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A special issue of Pharmaceutics (ISSN 1999-4923). This special issue belongs to the section "Nanomedicine and Nanotechnology".

Deadline for manuscript submissions: 30 April 2025 | Viewed by 8319

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Dr. Carla Serri

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Department of Medicine, Surgery and Pharmacy, University of Sassari, Via Muroni 23/a, 07100 Sassari, Italy
Interests: polymeric nanoparticles; nanomedicine; pharmaceutical technology; lipid nanoparticles; nanoprecipitation; nanoparticles loading poorly soluble drugs; drug delivery
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Special Issue Information

Dear Colleagues,

Nanotechnology is a scientific branch focused on designing, fabricating, and applying nanostructures and nanomaterials at the nanometer scale. There has been growing interest in using nanotechnologies to produce and investigate carriers for drug delivery. In this sense, nanocarriers (such as liposomes and derivatives, metal nanoparticles, carbon nanoparticles and nanotubes, nanocrystals, polymeric nanospheres, nanocapsules and micelles) can be used to control the release and delivery of Active Pharmaceutical Ingredients (APIs), enhance the dissolution of poorly soluble APIs and improve their bioavailability and decrease the side effects.

In this Special Issue of Pharmaceutics, original research articles and reviews regarding nanotechnology applications in the pharmaceutical field are welcome. Herein, we intend to highlight the advances in new technologies for the development of different types of nanocarriers via the use of green techniques and materials. Articles centred on formulation strategies to encapsulate biological macromolecules are particularly appreciated.

I look forward to receiving your contributions.

Dr. Carla Serri
Guest Editor

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Keywords

biomaterials
nanomedicine
nanotechnology
formulations
green production technologies
biological macromolecule nanoencapsulation

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Published Papers (5 papers)

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Research

19 pages, 3385 KiB

Open AccessArticle

Bioactive Properties and In Vitro Digestive Release of Cannabidiol (CBD) from Tailored Composites Based on Carbon Materials

by Karol Zapata, Angie D. Vélez, Jorge A. Correa, Francisco Carrasco-Marín, Benjamín A. Rojano, Camilo A. Franco and Farid B. Cortés

Pharmaceutics 2024, 16(9), 1132; https://doi.org/10.3390/pharmaceutics16091132 - 27 Aug 2024

Viewed by 801

Abstract

The use of carriers to improve cannabidiol (CBD) bioavailability during digestion is at the forefront of research. The main objective of this research was to evaluate CBD bioactivity and develop CBD composites based on tailored carbon support to improve availability under digestive conditions. The antioxidant capacity of CBD was evaluated using spectrophotometric methods, and anti-proliferative assays were carried out using human colon carcinoma cells (SW480). Twenty-four composites of CBD + carbon supports were developed, and CBD desorption tests were carried out under simulated digestive conditions. The antioxidant capacity of CBD was comparable to and superior to Butylhydrox-ytoluene (BHT), a commercial antioxidant. CBD reflected an IC-50 of 10,000 mg/L against SW480 cancer cells. CBD in biological systems can increase the shelf life of lipid and protein foods by 7 and 470 days, respectively. Finally, acid carbons showed major CBD adsorption related to electrostatic interactions, but basic carbons showed better delivery properties related to electrostatic repulsion. A tailored composite was achieved with a CBD load of 27 mg/g with the capacity to deliver 1.1 mg, 21.8 mg, and 4 mg to the mouth, stomach, and duodenum during 18 h, respectively. This is a pioneering study since the carriers were intelligently developed to improve CBD release. Full article

(This article belongs to the Special Issue Advances in Nanotechnology-Based Drug Delivery Systems)

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12 pages, 1413 KiB

Open AccessArticle

Synthesis, Characterization, and Cytotoxicity Evaluation of Chlorambucil-Functionalized Mesoporous Silica Nanoparticles

by Juliana Camila Fischer Karnopp, Juliana Jorge, Jaqueline Rodrigues da Silva, Diego Boldo, Kristiane Fanti Del Pino Santos, Adriana Pereira Duarte, Gustavo Rocha de Castro, Ricardo Bentes de Azevedo, Ariadna Lafourcade Prada, Jesús Rafael Rodríguez Amado and Marco Antonio Utrera Martines

Pharmaceutics 2024, 16(8), 1086; https://doi.org/10.3390/pharmaceutics16081086 - 19 Aug 2024

