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Pharmaceutics
Special Issues
Nanotechnology in Drug Delivery and Controlled Release
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Nanotechnology in Drug Delivery and Controlled Release

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

Deadline for manuscript submissions: closed (20 July 2023) | Viewed by 13902

Special Issue Editors

Prof. Dr. Yan Pang

E-Mail Website
Guest Editor
Shanghai Key Laboratory of Orbital Diseases and Ocular Oncology, Department of Ophthalmology, Shanghai Ninth People’s Hospital, School of Medicine, Shanghai Jiao Tong University, Shanghai 200011, China
Interests: functional polymer; drug delivery systems; nanocarriers; ocular related delivery systems; oral delivery
Dr. Wen Tang

E-Mail Website
Guest Editor
South China Advanced Institute for Soft Matter Science and Technology, School of Emergent Soft Matter, South China University of Technology, Guangzhou 510640, Guangdong, China
Interests: stimuli-responsive drug delivery; bioactive polymer; antibacterial materials

Special Issue Information

Dear Colleagues,

In the field of medicine, nanotechnology has attracted great interest due to its ability to solve many problems that cannot be overcome using conventional drugs, such as lack of targeting ability, systemic toxicity, concentration changes, etc. Nanotechnology has also made remarkable progress in drug delivery and controlled release in the past decades. Through combination with various organic or inorganic natural or synthetic nanomaterials, properties such as drug solubility, blood circulation time, and in vivo distribution can be altered. Moreover, sustained or stimulated response release can enhance the therapeutic efficacy of the drug, allowing it to be used to treat various conditions such as cancer, chronic inflammation, and infection in addition to diseases related to various organs (ocular diseases, dental diseases, heart diseases, brain diseases, and so on). Although much has been achieved in the existing research, challenges remain, and the development of more precise and intelligent nanodrug delivery systems holds promise.

This Special Issue aims to highlight recent advances in the field of drug delivery, particularly novel design and smart strategies to tackle biosafety and drug efficacy issues. Thus, we invites all researchers to publish work on the following topics in this Special Issue of Pharmaceutics “Nanotechnology in Drug Delivery and Controlled Release”: nanodrug delivery systems using stimulus-responsive and smart biomaterials; nanotechnology to overcome the drug delivery barriers including the blood–brain barrier, ocular barriers, intestinal barriers, biofilms, and so on; multifunctional targeted therapeutic nanoparticles, such as the combination of chemotherapy, immunotherapy, photodynamic therapy, thermodynamic therapy, etc.; interactions between nanodrug and living system to address biosafety issues. Original research papers, communications, and review articles are all welcome for submission to this Special Issue.

Prof. Dr. Yan Pang
Dr. Wen Tang
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

  • nanosized drug delivery systems
  • nanomedicine
  • controlled drug release
  • targeted drug delivery
  • stimuli-responsive nanocarriers
  • drug efficacy
  • biosafety

Published Papers (6 papers)

