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16 pages, 339 KiB

Open AccessArticle

Relationship between the Polymer Blend Using Chitosan, Polyethylene Glycol, Polyvinyl Alcohol, Polyvinylpyrrolidone, and Antimicrobial Activities against Staphylococcus aureus

by Linh Doan and Khoa Tran

Pharmaceutics 2023, 15(10), 2453; https://doi.org/10.3390/pharmaceutics15102453 - 13 Oct 2023

Cited by 5 | Viewed by 1610

Abstract

The findings from Pareto charts, main effect plots, and interaction plots demonstrate the importance of polymer concentration. Increasing concentration improves the inhibition percentage and decreases the MIC₅₀. However, the primary factor that influences these changes is chitosan (CS). Additionally, the interaction [...] Read more.

The findings from Pareto charts, main effect plots, and interaction plots demonstrate the importance of polymer concentration. Increasing concentration improves the inhibition percentage and decreases the MIC₅₀. However, the primary factor that influences these changes is chitosan (CS). Additionally, the interaction between CS and PVP, along with other polymers, plays a crucial role in achieving better antimicrobial effects. These results enhance our understanding of the antimicrobial properties of the studied polymers and offer valuable insights for developing effective antimicrobial formulations. The MIC₅₀ value of M1–M16 was at a polymer percentage of 12.5%. At 12.5% polymer percentage, with the limits of [PVA], [PEG], and [PVP] being 0.002–0.004 g/mL and [CS] being 0.001–0.002 g/mL, using the 2-level full factorial method, the inhibition percentage is equal to 174.1 − 27,812 PVA − 18,561 PVP − 25,960 PEG − 38,752 CS + 9,263,047 PVA*PVP + 10,430,763 PVA*PEG + 15,397,157 PVA*CS + 7,088,313 PVP*PEG + 7,841,221 PVP*CS + 14,228,046 PEG*CS − 3,367,292,860 PVA*PVP*PEG − 5,671,998,721 PVA*PVP*CS − 6,619,041,275 PVA*PEG*CS − 3,917,095,529 PVP*PEG*CS + 2,273,661,969,470 PVA*PVP*PEG*CS. Theoretically, the most economical concentrations of PVA, PVP, PEG, and CS are 0.002, 0.002, 0.002, and 0.001 mg/mL at a concentration of 12.5% to reach an inhibition percentage of 99.162%, which coincides with the MBC value. Full article

(This article belongs to the Special Issue New Properties of Supramolecular Complexes and Drug Nanoparticles)

17 pages, 2490 KiB

Open AccessArticle

Radiothermal Emission of Nanoparticles with a Complex Shape as a Tool for the Quality Control of Pharmaceuticals Containing Biologically Active Nanoparticles

by Anton V. Syroeshkin, Gleb V. Petrov, Viktor V. Taranov, Tatiana V. Pleteneva, Alena M. Koldina, Ivan A. Gaydashev, Ekaterina S. Kolyabina, Daria A. Galkina, Ekaterina V. Sorokina, Elena V. Uspenskaya, Ilaha V. Kazimova, Mariya A. Morozova, Varvara V. Lebedeva, Stanislav A. Cherepushkin, Irina V. Tarabrina, Sergey A. Syroeshkin, Alexander V. Tertyshnikov and Tatiana V. Grebennikova

Pharmaceutics 2023, 15(3), 966; https://doi.org/10.3390/pharmaceutics15030966 - 16 Mar 2023

Cited by 5 | Viewed by 2327

Abstract

It has recently been shown that the titer of the SARS-CoV-2 virus decreases in a cell culture when the cell suspension is irradiated with electromagnetic waves at a frequency of 95 GHz. We assumed that a frequency range in the gigahertz and sub-terahertz [...] Read more.

