review
Approaches to Improve Macromolecule and Nanoparticle Accumulation in the Tumor Microenvironment by the Enhanced Permeability and Retention Effect
by Victor Ejigah, Oluwanifemi Owoseni, Perpetue Bataille-Backer, Omotola D. Ogundipe, Funmilola A. Fisusi and Simeon K. Adesina
Polymers 2022, 14(13), 2601; https://doi.org/10.3390/polym14132601 - 27 Jun 2022
Cited by 73 | Viewed by 4957
Abstract
Passive targeting is the foremost mechanism by which nanocarriers and drug-bearing macromolecules deliver their payload selectively to solid tumors. An important driver of passive targeting is the enhanced permeability and retention (EPR) effect, which is the cornerstone of most carrier-based tumor-targeted drug delivery [...] Read more.
Passive targeting is the foremost mechanism by which nanocarriers and drug-bearing macromolecules deliver their payload selectively to solid tumors. An important driver of passive targeting is the enhanced permeability and retention (EPR) effect, which is the cornerstone of most carrier-based tumor-targeted drug delivery efforts. Despite the huge number of publications showcasing successes in preclinical animal models, translation to the clinic has been poor, with only a few nano-based drugs currently being used for the treatment of cancers. Several barriers and factors have been adduced for the low delivery efficiency to solid tumors and poor clinical translation, including the characteristics of the nanocarriers and macromolecules, vascular and physiological barriers, the heterogeneity of tumor blood supply which affects the homogenous distribution of nanocarriers within tumors, and the transport and penetration depth of macromolecules and nanoparticles in the tumor matrix. To address the challenges associated with poor tumor targeting and therapeutic efficacy in humans, the identified barriers that affect the efficiency of the enhanced permeability and retention (EPR) effect for macromolecular therapeutics and nanoparticle delivery systems need to be overcome. In this review, approaches to facilitate improved EPR delivery outcomes and the clinical translation of novel macromolecular therapeutics and nanoparticle drug delivery systems are discussed. Full article
(This article belongs to the Special Issue Polymeric Nanoparticles for Biomedical Applications)
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28 pages, 1504 KiB  
Review
Polymeric Nanoparticles-Loaded Hydrogels for Biomedical Applications: A Systematic Review on In Vivo Findings
by Débora Nunes, Stéphanie Andrade, Maria João Ramalho, Joana A. Loureiro and Maria Carmo Pereira
Polymers 2022, 14(5), 1010; https://doi.org/10.3390/polym14051010 - 2 Mar 2022
Cited by 58 | Viewed by 6761
Abstract
Clinically available medications face several hurdles that limit their therapeutic activity, including restricted access to the target tissues due to biological barriers, low bioavailability, and poor pharmacokinetic properties. Drug delivery systems (DDS), such as nanoparticles (NPs) and hydrogels, have been widely employed to [...] Read more.
Clinically available medications face several hurdles that limit their therapeutic activity, including restricted access to the target tissues due to biological barriers, low bioavailability, and poor pharmacokinetic properties. Drug delivery systems (DDS), such as nanoparticles (NPs) and hydrogels, have been widely employed to address these issues. Furthermore, the DDS improves drugs’ therapeutic efficacy while reducing undesired side effects caused by the unspecific distribution over the different tissues. The integration of NPs into hydrogels has emerged to improve their performance when compared with each DDS individually. The combination of both DDS enhances the ability to deliver drugs in a localized and targeted manner, paired with a controlled and sustained drug release, resulting in increased drug therapeutic effectiveness. With the incorporation of the NPs into hydrogels, it is possible to apply the DDS locally and then provide a sustained release of the NPs in the site of action, allowing the drug uptake in the required location. Additionally, most of the materials used to produce the hydrogels and NPs present low toxicity. This article provides a systematic review of the polymeric NPs-loaded hydrogels developed for various biomedical applications, focusing on studies that present in vivo data. Full article
(This article belongs to the Special Issue Polymeric Nanoparticles for Biomedical Applications)
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Graphical abstract

25 pages, 2109 KiB  
Review
Polysaccharide-Drug Conjugates: A Tool for Enhanced Cancer Therapy
by Neena Yadav, Arul Prakash Francis, Veeraraghavan Vishnu Priya, Shankargouda Patil, Shazia Mustaq, Sameer Saeed Khan, Khalid J. Alzahrani, Hamsa Jameel Banjer, Surapaneni Krishna Mohan, Ullas Mony and Rukkumani Rajagopalan
Polymers 2022, 14(5), 950; https://doi.org/10.3390/polym14050950 - 27 Feb 2022
Cited by 32 | Viewed by 5559
Abstract
Cancer is one of the most widespread deadly diseases, following cardiovascular disease, worldwide. Chemotherapy is widely used in combination with surgery, hormone and radiation therapy to treat various cancers. However, chemotherapeutic drugs can cause severe side effects due to non-specific targeting, poor bioavailability, [...] Read more.
