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Nanostructured Drug Delivery Systems: Modeling, Preparation and Characterisation

A special issue of International Journal of Molecular Sciences (ISSN 1422-0067). This special issue belongs to the section "Materials Science".

Deadline for manuscript submissions: closed (31 December 2022) | Viewed by 15043

Special Issue Editors

Special Issue Information

Dear Colleagues,

Nanostructured objects are systems with one or more dimensions or features reduced to the nanoscale, presenting some unique and sometimes unprecedented physicochemical properties. The possibility of manipulating and regulating these properties makes them suitable for a variety of nanomedical applications. In recent years, low-dimensional structures with specific advanced functional properties have attracted extremely extensive research interest in pharmaceutical and healthcare fields. The nano-encapsulation of drugs or nutrients is a promising and broadly applied formulation technology that enables several interesting novel delivery concepts. Despite decades of technical development, nanostructured materials face considerable challenges in bringing them closer to successful and widespread practical application.

The aim of this Special Issue of the International Journal of Molecular Sciences is to bring together original and high-quality research papers covering the most recent advances as well as comprehensive reviews addressing state-of-the-art topics in the field of the design, synthesis, and chemical/physicochemical characterization of nanostructured drug delivery systems.

Preferred topics:

  • Modeling of drug–carrier interactions by advanced measuring methods;
  • Design and synthesis of biocompatible and nanostructured drug delivery particles;
  • Application of hydrogels, aerogels and polymer/surfactant associates as drug carriers;
  • Characterisation and modification of the drug dissolution process;
  • Encapsulation and controlled release of proteins, vitamins and minerals.

In advance, I would like to gratefully acknowledge the authors and reviewers who will participate to the elaboration of this Special Issue and that will contribute to the development of research based on the nanostructured drug delivery systems.

Dr. Ádám Juhász
Dr. Edit Csapó
Guest Editors

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Keywords

  • nanostructured materials
  • drug delivery
  • drug-carrier interactions
  • hydrogel
  • aerogels
  • associated colloids
  • surfactants
  • macromolecules
  • porous materials
  • hybrid materials
  • controlled release

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Related Special Issue

Published Papers (7 papers)