Cited by 1 | Viewed by 1059

Abstract

This study describes the synthesis and characterization of chlorambucil (CLB)-functionalized mesoporous silica nanoparticles (MSNs) for potential application in cancer therapy. The nanoparticles were designed with a diameter between 20 and 50 nm to optimize cellular uptake and avoid rapid clearance from the bloodstream. The synthesis method involved modifying a previously reported technique to reduce particle size. Successful functionalization with CLB was confirmed through various techniques, including Fourier transform infrared spectroscopy (FTIR) and elemental analysis. The cytotoxicity of the CLB-functionalized nanoparticles (MSN@NH₂-CLB) was evaluated against human lung adenocarcinoma cells (A549) and colon carcinoma cells (CT26WT). The results suggest significantly higher cytotoxicity of MSN@NH₂-CLB compared to unbound CLB, with improved selectivity towards cancer cells over normal cells. This suggests that MSN@NH₂-CLB holds promise as a drug delivery system for targeted cancer therapy. Full article

(This article belongs to the Special Issue Advances in Nanotechnology-Based Drug Delivery Systems)

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23 pages, 7257 KiB

Open AccessArticle

Green Solid Lipid Nanoparticles by Fatty Acid Coacervation: An Innovative Nasal Delivery Tool for Drugs Targeting Cerebrovascular and Neurological Diseases

by Annalisa Bozza, Valentina Bordano, Arianna Marengo, Elisabetta Muntoni, Elisabetta Marini, Loretta Lazzarato, Chiara Dianzani, Chiara Monge, Arianna Carolina Rosa, Luigi Cangemi, Maria Carmen Valsania, Barbara Colitti, Ezio Camisassa and Luigi Battaglia

Pharmaceutics 2024, 16(8), 1051; https://doi.org/10.3390/pharmaceutics16081051 - 8 Aug 2024

Viewed by 1156

Abstract

Cerebrovascular and neurological diseases are characterized by neuroinflammation, which alters the neurovascular unit, whose interaction with the choroid plexus is critical for maintaining brain homeostasis and producing cerebrospinal fluid. Dysfunctions in such process can lead to conditions such as idiopathic normal pressure hydrocephalus, a common disease in older adults. Potential pharmacological treatments, based upon intranasal administration, are worthy of investigation because they might improve symptoms and avoid surgery by overcoming the blood–brain barrier and avoiding hepatic metabolism. Nasal lipid nanocarriers, such as solid lipid nanoparticles, may increase the nasal retention and permeation of drugs. To this aim, green solid lipid nanoparticles, obtained by coacervation from natural soaps, are promising vehicles due to their specific lipid matrix composition and the unsaponifiable fraction, endowed with antioxidant and anti-inflammatory properties, and thus suitable for restoring the neurovascular unit function. In this experimental work, such green solid lipid nanoparticles, fully characterized from a physico-chemical standpoint, were loaded with a drug combination suitable for reverting hydrocephalus symptoms, allowing us to obtain a non-toxic formulation, a reduction in the production of the cerebrospinal fluid in vitro, and a vasoprotective effect on an isolated vessel model. The pharmacokinetics and biodistribution of fluorescently labelled nanoparticles were also tested in animal models. Full article

(This article belongs to the Special Issue Advances in Nanotechnology-Based Drug Delivery Systems)

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18 pages, 3072 KiB

Open AccessArticle

Hyaluronic Acid-Based Nanoparticles Loaded with Rutin as Vasculo-Protective Tools against Anthracycline-Induced Endothelial Damages

by Carla Serri, Vincenzo Quagliariello, Iriczalli Cruz-Maya, Vincenzo Guarino, Nicola Maurea, Paolo Giunchedi, Giovanna Rassu and Elisabetta Gavini

Pharmaceutics 2024, 16(8), 985; https://doi.org/10.3390/pharmaceutics16080985 - 25 Jul 2024

