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Pharmaceutics
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Advanced Nanomaterials for Drug Delivery
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Advanced Nanomaterials for 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 April 2024 | Viewed by 20542

Special Issue Editors

Dr. Roxana Cristina Popescu

E-Mail Website
Guest Editor
“Horia Hulubei” National Insitute of Physics and Nuclear Engineering (IFIN-HH), 30 Reactorului Street, 077125 Magurele, Romania
Interests: nanobiomaterials; drug delivery; cancer therapy; radiobiology; biocompatibility
Special Issues, Collections and Topics in MDPI journals
Dr. Diana Savu

E-Mail Website
Guest Editor
Department of Life and Environmental Physics, Horia Hulubei National Institute of Physics and Nuclear Engineering, 077125 Magurele, Romania
Interests: radioresistant cancer cell biology; tumor cell radiosensitization; DNA damage signaling; mitochondria–nucleus communication; radiation-induced bystander effects; radiation response biomarkers; tumor microenvironment
Special Issues, Collections and Topics in MDPI journals

Special Issue Information

Dear Colleagues,

We are pleased to invite you to contribute to a Special Issue of Nanomaterials entitled “Nanomaterials for Drug Delivery”. It is known that nanoparticle-based systems for therapeutic applications have the ability to pass biological barriers and to target the affected tissues. In the case of drug delivery systems based on nanoparticles, they can enter and accumulate in the targeted cells and reach the drug therapeutic target, while reducing its systemic toxicity. Moreover, the release of the drug can be controlled and triggered by environmental factors such as pH, light, enzymes, etc. 

The Special Issue aims to cover recent advancements in nanoparticle design and obtaining for drug delivery applications, characterization, and evaluation, as well as in vitro, in vivo, clinical, or in silico testing. Applications such as cancer therapy, antimicrobial, antiviral, wound healing, or tissue regeneration can be addressed. 

We look forward to receiving your contributions.

Dr. Roxana Cristina Popescu
Dr. Diana Savu
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

  • nanomaterials
  • drug delivery systems
  • cancer therapy
  • antimicrobial applications
  • antiviral applications

Published Papers (7 papers)