It has recently been shown that the titer of the SARS-CoV-2 virus decreases in a cell culture when the cell suspension is irradiated with electromagnetic waves at a frequency of 95 GHz. We assumed that a frequency range in the gigahertz and sub-terahertz ranges was one of the key aspects in the “tuning” of flickering dipoles in the dispersion interaction process of the surfaces of supramolecular structures. To verify this assumption, the intrinsic thermal radio emission in the gigahertz range of the following nanoparticles was studied: virus-like particles (VLP) of SARS-CoV-2 and rotavirus A, monoclonal antibodies to various RBD epitopes of SARS-CoV-2, interferon-α, antibodies to interferon-γ, humic–fulvic acids, and silver proteinate. At 37 °C or when activated by light with λ = 412 nm, these particles all demonstrated an increased (by two orders of magnitude compared to the background) level of electromagnetic radiation in the microwave range. The thermal radio emission flux density specifically depended on the type of nanoparticles, their concentration, and the method of their activation. The thermal radio emission flux density was capable of reaching 20 μW/(m² sr). The thermal radio emission significantly exceeded the background only for nanoparticles with a complex surface shape (nonconvex polyhedra), while the thermal radio emission from spherical nanoparticles (latex spheres, serum albumin, and micelles) did not differ from the background. The spectral range of the emission apparently exceeded the frequencies of the Ka band (above 30 GHz). It was assumed that the complex shape of the nanoparticles contributed to the formation of temporary dipoles which, at a distance of up to 100 nm and due to the formation of an ultrahigh strength field, led to the formation of plasma-like surface regions that acted as emitters in the millimeter range. Such a mechanism makes it possible to explain many phenomena of the biological activity of nanoparticles, including the antibacterial properties of surfaces. Full article

(This article belongs to the Special Issue New Properties of Supramolecular Complexes and Drug Nanoparticles)

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14 pages, 1762 KiB

Open AccessCommunication

Supramolecular Organization in Salts of Riluzole with Dihydroxybenzoic Acids—The Key Role of the Mutual Arrangement of OH Groups

by Alexander P. Voronin, Artem O. Surov, Andrei V. Churakov and Mikhail V. Vener

Pharmaceutics 2023, 15(3), 878; https://doi.org/10.3390/pharmaceutics15030878 - 8 Mar 2023

Cited by 6 | Viewed by 1909

Abstract

Intermolecular interactions, in particular hydrogen bonds, play a key role in crystal engineering. The ability to form hydrogen bonds of various types and strengths causes competition between supramolecular synthons in pharmaceutical multicomponent crystals. In this work, we investigate the influence of positional isomerism [...] Read more.

Intermolecular interactions, in particular hydrogen bonds, play a key role in crystal engineering. The ability to form hydrogen bonds of various types and strengths causes competition between supramolecular synthons in pharmaceutical multicomponent crystals. In this work, we investigate the influence of positional isomerism on the packing arrangements and the network of hydrogen bonds in multicomponent crystals of the drug riluzole with hydroxyl derivatives of salicylic acid. The supramolecular organization of the riluzole salt containing 2,6-dihydroxybenzoic acid differs from that of the solid forms with 2,4- and 2,5-dihydroxybenzoic acids. Because the second OH group is not at position 6 in the latter crystals, intermolecular charge-assisted hydrogen bonds are formed. According to periodic DFT calculations, the enthalpy of these H-bonds exceeds 30 kJ·mol⁻¹. The positional isomerism appears to have little effect on the enthalpy of the primary supramolecular synthon (65–70 kJ·mol⁻¹), but it does result in the formation of a two-dimensional network of hydrogen bonds and an increase in the overall lattice energy. According to the results of the present study, 2,6-dihydroxybenzoic acid can be treated as a promising counterion for the design of pharmaceutical multicomponent crystals. Full article

(This article belongs to the Special Issue New Properties of Supramolecular Complexes and Drug Nanoparticles)

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21 pages, 13449 KiB

Open AccessArticle

pH-Responsible Doxorubicin-Loaded Fe₃O₄@CaCO₃ Nanocomposites for Cancer Treatment

by Victoriya Popova, Yuliya Poletaeva, Alexey Chubarov and Elena Dmitrienko

Pharmaceutics 2023, 15(3), 771; https://doi.org/10.3390/pharmaceutics15030771 - 26 Feb 2023

Cited by 13 | Viewed by 3764

Abstract

A magnetic nanocomposite (MNC) is an integrated nanoplatform that combines a set of functions of two types of materials. A successful combination can give rise to a completely new material with unique physical, chemical, and biological properties. The magnetic core of MNC provides [...] Read more.