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Research

14 pages, 1764 KiB  
Article
In Vivo Sustained Release of the Retrograde Transport Inhibitor Retro-2.1 Formulated in a Thermosensitive Hydrogel
by Robin Vinck, Laetitia Anvi Nguyen, Mathilde Munier, Lucie Caramelle, Diana Karpman, Julien Barbier, Alain Pruvost, Jean-Christophe Cintrat and Daniel Gillet
Int. J. Mol. Sci. 2022, 23(23), 14611; https://doi.org/10.3390/ijms232314611 - 23 Nov 2022
Cited by 2 | Viewed by 1238
Abstract
A recently developed inhibitor of retrograde transport, namely Retro-2.1, proved to be a potent and broad-spectrum lead in vitro against intracellular pathogens, such as toxins, parasites, intracellular bacteria and viruses. To circumvent its low aqueous solubility, a formulation in poly(ethylene glycol)-block-poly(D,L)lactide [...] Read more.
A recently developed inhibitor of retrograde transport, namely Retro-2.1, proved to be a potent and broad-spectrum lead in vitro against intracellular pathogens, such as toxins, parasites, intracellular bacteria and viruses. To circumvent its low aqueous solubility, a formulation in poly(ethylene glycol)-block-poly(D,L)lactide micelle nanoparticles was developed. This formulation enabled the study of the pharmacokinetic parameters of Retro-2.1 in mice following intravenous and intraperitoneal injections, revealing a short blood circulation time, with an elimination half-life of 5 and 6.7 h, respectively. To explain the poor pharmacokinetic parameters, the metabolic stability of Retro-2.1 was studied in vitro and in vivo, revealing fast cytochrome-P-450-mediated metabolism into a less potent hydroxylated analogue. Subcutaneous injection of Retro-2.1 formulated in a biocompatible and bioresorbable polymer-based thermosensitive hydrogel allowed for sustained release of the drug, with an elimination half-life of 19 h, and better control of its metabolism. This study provides a guideline on how to administer this promising lead in vivo in order to study its efficacy. Full article
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20 pages, 3565 KiB  
Article
Preparation of Nano/Microcapsules of Ozonated Olive Oil in Hyaluronan Matrix and Analysis of Physicochemical and Microbiological (Biological) Properties of the Obtained Biocomposite
by Gohar Khachatryan, Lusine Khachatryan, Magdalena Krystyjan, Anna Lenart-Boroń, Marcel Krzan, Klaudia Kulik, Anna Białecka, Maja Grabacka, Nikola Nowak and Karen Khachatryan
Int. J. Mol. Sci. 2022, 23(22), 14005; https://doi.org/10.3390/ijms232214005 - 13 Nov 2022
Cited by 7 | Viewed by 2297
Abstract
Hydrogels, based on natural polymers, such as hyaluronic acid, are gaining an increasing popularity because of their biological activity. The antibacterial effect of ozone is widely known and used, but the instability the gas causes, severely limits its application. Ozone entrapment in olive [...] Read more.
Hydrogels, based on natural polymers, such as hyaluronic acid, are gaining an increasing popularity because of their biological activity. The antibacterial effect of ozone is widely known and used, but the instability the gas causes, severely limits its application. Ozone entrapment in olive oil by its reaction with an unsaturated bond, allows for the formation of stable, therapeutically active ozone derivatives. In this study, we obtained an innovative hydrogel, based on hyaluronic acid containing micro/nanocapsules of ozonated olive oil. By combination of the biocompatible polymer with a high regenerative capacity and biologically active ingredients, we obtained a hydrogel with regenerative properties and a very weak inhibitory effect against both bacterial commensal skin microbiota and pathogenic Candida-like yeasts. We assessed the stability and rheological properties of the gel, determined the morphology of the composite, using scanning electron microscopy (SEM) and particle size by the dynamic light scattering (DLS) method. We also performed Attenuated total reflectance Fourier transform infrared (FTIR-ATR) spectroscopy. The functional properties, including the antimicrobial potential were assessed by the microbiological analysis and in vitro testing on the HaCat human keratinocyte cell line. The studies proved that the obtained emulsions were rheologically stable, exhibited an antimicrobial effect and did not show cytotoxicity in the HaCat keratinocyte model. Full article
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8 pages, 2290 KiB  
Article
PLGA–TiO2 as a Carrier System for Drug Release
by M. I. Torres-Ramos, M. F. Martín-Marquez, María del Carmen Leal-Moya, Suresh Ghotekar, Jorge Alberto Sánchez-Burgos and Alejandro Pérez-Larios
Int. J. Mol. Sci. 2022, 23(18), 10755; https://doi.org/10.3390/ijms231810755 - 15 Sep 2022
Cited by 8 | Viewed by 1963
Abstract
This paper reports the results of the PLGA–TiO2 nanocomposite regarding the green synthesis of titanium dioxide nanoparticles using a natural extract, its characterization, and encapsulation with poly(lactic-co-glycolic acid) (PLGA). UV–visible spectrometry was used for the identification of terpenes present in the extracts. [...] Read more.
This paper reports the results of the PLGA–TiO2 nanocomposite regarding the green synthesis of titanium dioxide nanoparticles using a natural extract, its characterization, and encapsulation with poly(lactic-co-glycolic acid) (PLGA). UV–visible spectrometry was used for the identification of terpenes present in the extracts. The morphology of the nanoparticles was determined by scanning electron microscopy. Infrared spectroscopy was used for the determination of functional groups, while X-ray diffraction was used to determine the crystal structure. The analysis of the extended release of the encapsulated extract in the matrix of the nanomaterial resulted in a maximum visible UV absorbance at approximately 260 nm and confirmed the synthesis of titanium dioxide nanoparticles. Moreover, terpenes enhance synthesis and stabilize titanium dioxide nanoparticles. The synthesized structures are spherical and amorphous, 44 nm in size, and encapsulated at 65 nm. Full article
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11 pages, 1827 KiB  
Article
Polyoxometalate Nanoparticles as a Potential Glioblastoma Therapeutic via Lipid-Mediated Cell Death
by Michael S. Petronek, Bryan G. Allen, Gregor Luthe and Jeffrey M. Stolwijk
Int. J. Mol. Sci. 2022, 23(15), 8263; https://doi.org/10.3390/ijms23158263 - 27 Jul 2022
Cited by 3 | Viewed by 2200
Abstract
Polyoxometalate nanoparticles (POMs) are a class of compounds made up of multiple transition metals linked together using oxygen atoms. POMs commonly include group 6 transition metals, with two of the most common forms using molybdenum and tungsten. POMs are suggested to exhibit antimicrobial [...] Read more.