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Research

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21 pages, 4277 KiB  
Article
Influence of Surface-Modification via PEGylation or Chitosanization of Lipidic Nanocarriers on In Vivo Pharmacokinetic/Pharmacodynamic Profiles of Apixaban
by Mohamed F. Zaky, Taha M. Hammady, Shadeed Gad, Abdullah Alattar, Reem Alshaman, Ann Hegazy, Sawsan A. Zaitone, Mamdouh Mostafa Ghorab and Mohamed A. Megahed
Pharmaceutics 2023, 15(6), 1668; https://doi.org/10.3390/pharmaceutics15061668 - 07 Jun 2023
Cited by 1 | Viewed by 1265
Abstract
Nanostructured lipid carriers (NLCs) have been proven to significantly improve the bioavailability and efficacy of many drugs; however, they still have many limitations. These limitations could hinder their potential for enhancing the bioavailability of poorly water-soluble drugs and, therefore, require further amendments. From [...] Read more.
Nanostructured lipid carriers (NLCs) have been proven to significantly improve the bioavailability and efficacy of many drugs; however, they still have many limitations. These limitations could hinder their potential for enhancing the bioavailability of poorly water-soluble drugs and, therefore, require further amendments. From this perspective, we have investigated how the chitosanization and PEGylation of NLCs affected their ability to function as a delivery system for apixaban (APX). These surface modifications could enhance the ability of NLCs to improve the bioavailability and pharmacodynamic activity of the loaded drug. In vitro and in vivo studies were carried out to examine APX-loaded NLCs, chitosan-modified NLCs, and PEGylated NLCs. The three nanoarchitectures displayed a Higuchi-diffusion release pattern in vitro, in addition to having their vesicular outline proven via electron microscopy. PEGylated and chitosanized NLCs retained good stability over 3 months, versus the nonPEGylated and nonchitosanized NLCs. Interestingly, APX-loaded chitosan-modified NLCs displayed better stability than the APX-loaded PEGylated NLCs, in terms of mean vesicle size after 90 days. On the other hand, the absorption profile of APX (AUC0-inf) in rats pretreated with APX-loaded PEGylated NLCs (108.59 µg·mL−1·h−1) was significantly higher than the AUC0-inf of APX in rats pretreated with APX-loaded chitosan-modified NLCs (93.397 µg·mL−1·h−1), and both were also significantly higher than AUC0-inf of APX-Loaded NLCs (55.435 µg·mL−1·h−1). Chitosan-coated NLCs enhanced APX anticoagulant activity with increased prothrombin time and activated partial thromboplastin time by 1.6- and 1.55-folds, respectively, compared to unmodified NLCs, and by 1.23- and 1.37-folds, respectively, compared to PEGylated NLCs. The PEGylation and chitosanization of NLCs enhanced the bioavailability and anticoagulant activity of APX over the nonmodified NLCs; this highlighted the importance of both approaches. Full article
(This article belongs to the Special Issue Advanced Nanomaterials for Drug Delivery)
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15 pages, 3525 KiB  
Article
A Macrophage Membrane–Polymer Hybrid Biomimetic Nanoplatform for Therapeutic Delivery of Somatostatin Peptide to Chronic Pancreatitis
by Fang Wang, Yu Deng, Luying Yu, Ao Zhou, Jieting Wang, Jingyan Jia, Ning Li, Fadian Ding, Wei Lian, Qicai Liu, Yu Yang and Xinhua Lin
Pharmaceutics 2022, 14(11), 2341; https://doi.org/10.3390/pharmaceutics14112341 - 30 Oct 2022
Cited by 1 | Viewed by 1683
Abstract
The clinical translation of therapeutic peptides is generally challenged by multiple issues involving absorption, distribution, metabolism and excretion. In this study, a macrophage membrane-coated poly(lactic-co-glycolic acid) (PLGA) nanodelivery system was developed to enhance the bioavailability of the somatostatin (SST) peptide, which faces the [...] Read more.
The clinical translation of therapeutic peptides is generally challenged by multiple issues involving absorption, distribution, metabolism and excretion. In this study, a macrophage membrane-coated poly(lactic-co-glycolic acid) (PLGA) nanodelivery system was developed to enhance the bioavailability of the somatostatin (SST) peptide, which faces the hurdles of short half-life and potential side effects in the treatment of chronic pancreatitis. Using a facile nanoprecipitation strategy, SST was loaded in the nanoparticles with an encapsulation efficiency (EE) and a loading efficiency (LE) of 73.68 ± 3.56% and 1.47 ± 0.07%, respectively. The final formulation of SST-loaded nanoparticles with the camouflage of macrophage membrane (MP-SST) showed a mean diameter of 151 ± 4 nm and an average zeta potential of −29.6 ± 0.3 mV, which were stable long term during storage. With an above 90% cell viability, a hemolysis level of about 2% (<5%) and a preference for being ingested by activated endothelial cells compared to macrophages, the membrane–polymer hybrid nanoparticle showed biocompatibility and targeting capability in vitro. After being intravenously administered to mice with chronic pancreatitis, the MP-SST increased the content of SST in the serum (123.6 ± 13.6 pg/mL) and pancreas (1144.9 ± 206.2 pg/g) compared to the treatment of (Dulbecco’s phosphate-buffered saline) DPBS (61.7 ± 6.0 pg/mL in serum and 740.2 ± 172.4 pg/g in the pancreas). The recovery of SST by MP-SST downregulated the expressions of chronic pancreatitis-related factors and alleviated the histologic severity of the pancreas to the greatest extent compared to other treatment groups. This augmentation of SST therapeutic effects demonstrated the superiority of integrating the synthetic polymer with biological membranes in the design of nanoplatforms for advanced and smart peptide delivery. Other peptides like SST can also be delivered via the membrane–polymer hybrid nanosystem for the treatment of diseases, broadening and promoting the potential clinical applications of peptides as therapeutics. Full article
(This article belongs to the Special Issue Advanced Nanomaterials for Drug Delivery)
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12 pages, 7676 KiB  
Article
Influence of Polymer Shell Molecular Weight on Functionalized Iron Oxide Nanoparticles Morphology and In Vivo Biodistribution
by Roxana Cristina Popescu, Bogdan Ştefan Vasile, Diana Iulia Savu, George Dan Mogoşanu, Ludovic Everard Bejenaru, Ecaterina Andronescu, Alexandru Mihai Grumezescu and Laurenţiu Mogoantă