A magnetic nanocomposite (MNC) is an integrated nanoplatform that combines a set of functions of two types of materials. A successful combination can give rise to a completely new material with unique physical, chemical, and biological properties. The magnetic core of MNC provides the possibility of magnetic resonance or magnetic particle imaging, magnetic field-influenced targeted delivery, hyperthermia, and other outstanding applications. Recently, MNC gained attention for external magnetic field-guided specific delivery to cancer tissue. Further, drug loading enhancement, construction stability, and biocompatibility improvement may lead to high progress in the area. Herein, the novel method for nanoscale Fe₃O₄@CaCO₃ composites synthesis was proposed. For the procedure, oleic acid-modified Fe₃O₄ nanoparticles were coated with porous CaCO₃ using an ion coprecipitation technique. PEG-2000, Tween 20, and DMEM cell media was successfully used as a stabilization agent and template for Fe₃O₄@CaCO₃ synthesis. Transmission electron microscopy (TEM), Fourier transform infrared (FTIR) spectroscopy, and dynamic light scattering (DLS) data were used for the Fe₃O₄@CaCO₃ MNC’s characterization. To improve the nanocomposite properties, the concentration of the magnetic core was varied, yielding optimal size, polydispersity, and aggregation ability. The resulting Fe₃O₄@CaCO₃ had a size of 135 nm with narrow size distributions, which is suitable for biomedical applications. The stability experiment in various pH, cell media, and fetal bovine serum was also evaluated. The material showed low cytotoxicity and high biocompatibility. An excellent anticancer drug doxorubicin (DOX) loading of up to 1900 µg/mg (DOX/MNC) was demonstrated. The Fe₃O₄@CaCO₃/DOX displayed high stability at neutral pH and efficient acid-responsive drug release. The series of DOX-loaded Fe₃O₄@CaCO₃ MNCs indicated effective inhibition of Hela and MCF-7 cell lines, and the IC 50 values were calculated. Moreover, 1.5 μg of the DOX-loaded Fe₃O₄@CaCO₃ nanocomposite is sufficient to inhibit 50% of Hela cells, which shows a high prospect for cancer treatment. The stability experiments for DOX-loaded Fe₃O₄@CaCO₃ in human serum albumin solution indicated the drug release due to the formation of a protein corona. The presented experiment showed the “pitfalls” of DOX-loaded nanocomposites and provided step-by-step guidance on efficient, smart, anticancer nanoconstruction fabrication. Thus, the Fe₃O₄@CaCO₃ nanoplatform exhibits good performance in the cancer treatment area. Full article

(This article belongs to the Special Issue New Properties of Supramolecular Complexes and Drug Nanoparticles)

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12 pages, 3088 KiB

Open AccessArticle

Toward Pathogenic Biofilm Suppressors: Synthesis of Amino Derivatives of Pillar[5]arene and Supramolecular Assembly with DNA

by Yulia I. Aleksandrova, Dmitriy N. Shurpik, Viktoriya A. Nazmutdinova, Olga A. Mostovaya, Evgenia V. Subakaeva, Evgenia A. Sokolova, Pavel V. Zelenikhin and Ivan I. Stoikov

Pharmaceutics 2023, 15(2), 476; https://doi.org/10.3390/pharmaceutics15020476 - 31 Jan 2023

Cited by 6 | Viewed by 2116

Abstract

New amino derivatives of pillar[5]arene were obtained in three stages with good yields. It was shown that pillar[5]arene containing thiaether and tertiary amino groups formed supramolecular complexes with low molecular weight model DNA. Pillar[5]arene formed complexes with a DNA nucleotide pair at a [...] Read more.

New amino derivatives of pillar[5]arene were obtained in three stages with good yields. It was shown that pillar[5]arene containing thiaether and tertiary amino groups formed supramolecular complexes with low molecular weight model DNA. Pillar[5]arene formed complexes with a DNA nucleotide pair at a ratio of 1:2 (macrocycle/DNA base pairs), as demonstrated by UV-visible and fluorescence spectroscopy. The association constants of pillar[5]arene with DNA were lgKass1:1 = 2.38 and lgKass1:2 = 5.07, accordingly. By using dynamic light scattering and transmission electron microscopy, it was established that the interaction of pillar[5]arene containing thiaether and tertiary amino groups (concentration of 10−5 M) with a model nucleic acid led to the formation of stable nanosized macrocycle/DNA associates with an average particle size of 220 nm. It was shown that the obtained compounds did not exhibit a pronounced toxicity toward human adenocarcinoma cells (A549) and bovine lung epithelial cells (LECs). The hypothesis about a possible usage of the synthesized macrocycle for the aggregation of extracellular bacterial DNA in a biofilm matrix was confirmed by the example of St. Aureus. It was found that pillar[5]arene at a concentration of 10⁻⁵ M was able to reduce the thickness of the St. Aureus biofilm by 15%. Full article