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Research

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14 pages, 4907 KiB  
Article
Ganglioside GM3-Functionalized Reconstituted High-Density Lipoprotein (GM3-rHDL) as a Novel Nanocarrier Enhances Antiatherosclerotic Efficacy of Statins in apoE−/− C57BL/6 Mice
by Bo Wei, Yuanfang Li, Meiying Ao, Wenxiang Shao, Kun Wang, Tong Rong, Yun Zhou and Yong Chen
Pharmaceutics 2022, 14(11), 2534; https://doi.org/10.3390/pharmaceutics14112534 - 20 Nov 2022
Cited by 4 | Viewed by 1474
Abstract
Previously, we found that exogenous ganglioside GM3 had an antiatherosclerotic efficacy and that its antiatherosclerotic efficacy could be enhanced by reconstituted high-density lipoprotein (rHDL). In this study, we hypothesized that GM3-functionalized rHDL (i.e., GM3-rHDL) as a nanocarrier can promote the efficacy of traditional [...] Read more.
Previously, we found that exogenous ganglioside GM3 had an antiatherosclerotic efficacy and that its antiatherosclerotic efficacy could be enhanced by reconstituted high-density lipoprotein (rHDL). In this study, we hypothesized that GM3-functionalized rHDL (i.e., GM3-rHDL) as a nanocarrier can promote the efficacy of traditional antiatherosclerotic drugs (e.g., statins). To test this hypothesis, lovastatin (LT) was used as a representative of statins, and LT-loaded GM3-rHDL nanoparticle (LT-GM3-rHDL or LT@GM3-rHDL; a mean size of ~142 nm) and multiple controls (e.g., GM3-rHDL without LT, LT-loaded rHDL or LT-rHDL, and other nanoparticles) were prepared. By using two different microsphere-based methods, the presences of apolipoprotein A-I (apoA-I) and/or GM3 in nanoparticles and the apoA-I-mediated macrophage-targeting ability of apoA-I/rHDL-containing nanoparticles were verified in vitro. Moreover, LT-GM3-rHDL nanoparticle had a slowly sustained LT release in vitro and the strongest inhibitory effect on the foam cell formation of macrophages (a key event of atherogenesis). After single administration of rHDL-based nanoparticles, a higher LT concentration was detected shortly in the atherosclerotic plaques of apoE−/− mice than non-rHDL-based nanoparticles, suggesting the in vivo plaque-targeting ability of apoA-I/rHDL-containing nanoparticles. Finally, among all nanoparticles LT-GM3-rHDL induced the largest decreases in the contents of blood lipids and in the areas of atherosclerotic plaques at various aortic locations in apoE−/− mice fed a high-fat diet for 12 weeks, supporting that LT-GM3-rHDL has the best in vivo antiatherosclerotic efficacy among the tested nanoparticles. Our data imply that GM3-functionalized rHDL (i.e., GM3-rHDL) can be utilized as a novel nanocarrier to enhance the efficacy of traditional antiatherosclerotic drugs (e.g., statins). Full article
(This article belongs to the Special Issue Nanotechnology in Drug Delivery and Controlled Release)
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13 pages, 1384 KiB  
Article
Transfer Phenomena of Nanoliposomes by Live Imaging of Primary Cultures of Cortical Neurons
by Elodie Passeri, Philippe Bun, Kamil Elkhoury, Michel Linder, Catherine Malaplate, Frances T. Yen and Elmira Arab-Tehrany
Pharmaceutics 2022, 14(10), 2172; https://doi.org/10.3390/pharmaceutics14102172 - 12 Oct 2022
Cited by 3 | Viewed by 1331
Abstract
Soft nanoparticles, and in particular, nanoliposomes (NL), have attracted increasing interest for their use in food, nutraceuticals, and in particular, in pharmaceutics for drug delivery. Recent data using salmon lecithin NL suggest that these NL, rich in omega-3 (n-3) fatty acids, can improve [...] Read more.
Soft nanoparticles, and in particular, nanoliposomes (NL), have attracted increasing interest for their use in food, nutraceuticals, and in particular, in pharmaceutics for drug delivery. Recent data using salmon lecithin NL suggest that these NL, rich in omega-3 (n-3) fatty acids, can improve the bioavailability and transport of molecules through the blood brain barrier (BBB) to target the brain for the prevention and treatment of neurodegenerative diseases. The objective of this study was to characterize the physicochemical properties and analyze the transfer phenomena of salmon lecithin NL over time in neurons to better understand the behavior of NL in an intracellular environment. To test this, primary cultures of cortical neurons from rat embryos were incubated with salmon lecithin NL from day 3 after cell culture, for up to 104 h. The physicochemical properties of NL such as size, speed, morphology and the diffusion coefficient in the live cultures, were studied over time. Image analysis of cell morphology showed dendritic growth and neuronal arborization after 48 h of exposure to NL, for up to 104 h. Results showed an NL stability in size, speed and diffusion coefficient over time, with a peak at 48 h, and then a return to baseline value at the end of incubation. The average speed and diffusion coefficient achieved provided important information on the mode of entry of NL into neurons, and on the slow diffusion rate of NL into the cells. Analysis of videos from 2 h to 104 h showed that significant levels of NL were already internalized by neurons after 3 h incubation. NL appearance and intracellular distribution indicated that they were packed in intracellular compartments similar to endocytic vesicles, suggesting internalization by an active endocytic-like process. The results obtained here demonstrate internalization of NL by cortical neurons by an active endocytic-like process, and suggest the potential use of NL for time-release of therapeutics aimed towards prevention or treatment of neurodegenerative diseases. Full article