Pharmaceutics 2022, 14(9), 1877; https://doi.org/10.3390/pharmaceutics14091877 - 05 Sep 2022
Cited by 3 | Viewed by 1489
Abstract
Iron oxide nanoparticles (IONPs) have been extensively used in different biomedical applications due to their biocompatibility and magnetic properties. However, different functionalization approaches have been developed to improve their time-life in the systemic circulation. Here, we have synthesized IONPs using a modified Massart [...] Read more.
Iron oxide nanoparticles (IONPs) have been extensively used in different biomedical applications due to their biocompatibility and magnetic properties. However, different functionalization approaches have been developed to improve their time-life in the systemic circulation. Here, we have synthesized IONPs using a modified Massart method and functionalized them in situ with polyethylene glycol with different molecular weights (20 K and 35 K). The resulting nanoparticles were characterized in terms of morphology, structure, and composition using transmission electron microscopy (TEM) and selected area electron diffraction (SAED). In vivo biodistribution was evaluated in Balb/c mice, the presence of IONP being evidenced through histopathological investigations. IONP morphological characterization showed a change in shape (from spherical to rhombic) and size with molecular weight, while structural characterization proved the obtaining of highly crystalline samples of spinel structured cubic face-centered magnetite. In vivo biodistribution in a mice model proved the biocompatibility of all of the IONP samples. All NPs were cleared through the liver, spleen, and lungs, while bare IONPs were also evidenced in kidneys. Full article
(This article belongs to the Special Issue Advanced Nanomaterials for Drug Delivery)
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15 pages, 2480 KiB  
Article
Optimization of a Cefuroxime Axetil-Loaded Liquid Self-Nanoemulsifying Drug Delivery System: Enhanced Solubility, Dissolution and Caco-2 Cell Uptake
by Arshad Ali Khan, Akhtar Atiya, Safia Akhtar, Yogesh Yadav, Kamal A. Qureshi, Mariusz Jaremko and Syed Mahmood
Pharmaceutics 2022, 14(4), 772; https://doi.org/10.3390/pharmaceutics14040772 - 01 Apr 2022
Cited by 4 | Viewed by 2236
Abstract
Cefuroxime axetil (CA) is an oral cephalosporin which hydrolyzes rapidly to the active parent compound cefuroxime. CA is known to have incomplete oral bioavailability (30–50%) due to its poor solubility and enzymatic conversion to cefuroxime in the gut lumen. In order to overcome [...] Read more.
Cefuroxime axetil (CA) is an oral cephalosporin which hydrolyzes rapidly to the active parent compound cefuroxime. CA is known to have incomplete oral bioavailability (30–50%) due to its poor solubility and enzymatic conversion to cefuroxime in the gut lumen. In order to overcome these drawbacks, a lipid-based self-nanoemulsifying drug delivery system (SNEDDS) has been developed and optimized. The SNEDDS formulations were prepared using the aqueous phase titration method. The greatest self-emulsifying area was found in the 2:1 Smix ratio. As a result, different SNEDDS formulations were carefully selected from this phase diagram based on their smaller droplet size < 100 nm, polydispersity index ≤ 0.5, dispersibility (Grade A), and transmittance (%) > 85%. Thermodynamic stability tests were carried out in order to rule out any metastable/unstable SNEDDS formulations. The droplet size, polydispersity index, zeta potential, and entrapment efficiency (% EE) of optimized CA-loaded SNEDDS (C-3) were 18.50 ± 1.83 nm, 0.064 ± 0.008, −22.12 ± 1.20 mV, and 97.62 ± 1.06%, respectively. In vitro release studies revealed that the SNEDDS formulation had increased CA solubility. CA-SNEDDS-C3 increased CA cellular uptake, possibly due to increased CA solubility and the inhibition of enzymatic conversion to cefuroxime. Finally, in terms of the improvement of oral bioavailability, CA-loaded-SNEDDS could be a viable alternative to commercially available CA formulations. Full article
(This article belongs to the Special Issue Advanced Nanomaterials for Drug Delivery)
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22 pages, 8831 KiB  
Article
Multifunctional Biomimetic Nanofibrous Scaffold Loaded with Asiaticoside for Rapid Diabetic Wound Healing
by Sneha Anand, Paruvathanahalli Siddalingam Rajinikanth, Dilip Kumar Arya, Prashant Pandey, Ravi K. Gupta, Ruchi Sankhwar and Kumarappan Chidambaram
Pharmaceutics 2022, 14(2), 273; https://doi.org/10.3390/pharmaceutics14020273 - 24 Jan 2022
Cited by 36 | Viewed by 3973
Abstract
Diabetes mellitus is a chronic disease with a high mortality rate and many complications. A non-healing diabetic foot ulcer (DFU) is one the most serious complications, leading to lower-extremity amputation in 15% of diabetic patients. Nanofibers are emerging as versatile wound dressing due [...] Read more.
Diabetes mellitus is a chronic disease with a high mortality rate and many complications. A non-healing diabetic foot ulcer (DFU) is one the most serious complications, leading to lower-extremity amputation in 15% of diabetic patients. Nanofibers are emerging as versatile wound dressing due to their unique wound healing properties, such as a high surface area to volume ratio, porosity, and ability to maintain a moist wound environment capable of delivering sustained drug release and oxygen supply to a wound. The present study was aimed to prepare and evaluate a polyvinyl alcohol (PVA)–sodium alginate (SA)–silk fibroin (SF)-based multifunctional nanofibrous scaffold loaded with asiaticoside (AT) in diabetic rats. The SEM findings showed that fibers’ diameters ranged from 100–200 nm, and tensile strengths ranged from 12.41–16.80 MPa. The crosslinked nanofibers were sustained AT over an extended period. The MTT and scratch assay on HaCat cells confirmed low cytotoxicity and significant cell migration, respectively. Antimicrobial tests revealed an excellent anti-microbial efficacy against P. aeruginosa and S. aureus bacteria. In-vivo study demonstrated better wound healing efficacy in diabetic rats. In addition, the histopathological studies showed its ability to restore the normal structure of the skin. The present study concluded that developed multifunctional nanofibers have a great potential for diabetic wound healing applications. Full article
(This article belongs to the Special Issue Advanced Nanomaterials for Drug Delivery)
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Review