(This article belongs to the Special Issue New Properties of Supramolecular Complexes and Drug Nanoparticles)

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27 pages, 7861 KiB

Open AccessArticle

Selenium Nanoparticles Can Influence the Immune Response Due to Interactions with Antibodies and Modulation of the Physiological State of Granulocytes

by Venera V. Khabatova, Dmitriy A. Serov, Irina V. Tikhonova, Maxim E. Astashev, Egor I. Nagaev, Ruslan M. Sarimov, Tatiana A. Matveyeva, Alexander V. Simakin and Sergey V. Gudkov

Pharmaceutics 2022, 14(12), 2772; https://doi.org/10.3390/pharmaceutics14122772 - 11 Dec 2022

Cited by 6 | Viewed by 2344

Abstract

Currently, selenium nanoparticles (SeNPs) are considered potential immunomodulatory agents and as targets for activity modulation are granulocytes, which have the most abundant population of immune blood cells. The present study aims to evaluate the cytotoxic effect and its effect on the functional responses [...] Read more.

Currently, selenium nanoparticles (SeNPs) are considered potential immunomodulatory agents and as targets for activity modulation are granulocytes, which have the most abundant population of immune blood cells. The present study aims to evaluate the cytotoxic effect and its effect on the functional responses of granulocytes. In addition to the intrinsic activity of SeNPs, we studied the activity of the combination of SeNPs and IgG antibodies. Using laser ablation and fragmentation, we obtained nanoparticles with an average size of 100 nm and a rather narrow size evolution. The resulting nanoparticles do not show acute toxicity to primary cultures of fibroblasts and hepatocytes, epithelial-like cell line L-929 and granulocyte-like culture of HL-60 at a concentration of 10⁹ NPs/mL. SeNPs at a concentration of 10¹⁰ NPs/mL reduced the viability of HL-60 cells by no more than 10% and did not affect the viability of the primary culture of mouse granulocytes, and did not have a genotoxic effect on progenitor cells. The addition of SeNPs can affect the production of reactive oxygen species (ROS) by mouse bone marrow granulocytes, modulate the proportion of granulocytes with calcium spikes and enhance fMLF-induced granulocytes degranulation. SeNPs can modulate the effect of IgG on the physiological responses of granulocytes. We studied the expression level of genes associated with inflammation and cell stress. SeNPs increase the expression of catalase, NF-κB, Xrcc5 and some others; antibodies enhance the effect of SeNPs, but IgG without SeNPs decreases the expression level of these genes. This fact can be explained by the interaction between SeNPs and IgG. It has been established that antibodies interact with SeNPs. We showed that antibodies bind to the surface of selenium nanoparticles and are present in aqueous solutions in a bound form from DLS methods, ultraviolet–visible spectroscopy, vibrational–rotational spectrometry, fluorescence spectrometry, and refractometry. At the same time, in a significant part of the antibodies, a partial change in the tertiary and secondary structure is observed. The data obtained will allow a better understanding of the principles of the interaction of immune cells with antibodies and SeNPs and, in the future, may serve to create a new generation of immunomodulators. Full article

(This article belongs to the Special Issue New Properties of Supramolecular Complexes and Drug Nanoparticles)

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23 pages, 4876 KiB

Open AccessArticle

Cytoprotective Properties of a New Nanocomplex of Selenium with Taxifolin in the Cells of the Cerebral Cortex Exposed to Ischemia/Reoxygenation

by Elena G. Varlamova, Venera V. Khabatova, Sergey V. Gudkov, Egor Y. Plotnikov and Egor A. Turovsky

Pharmaceutics 2022, 14(11), 2477; https://doi.org/10.3390/pharmaceutics14112477 - 16 Nov 2022

Cited by 17 | Viewed by 1941

Abstract

The neuroprotective effect of the natural antioxidant taxifolin (TAX) is well known for ischemic pathologies. However, the limitations of taxifolin application are described—poor solubility, low ability to penetrate the blood–brain barrier, and side effects from high doses for stroke therapy. We proposed the [...] Read more.