Cancer is one of the most widespread deadly diseases, following cardiovascular disease, worldwide. Chemotherapy is widely used in combination with surgery, hormone and radiation therapy to treat various cancers. However, chemotherapeutic drugs can cause severe side effects due to non-specific targeting, poor bioavailability, low therapeutic indices, and high dose requirements. Several drug carriers successfully overcome these issues and deliver drugs to the desired sites, reducing the side effects. Among various drug delivery systems, polysaccharide-based carriers that target only the cancer cells have been developed to overcome the toxicity of chemotherapeutics. Polysaccharides are non-toxic, biodegradable, hydrophilic biopolymers that can be easily modified chemically to improve the bioavailability and stability for delivering therapeutics into cancer tissues. Different polysaccharides, such as chitosan, alginates, cyclodextrin, pullulan, hyaluronic acid, dextran, guar gum, pectin, and cellulose, have been used in anti-cancer drug delivery systems. This review highlights the recent progress made in polysaccharides-based drug carriers in anti-cancer therapy. Full article
(This article belongs to the Special Issue Polymeric Nanoparticles for Biomedical Applications)
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21 pages, 2448 KiB  
Review
Angiopep-2-Modified Nanoparticles for Brain-Directed Delivery of Therapeutics: A Review
by Saffiya Habib and Moganavelli Singh
Polymers 2022, 14(4), 712; https://doi.org/10.3390/polym14040712 - 12 Feb 2022
Cited by 46 | Viewed by 5456
Abstract
Nanotechnology has opened up a world of possibilities for the treatment of brain disorders. Nanosystems can be designed to encapsulate, carry, and deliver a variety of therapeutic agents, including drugs and nucleic acids. Nanoparticles may also be formulated to contain photosensitizers or, on [...] Read more.
Nanotechnology has opened up a world of possibilities for the treatment of brain disorders. Nanosystems can be designed to encapsulate, carry, and deliver a variety of therapeutic agents, including drugs and nucleic acids. Nanoparticles may also be formulated to contain photosensitizers or, on their own, serve as photothermal conversion agents for phototherapy. Furthermore, nano-delivery agents can enhance the efficacy of contrast agents for improved brain imaging and diagnostics. However, effective nano-delivery to the brain is seriously hampered by the formidable blood–brain barrier (BBB). Advances in understanding natural transport routes across the BBB have led to receptor-mediated transcytosis being exploited as a possible means of nanoparticle uptake. In this regard, the oligopeptide Angiopep-2, which has high BBB transcytosis capacity, has been utilized as a targeting ligand. Various organic and inorganic nanostructures have been functionalized with Angiopep-2 to direct therapeutic and diagnostic agents to the brain. Not only have these shown great promise in the treatment and diagnosis of brain cancer but they have also been investigated for the treatment of brain injury, stroke, epilepsy, Parkinson’s disease, and Alzheimer’s disease. This review focuses on studies conducted from 2010 to 2021 with Angiopep-2-modified nanoparticles aimed at the treatment and diagnosis of brain disorders. Full article
(This article belongs to the Special Issue Polymeric Nanoparticles for Biomedical Applications)
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