(This article belongs to the Special Issue Nanotechnology in Drug Delivery and Controlled Release)
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18 pages, 4365 KiB  
Article
Preparation and Study of Solid Lipid Nanoparticles Based on Curcumin, Resveratrol and Capsaicin Containing Linolenic Acid
by Roberta Cassano, Simona Serini, Federica Curcio, Sonia Trombino and Gabriella Calviello
Pharmaceutics 2022, 14(8), 1593; https://doi.org/10.3390/pharmaceutics14081593 - 30 Jul 2022
Cited by 10 | Viewed by 1647
Abstract
Linolenic acid (LNA) is the most highly consumed polyunsaturated fatty acid found in the human diet. It possesses anti-inflammatory effects and the ability to reverse skin-related disorders related to its deficiency. The purpose of this work was to encapsulate LNA in solid lipid [...] Read more.
Linolenic acid (LNA) is the most highly consumed polyunsaturated fatty acid found in the human diet. It possesses anti-inflammatory effects and the ability to reverse skin-related disorders related to its deficiency. The purpose of this work was to encapsulate LNA in solid lipid nanoparticles (SLNs) based on curcumin, resveratrol and capsaicin for the treatment of atopic dermatitis. These compounds were first esterified with oleic acid to obtain two moonoleate and one oleate ester, then they were used for SLN matrix realization through the emulsification method. The intermediates of the esterification reaction were characterized by FT-IR and 1N-MR analysis. SLNs were characterized by dimensional analysis and encapsulation efficiency. Skin permeation studies, antioxidant and anti-inflammatory activities were evaluated. LNA was released over 24 h from nanoparticles, and resveratrol monooleate-filled SLNs exhibited a good antioxidant activity. The curcumin-based SLNs loaded or not with LNA did not induce significant cytotoxicity in NCTC 2544 and THP-1 cells. Moreover, these SLNs loaded with LNA inhibited the production of IL-6 in NCTC 2544 cells. Overall, our data demonstrate that the synthesized SLNs could represent an efficacious way to deliver LNA to skin cells and to preserve the anti-inflammatory properties of LNA for the topical adjuvant treatment of atopic dermatitis. Full article
(This article belongs to the Special Issue Nanotechnology in Drug Delivery and Controlled Release)
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17 pages, 4127 KiB  
Article
Folate-Modified Chitosan 5-Flourouraci Nanoparticles-Embedded Calcium Alginate Beads for Colon Targeted Delivery
by Shafi Ullah, Asif Nawaz, Arshad Farid, Muhammad Shahid Latif, Muhammad Fareed, Shakira Ghazanfar, Charis M. Galanakis, Abdulhakeem S. Alamri, Majid Alhomrani and Syed Mohammed Basheeruddin Asdaq
Pharmaceutics 2022, 14(7), 1366; https://doi.org/10.3390/pharmaceutics14071366 - 28 Jun 2022
Cited by 4 | Viewed by 1728
Abstract
Gel beads are formed when alginate acid reacts with divalent cations, particularly Ca2+. As a result of this feature, it is one of the best materials for making gel beads. Furthermore, it swells only slightly at acidic pH, resulting in stable [...] Read more.
Gel beads are formed when alginate acid reacts with divalent cations, particularly Ca2+. As a result of this feature, it is one of the best materials for making gel beads. Furthermore, it swells only slightly at acidic pH, resulting in stable alginate acid beads, but swells and dissolves rapidly at higher pH values, leading to pH-responsive release. Our current study aimed to embed folate-modified chitosan 5FU nanoparticles (FA-CS-5FU-NPs) into calcium alginate beads for colon-targeted delivery. Calcium alginate beads were developed successfully. Based on the method of drying, two types of beads were obtained: freeze-dried folate-modified chitosan 5FU nanoparticles-embedded beads (FA-CS-5FU-NP-Bf) and oven-dried folate-modified chitosan 5FU nanoparticles-embedded beads (FA-CS-5FU-NP-Bo). The size of (FA-CS-5FU-NP-Bf) was significantly larger than (FA-CS-5FU-NP-Bo). Swelling index (SI), erosion index (EI), and water-uptake index (WUI) of (FA-CS-5FU-NP-Bf) beads were significantly higher than FA-CS-5FU-NP-Bo beads at simulated intestinal pH. An insignificant difference was observed in the release rate of 5FU between (FA-CS-5FU-NP-Bf) and FA-CS-5FU-NP-Bo. The release rate of FA-CS-5FU-NPs was significantly higher than FA-CS-5FU-NP-Bf and FA-CS-5FU-NP-Bo. Pharmacokinetic parameters of 5FU solution, FA-CS-5FU-NPs, and FA-CS-5FU-NP-Bo were analyzed. Solution of pure 5FU showed significantly higher Cmax and lower AUC, T1/2, and Vd than both FA-CS-5FU-NPs and FA-CS-5FU-NPs-Bo, suggesting that FA-CS-5FU-NPs and FA-CS-5FU-NPs-Bo have sustained-release behavior. Biodistribution studies also show that maximum drug amounts were found in the colon from nanoparticles-embedded beads. FA-CS-5FU-NPs-Bo avoid releasing drugs in the stomach and small intestine and make them available in the colon region in higher concentrations to target the colon region specifically. Full article
(This article belongs to the Special Issue Nanotechnology in Drug Delivery and Controlled Release)
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Review