Polyoxometalate nanoparticles (POMs) are a class of compounds made up of multiple transition metals linked together using oxygen atoms. POMs commonly include group 6 transition metals, with two of the most common forms using molybdenum and tungsten. POMs are suggested to exhibit antimicrobial effects. In this study, we developed two POM preparations to study anti-cancer activity. We found that Mo-POM (NH4)Mo7O24) and W-POM (H3PW12O40) have anti-cancer effects on glioblastoma cells. Both POMs induced morphological changes marked by membrane swelling and the presence of multinucleated cells that may indicate apoptosis induction along with impaired cell division. We also observed significant increases in lipid oxidation events, suggesting that POMs are redox-active and can catalyze detrimental oxidation events in glioblastoma cells. Here, we present preliminary indications that molybdenum polyoxometalate nanoparticles may act like ferrous iron to catalyze the oxidation of phospholipids. These preliminary results suggest that Mo-POMs (NH4)Mo7O24) and W-POMs (H3PW12O40) may warrant further investigation into their utility as adjunct cancer therapies. Full article
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18 pages, 4330 KiB  
Article
Halochromic Behavior and Anticancer Effect of New Synthetic Anthocyanidins Complexed with β-Cyclodextrin Derivatives
by Iulia Păușescu, Izolda Kántor, György Babos, Zoltán May, Andrea Fodor-Kardos, Zsombor Miskolczy, László Biczók, Francisc Péter, Mihai Medeleanu and Tivadar Feczkó
Int. J. Mol. Sci. 2022, 23(15), 8103; https://doi.org/10.3390/ijms23158103 - 22 Jul 2022
Cited by 2 | Viewed by 1663
Abstract
Anthocyanidins, the aglycons of anthocyanins, are known, beyond their function in plants, also as compounds with a wide range of biological and pharmacological activities, including cytostatic effect against various cancer cells. The nature and position of the substituents in the flavylium cation is [...] Read more.
Anthocyanidins, the aglycons of anthocyanins, are known, beyond their function in plants, also as compounds with a wide range of biological and pharmacological activities, including cytostatic effect against various cancer cells. The nature and position of the substituents in the flavylium cation is essential for such biological properties, as well as the equilibrium between the multistate of the different chemical species that are generated by the flavylium cation, including quinoidal base, hemiketal, and cis- and trans-chalcones. In this work, eight new flavylium derivatives were synthesized, characterized for confirmation of the structure by FT-IR and 2D-NMR, and investigated in vitro as possible cytostatic compounds against HCT116 and HepG2 cancer cells. The most active two compounds were explored for their halochromic properties that can influence the biological activity and subjected to molecular encapsulation in β-cyclodextrin derivatives in order to increase their solubility in water and bioavailability. The anticancer effect was influenced by the position (6-, 7-, or 8-) of the methoxy group in the β-ring of the methoxy-4′-hydroxy-3′-methoxyflavylium cation, while the study of the halochromic properties revealed the important role played by the chalcone species of the pH-dependent multistate in both the uncomplexed and inclusion complex forms of these anthocyanidins. Full article
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13 pages, 2378 KiB  
Article
Oxygen and Drug-Carrying Periodic Mesoporous Organosilicas for Enhanced Cell Viability under Normoxic and Hypoxic Conditions
by Ravi Kumar and Nermin Seda Kehr
Int. J. Mol. Sci. 2022, 23(8), 4365; https://doi.org/10.3390/ijms23084365 - 14 Apr 2022
Cited by 4 | Viewed by 2111
Abstract
Over the last decade, inorganic/organic hybrids have been exploited for oxygen-carrying materials and drug delivery. Its low-cost synthesis, controlled shape and size, and stability have made it a viable delivery strategy for therapeutic agents. Rutin (quercetin-3-O-rutinoside) is a bioflavonoid found in [...] Read more.
Over the last decade, inorganic/organic hybrids have been exploited for oxygen-carrying materials and drug delivery. Its low-cost synthesis, controlled shape and size, and stability have made it a viable delivery strategy for therapeutic agents. Rutin (quercetin-3-O-rutinoside) is a bioflavonoid found in fruits and vegetables. Rutin has a variety of pharmaceutical applications, but its low water solubility reduces its stability and bioavailability. As a result, we introduce a new and stable nanosystem for loading a low-soluble drug (rutin) into oxygen-carrying periodic mesoporous organosilicas (PMO-PFCs). Over the course of 14 days, this nanosystem provided a sustained oxygen level to the cells in both normoxic and hypoxic conditions. At different pH values, the drug release (rutin) profile is also observed. Furthermore, the rutin-coated PMO-PFCs interacted with both healthy and malignant cells. The healthy cells have better cell viability on the rutin-coated oxygen-carrying PMO-PFCs, while the malignant cells have a lower cell viability. Full article
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11 pages, 3968 KiB  
Article
Interaction of Aqueous Bovine Serum Albumin with Silica Aerogel Microparticles: Sorption Induced Aggregation
by Attila Forgács, Madalina Ranga, István Fábián and József Kalmár
Int. J. Mol. Sci. 2022, 23(5), 2816; https://doi.org/10.3390/ijms23052816 - 4 Mar 2022
Cited by 1 | Viewed by 2282
Abstract
Mesoporous silica aerogels have a wide range of potential applications in biotechnology, the food industry, pharmacy and medicine. Understanding the nature of the interactions of biomolecules with these porous nanostructured materials is essential for achieving optimum performance in the targeted applications. In this [...] Read more.
Mesoporous silica aerogels have a wide range of potential applications in biotechnology, the food industry, pharmacy and medicine. Understanding the nature of the interactions of biomolecules with these porous nanostructured materials is essential for achieving optimum performance in the targeted applications. In this study, the well-characterized bovine serum albumin (BSA) was chosen as a model protein to probe protein–aerogel interactions in the solution phase. Aqueous BSA was mixed with suspended silica aerogel microparticles, and the colloid system was monitored on-line by UV–vis spectrophotometry and turbidimetry. The global mathematical analysis of the time-resolved data reveals that the fast sorption of the protein on the aerogel microparticles follows a multistep binding mechanism. The extensive sorption of the protein eventually induces the aggregation of the covered aerogel due to the alteration of the electrical double layer of the particles. The interaction of BSA and silica aerogel is the strongest between pH = 4 and 5, because their native surface charges are the opposite in this pH range, as indicated by their respective zeta potentials. Full article
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