The neuroprotective effect of the natural antioxidant taxifolin (TAX) is well known for ischemic pathologies. However, the limitations of taxifolin application are described—poor solubility, low ability to penetrate the blood–brain barrier, and side effects from high doses for stroke therapy. We proposed the problem of targeted delivery of taxifolin and achievement effective concentrations could be solved by developing a nanocomplex of selenium nanoparticles (SeNPs) with taxifolin (Se–TAX). In this study, we developed a selenium–taxifolin nanocomplex based on selenium nanoparticles with a 100 nm size. It was shown that TAX, SeNPs, and Se–TAX were all able to suppress the production of ROS in neurons and astrocytes under exposure to exogenous H₂O₂ and ischemia-like conditions. However, the Se–TAX nanocomplex appeared to be the most effective, displaying a lower working concentration range and negligible pro-oxidant effect compared with pure SeNPs. The mechanism of Se–TAX beneficial effects involved the activation of some antioxidant enzymes and the suppression of ROS-generating systems during OGD/reoxygenation, while TAX and “naked” SeNPs were less effective in regulating the cellular redox status. Naked SeNPs inhibited a global increase in Ca²⁺ ions in cytosol, but not OGD-induced hyperexcitation of the neuroglial network, while Se–TAX suppressed both [Ca²⁺]i rise and hyperexcitation. The effect of TAX at similar doses appeared exclusively in inhibiting OGD-induced hyperexcitation. Analysis of necrosis and apoptosis after OGD/reoxygenation revealed the highest efficiency of the Se–TAX nanocomplex as well. Se–TAX suppressed the expression of proinflammatory and proapoptotic proteins with simultaneous activation of protective genes. We conclude that the Se–TAX nanocomplex combines the antioxidative features taxifolin and the antiapoptotic effect of nanoselenium, involving the regulation of Ca²⁺ dynamics. Full article

(This article belongs to the Special Issue New Properties of Supramolecular Complexes and Drug Nanoparticles)

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15 pages, 3022 KiB

Open AccessArticle

Second-Order Scattering Quenching in Fluorescence Spectra of Natural Humates as a Tracer of Formation Stable Supramolecular System for the Delivery of Poorly Soluble Antiviral Drugs on the Example of Mangiferin and Favipiravir

by Mariya A. Morozova, Vladimir N. Tumasov, Ilaha V. Kazimova, Tatiana V. Maksimova, Elena V. Uspenskaya and Anton V. Syroeshkin

Pharmaceutics 2022, 14(4), 767; https://doi.org/10.3390/pharmaceutics14040767 - 31 Mar 2022

Cited by 5 | Viewed by 2438

Abstract

In the present work, the methods of dynamic light scattering and fluorescence spectroscopy were applied to study the optical properties of aqueous dilutions of the humic substances complex (HC) as a potential drug delivery system. The supramolecular structures in the humate solution were [...] Read more.

In the present work, the methods of dynamic light scattering and fluorescence spectroscopy were applied to study the optical properties of aqueous dilutions of the humic substances complex (HC) as a potential drug delivery system. The supramolecular structures in the humate solution were characterized as monodisperse systems of the submicron range with a tendency to decrease in particle size with a decrease in the dry matter concentration. The slightly alkaline medium (8.3) of the studied aqueous dilutions of HC causes the absence of a pronounced fluorescence maximum in the region from 400 to 500 nm. However, the presence of an analytically significant, inversely proportional to the concentration second-order scattering (SOS) signal at 2λ_ex = λ_em was shown. In the examples of the antiviral substances mangiferin and favipiravir, it was shown that the use of the humic complex as a drug carrier makes it possible to increase the solubility by several times and simultaneously obtain a system with a smaller particle size of the dispersed phase. It has been shown that HC can interact with mangiferin and favipiravir to form stable structures, which lead to a significant decrease in SOS intensities on HC SOS spectra. The scattering wavelengths, λ_ex/λ_em, were registered at 350 nm/750 nm for mangiferin and 365 nm/730 nm for favipiravir, respectively. The increments of the scattering intensities (I0/I) turned out to be proportional to the concentration of antiviral components in a certain range of concentrations. Full article

(This article belongs to the Special Issue New Properties of Supramolecular Complexes and Drug Nanoparticles)

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13 pages, 1784 KiB

Open AccessArticle

Optical Properties of Crystalline Lactose Fluidized with Dilutions of Various Substances in the Terahertz Frequency Range

by Anna Baranova, Anastasiya Lykina, Daria Antonova and Olga Smolyanskaya

Pharmaceutics 2022, 14(1), 32; https://doi.org/10.3390/pharmaceutics14010032 - 24 Dec 2021

Cited by 8 | Viewed by 2974

Abstract

Lactose is a commonly used component of pharmaceutical medications in tablet form. It was previously shown that lactose changes conformationally after saturation in fluidized beds with active pharmaceutical ingredients obtained by repeated dilution of antibodies to interferon-gamma in combination with an external intensive [...] Read more.