Viewed by 857

Abstract

Anthracycline-based therapies exert endothelial damages through peroxidation and the production of proinflammatory cytokines, resulting in a high risk of cardiovascular complications in cancer patients. Hyaluronic acid-based hybrid nanoparticles (LicpHA) are effective pharmacological tools that can target endothelial cells and deliver drugs or nutraceuticals. This study aimed to prepared and characterized a novel LicpHA loaded with Rutin (LicpHA Rutin), a flavonoid with high antioxidant and anti-inflammatory properties, to protect endothelial cells against epirubicin-mediated endothelial damages. LicpHA Rutin was prepared using phosphatidylcholine, cholesterol, poloxamers, and hyaluronic acid by a modified nanoprecipitation technique. The chemical-physical characterization of the nanoparticles was carried out (size, zeta potential, morphology, stability, thermal analysis, and encapsulation efficiency). Cytotoxicity studies were performed in human endothelial cells exposed to epirubicin alone or in combination with Free-Rutin or LicpHA Rutin. Anti-inflammatory studies were performed through the intracellular quantification of NLRP-3, MyD-88, IL-1β, IL-6, IL17-α, TNF-α, IL-10, and IL-4 using selective ELISA methods. Morphological studies via TEM and image analysis highlighted a heterogeneous population of LicpHA particles with non-spherical shapes (circularity equal to 0.78 ± 0.14), and the particle size was slightly affected by Rutin entrapment (the mean diameter varied from 179 ± 4 nm to 209 ± 4 nm). Thermal analysis and zeta potential analyses confirmed the influence of Rutin on the chemical-physical properties of LicpHA Rutin, mainly indicated by the decrease in the surface negative charge (from −35 ± 1 mV to −30 ± 0.5 mV). Cellular studies demonstrated that LicpHA Rutin significantly reduced cell death and inflammation when compared to epirubicin alone. The levels of intracellular NLRP3, Myd-88, and proinflammatory cytokines were significantly lower in epirubicin + LicpHA Rutin-exposed cells when compared to epirubicin groups (p < 0.001). Hyaluronic acid-based nanoparticles loaded with Rutin exerts significant vasculo-protective properties during exposure to anthracyclines. The overall picture of this study pushes towards preclinical and clinical studies in models of anthracycline-induced vascular damages. Full article

(This article belongs to the Special Issue Advances in Nanotechnology-Based Drug Delivery Systems)

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23 pages, 19779 KiB

Open AccessEditor’s ChoiceArticle

Optimizing mRNA-Loaded Lipid Nanoparticles as a Potential Tool for Protein-Replacement Therapy

by Rocío Gambaro, Ignacio Rivero Berti, María José Limeres, Cristián Huck-Iriart, Malin Svensson, Silvia Fraude, Leah Pretsch, Shutian Si, Ingo Lieberwirth, Stephan Gehring, Maximiliano Cacicedo and Germán Abel Islan

Pharmaceutics 2024, 16(6), 771; https://doi.org/10.3390/pharmaceutics16060771 - 6 Jun 2024

Cited by 1 | Viewed by 3372

Abstract

Lipid nanoparticles (LNPs) tailored for mRNA delivery were optimized to serve as a platform for treating metabolic diseases. Four distinct lipid mixes (LMs) were formulated by modifying various components: LM1 (ALC-0315/DSPC/Cholesterol/ALC-0159), LM2 (ALC-0315/DOPE/Cholesterol/ALC-0159), LM3 (ALC-0315/DSPC/Cholesterol/DMG-PEG2k), and LM4 (DLin-MC3-DMA/DSPC/Cholesterol/ALC-0159). LNPs exhibited stability and homogeneity with a mean size of 75 to 90 nm, confirmed by cryo-TEM and SAXS studies. High mRNA encapsulation (95–100%) was achieved. LNPs effectively delivered EGFP-encoding mRNA to HepG2 and DC2.4 cell lines. LNPs induced cytokine secretion from human peripheral blood mononuclear cells (PBMCs), revealing that LM1, LM2, and LM4 induced 1.5- to 4-fold increases in IL-8, TNF-α, and MCP-1 levels, while LM3 showed minimal changes. Reporter mRNA expression was observed in LNP-treated PBMCs. Hemotoxicity studies confirmed formulation biocompatibility with values below 2%. In vivo biodistribution in mice post intramuscular injection showed significant mRNA expression, mainly in the liver. The modification of LNP components influenced reactogenicity, inflammatory response, and mRNA expression, offering a promising platform for selecting less reactogenic carriers suitable for repetitive dosing in metabolic disease treatment. Full article

(This article belongs to the Special Issue Advances in Nanotechnology-Based Drug Delivery Systems)

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