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19 pages, 757 KiB  
Review
Myocardial Cell Preservation from Potential Cardiotoxic Drugs: The Role of Nanotechnologies
by Adelaide Iervolino, Luigi Spadafora, Cristiano Spadaccio, Valentina Iervolino, Giuseppe Biondi Zoccai and Felicita Andreotti
Pharmaceutics 2023, 15(1), 87; https://doi.org/10.3390/pharmaceutics15010087 - 27 Dec 2022
Viewed by 2284
Abstract
Cardiotoxic therapies, whether chemotherapeutic or antibiotic, represent a burden for patients who may need to interrupt life-saving treatment because of serious complications. Cardiotoxicity is a broad term, spanning from forms of heart failure induction, particularly left ventricular systolic dysfunction, to induction of arrhythmias. [...] Read more.
Cardiotoxic therapies, whether chemotherapeutic or antibiotic, represent a burden for patients who may need to interrupt life-saving treatment because of serious complications. Cardiotoxicity is a broad term, spanning from forms of heart failure induction, particularly left ventricular systolic dysfunction, to induction of arrhythmias. Nanotechnologies emerged decades ago. They offer the possibility to modify the profiles of potentially toxic drugs and to abolish off-target side effects thanks to more favorable pharmacokinetics and dynamics. This relatively modern science encompasses nanocarriers (e.g., liposomes, niosomes, and dendrimers) and other delivery systems applicable to real-life clinical settings. We here review selected applications of nanotechnology to the fields of pharmacology and cardio-oncology. Heart tissue-sparing co-administration of nanocarriers bound to chemotherapeutics (such as anthracyclines and platinum agents) are discussed based on recent studies. Nanotechnology applications supporting the administration of potentially cardiotoxic oncological target therapies, antibiotics (especially macrolides and fluoroquinolones), or neuroactive agents are also summarized. The future of nanotechnologies includes studies to improve therapeutic safety and to encompass a broader range of pharmacological agents. The field merits investments and research, as testified by its exponential growth. Full article
(This article belongs to the Special Issue Nanotechnology in Drug Delivery and Controlled Release)
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34 pages, 1432 KiB  
Review
Hyaluronic Acid-Based Nanomaterials Applied to Cancer: Where Are We Now?
by Vera Machado, Mariana Morais and Rui Medeiros
Pharmaceutics 2022, 14(10), 2092; https://doi.org/10.3390/pharmaceutics14102092 - 30 Sep 2022
Cited by 10 | Viewed by 4811
Abstract
Cancer cells normally develop the ability to rewire or reprogram themselves to become resistant to treatments that were previously effective. Despite progress in understanding drug resistance, knowledge gaps remain regarding the underlying biological causes of drug resistance and the design of cancer treatments [...] Read more.
Cancer cells normally develop the ability to rewire or reprogram themselves to become resistant to treatments that were previously effective. Despite progress in understanding drug resistance, knowledge gaps remain regarding the underlying biological causes of drug resistance and the design of cancer treatments to overcome it. So, resistance acquisition remains a major problem in cancer treatment. Targeted therapeutics are considered the next generation of cancer therapy because they overcome many limitations of traditional treatments. Numerous tumor cells overexpress several receptors that have a high binding affinity for hyaluronic acid (HA), while they are poorly expressed in normal body cells. HA and its derivatives have the advantage of being biocompatible and biodegradable and may be conjugated with a variety of drugs and drug carriers for developing various formulations as anticancer therapies such as micelles, nanogels, and inorganic nanoparticles. Due to their stability in blood circulation and predictable delivery patterns, enhanced tumor-selective drug accumulation, and decreased toxicity to normal tissues, tumor-targeting nanomaterial-based drug delivery systems have been shown to represent an efficacious approach for the treatment of cancer. In this review, we aim to provide an overview of some in vitro and in vivo studies related to the potential of HA as a ligand to develop targeted nanovehicles for future biomedical applications in cancer treatment. Full article
(This article belongs to the Special Issue Nanotechnology in Drug Delivery and Controlled Release)
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