Lactose is a commonly used component of pharmaceutical medications in tablet form. It was previously shown that lactose changes conformationally after saturation in fluidized beds with active pharmaceutical ingredients obtained by repeated dilution of antibodies to interferon-gamma in combination with an external intensive vibration treatment. Moreover, it was revealed that these solutions are self-organized dispersed systems in which nano-objects are formed. Their biological activity and mechanism of action were previously established as well. The current work was dedicated to investigating the optical properties of fluidized lactose powders in the terahertz frequency range. Spectral analyses of powders of crystalline lactose saturated in fluidized beds with a diluted solution of either glycine buffer, antibodies to interferon-gamma, or water were carried out, intact lactose served as a control. All powders were tableted before testing. In the course of the study, the macroscopic parameters of the tablets were established, at which they had a stable shape and their THz optical properties had no parasitic diffraction losses. These tablets were analyzed using terahertz time-domain spectroscopy in the frequency range of 0.2–2.6 THz. The differentiation between the spectra was conducted using a principal component analysis. The differences between intact lactose and the lactose saturated with any of studied solutions were demonstrated. Additionally, lactose saturated with solutions of multiple dilutions of a substance (antibodies or glycine buffer) differed not only from intact lactose, but also from lactose saturated with a diluted solution of water. Moreover, discrimination of lactose formulations saturated with different substances (antibodies or glycine buffer) was also possible. Additionally, intact lactose differed from lactose saturated with diluted water. The methods reported could be useful for the quality control of the medications based on the technology of repeated dilution of an original substance. Full article

(This article belongs to the Special Issue New Properties of Supramolecular Complexes and Drug Nanoparticles)

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20 pages, 3567 KiB

Open AccessArticle

Nanodispersions of Polyelectrolytes Based on Humic Substances: Isolation, Physico-Chemical Characterization and Evaluation of Biological Activity

by Elena V. Uspenskaya, Anton V. Syroeshkin, Tatiana V. Pleteneva, Ilaha V. Kazimova, Tatiana V. Grebennikova, Irina T. Fedyakina, Varvara V. Lebedeva, Oleg E. Latyshev, Olesia V. Eliseeva, Viktor F. Larichev, Timur M. Garaev, Tatiana V. Maximova, Mariya A. Morozova and Pham My Hanh

Pharmaceutics 2021, 13(11), 1954; https://doi.org/10.3390/pharmaceutics13111954 - 18 Nov 2021

Cited by 7 | Viewed by 3361

Abstract

Natural polyelectrolytes, including in the form of complexes with colloidal particles, are increasingly used in pharmacy due to the possibility of regulated attachment of medicinal substances and their targeted delivery to the target organ. However, the formation, stability, and molecular-mass characteristics of polyelectrolyte [...] Read more.

Natural polyelectrolytes, including in the form of complexes with colloidal particles, are increasingly used in pharmacy due to the possibility of regulated attachment of medicinal substances and their targeted delivery to the target organ. However, the formation, stability, and molecular-mass characteristics of polyelectrolyte nanodispersions (ND) vary depending on the nature and composition of the medium of their origin. This is due to the lack of standardized approaches to quality control and regulatory documentation for most natural ND. In this paper, we first introduced the isolation, followed by investigations into their physico-chemical properties and bioactivity. Using the dried droplet method, we were able to detect the “coffee ring effect”. Fractographic studies of the surface structure of EHA and FA dried samples using SEM showed its heterogeneity and the presence of submicron particles encapsulated in the internal molecular cavities of polyelectrolyte. FTIR spectroscopy revealed the ND chemical structure of benzo-α-pyron and benzo-γ-pyron, consisting of nanoparticles and a branched frame part. The main elements detected by X-ray fluorescence in humic substance extract and fulvic acid include Si, P, S, K, Ca, Mn, Fe, Cu, Zn, whereas Fe is in high concentrations. The UV-spectra and fluorescent radiation demonstrated the possibility of studying the effect of the fulvate chromone structure on its optical properties. It is shown that dilution of the initial solutions of polyelectrolytes 1:10 contributes to the detection of smaller nanoparticles and an increase in the absolute value of the negative ζ-potential as a factor of ND stability. A study of the EHS effect on the SARS-CoV-2 virus infectious titer in the Vero E6 cell showed the effective against virus both in the virucidal scheme (the SI is 11.90–22.43) and treatment/prevention scheme (the SI is 34.85–57.33). We assume that polyelectrolyte ND prevent the binding of the coronavirus spike glycoprotein to the receptor. Taking into account the results obtained, we expect that the developed approach can become unified for the standardization of the ND natural polyelectrolytes complex, which has great prospects for use in pharmacy and medicine as a drug with antiviral activity. Full article