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33 pages, 3857 KiB  
Review
High Drug-Loading Nanomedicines for Tumor Chemo–Photo Combination Therapy: Advances and Perspectives
by Ya Wang, Yujie Zhang, Xiaojiang Zhang, Zhe Zhang, Junjun She, Daocheng Wu and Wei Gao
Pharmaceutics 2022, 14(8), 1735; https://doi.org/10.3390/pharmaceutics14081735 - 19 Aug 2022
Cited by 3 | Viewed by 2251
Abstract
The combination of phototherapy and chemotherapy (chemo–photo combination therapy) is an excellent attempt for tumor treatment. The key requirement of this technology is the high drug-loading nanomedicines, which can load either chemotherapy drugs or phototherapy agents at the same nanomedicines and simultaneously deliver [...] Read more.
The combination of phototherapy and chemotherapy (chemo–photo combination therapy) is an excellent attempt for tumor treatment. The key requirement of this technology is the high drug-loading nanomedicines, which can load either chemotherapy drugs or phototherapy agents at the same nanomedicines and simultaneously deliver them to tumors, and play a multimode therapeutic role for tumor treatment. These nanomedicines have high drug-loading efficiency (>30%) and good tumor combination therapeutic effect with important clinical application potential. Although there are many reports of high drug-loading nanomedicines for tumor therapy at present, systematic analyses on those nanomedicines remain lacking and a comprehensive review is urgently needed. In this review, we systematically analyze the current status of developed high drug-loading nanomedicines for tumor chemo–photo combination therapy and summarize their types, methods, drug-loading properties, in vitro and in vivo applications. The shortcomings of the existing high drug-loading nanomedicines for tumor chemo–photo combination therapy and the possible prospective development direction are also discussed. We hope to attract more attention for researchers in different academic fields, provide new insights into the research of tumor therapy and drug delivery system and develop these nanomedicines as the useful tool for tumor chemo–photo combination therapy in the future. Full article
(This article belongs to the Special Issue Advanced Nanomaterials for Drug Delivery)
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30 pages, 9360 KiB  
Review
An Overview of Nanotechnologies for Drug Delivery to the Brain
by Ahsan Ayub and Shawn Wettig
Pharmaceutics 2022, 14(2), 224; https://doi.org/10.3390/pharmaceutics14020224 - 19 Jan 2022
Cited by 35 | Viewed by 6320
Abstract
Drug delivery to the brain has been one of the toughest challenges researchers have faced to develop effective treatments for brain diseases. Owing to the blood–brain barrier (BBB), only a small portion of administered drug can reach the brain. A consequence of that [...] Read more.
Drug delivery to the brain has been one of the toughest challenges researchers have faced to develop effective treatments for brain diseases. Owing to the blood–brain barrier (BBB), only a small portion of administered drug can reach the brain. A consequence of that is the need to administer a higher dose of the drug, which, expectedly, leads to a variety of unwanted side effects. Research in a variety of different fields has been underway for the past couple of decades to address this very serious and frequently lethal problem. One area of research that has produced optimistic results in recent years is nanomedicine. Nanomedicine is the science birthed by fusing the fields of nanotechnology, chemistry and medicine into one. Many different types of nanomedicine-based drug-delivery systems are currently being studied for the sole purpose of improved drug delivery to the brain. This review puts together and briefly summarizes some of the major breakthroughs in this crusade. Inorganic nanoparticle-based drug-delivery systems, such as gold nanoparticles and magnetic nanoparticles, are discussed, as well as some organic nanoparticulate systems. Amongst the organic drug-delivery nanosystems, polymeric micelles and dendrimers are discussed briefly and solid polymeric nanoparticles are explored in detail. Full article
(This article belongs to the Special Issue Advanced Nanomaterials for Drug Delivery)
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