(This article belongs to the Special Issue New Properties of Supramolecular Complexes and Drug Nanoparticles)

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17 pages, 3642 KiB

Open AccessArticle

New Antifungal Compound: Impact of Cosolvency, Micellization and Complexation on Solubility and Permeability Processes

by Tatyana V. Volkova, Olga R. Simonova and German L. Perlovich

Pharmaceutics 2021, 13(11), 1865; https://doi.org/10.3390/pharmaceutics13111865 - 4 Nov 2021

Cited by 9 | Viewed by 2147

Abstract

Poor solubility of new antifungal of 1,2,4-triazole class (S-119)—a structural analogue of fluconazole in aqueous media was estimated. The solubility improvement using different excipients: biopolymers (PEGs, PVP), surfactants (Brij S20, pluronic F-127) and cyclodextrins (α-CD, β-CD, 2-HP-β-CD, 6-O-Maltosyl-β-CD) was assessed in buffer solutions [...] Read more.

Poor solubility of new antifungal of 1,2,4-triazole class (S-119)—a structural analogue of fluconazole in aqueous media was estimated. The solubility improvement using different excipients: biopolymers (PEGs, PVP), surfactants (Brij S20, pluronic F-127) and cyclodextrins (α-CD, β-CD, 2-HP-β-CD, 6-O-Maltosyl-β-CD) was assessed in buffer solutions pH 2.0 and pH 7.4. Additionally, 2-HP-β-CD and 6-O-Maltosyl-β-CD were proposed as promising solubilizers for S-119. According to the solubilization capacity and micelle/water partition coefficients in buffer pH 7.4 pluronic F-127 was shown to improve S-119 solubility better than Brij S20. Among biopolymers, the greatest increase in solubility was shown in PVP solutions (pH 7.4) at concentrations above 4 w/v%. Complex analysis of the driving forces of solubilization, micellization and complexation processes matched the solubility results and suggested pluronic F-127 and 6-O-Maltosyl-β-CD as the most effective solubilizing agents for S-119. The comparison of S-119 diffusion through the cellulose membrane and lipophilic PermeaPad barrier revealed a considerable effect of the lipid layer on the decrease in the permeability coefficient. According to the PermeaPad, S-119 was classified as a highly permeated substance. The addition of 1.5 w/v% CDs in donor solution moves it to low-medium permeability class. Full article

(This article belongs to the Special Issue New Properties of Supramolecular Complexes and Drug Nanoparticles)

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13 pages, 777 KiB

Open AccessArticle

Antibodies Processed Using High Dilution Technology Distantly Change Structural Properties of IFNγ Aqueous Solution

by Nikita Penkov

Pharmaceutics 2021, 13(11), 1864; https://doi.org/10.3390/pharmaceutics13111864 - 4 Nov 2021

Cited by 21 | Viewed by 2253

Abstract

Terahertz spectroscopy allows for the analysis of vibrations corresponding to the large-scale structural movements and collective dynamics of hydrogen-bonded water molecules. Previously, differences had been detected in the emission spectra of interferon-gamma (IFNγ) solutions surrounded by extremely diluted solutions of either IFNγ or [...] Read more.

Terahertz spectroscopy allows for the analysis of vibrations corresponding to the large-scale structural movements and collective dynamics of hydrogen-bonded water molecules. Previously, differences had been detected in the emission spectra of interferon-gamma (IFNγ) solutions surrounded by extremely diluted solutions of either IFNγ or antibodies to IFNγ without direct contact compared to a control. Here we aimed to analyse the structural properties of water in a sample of an aqueous solution of IFNγ via terahertz time-domain spectroscopy (THz-TDS). Tubes with the IFNγ solution were immersed in fluidised lactose saturated with test samples (dilutions of antibodies to IFNγ or control) and incubated at 37 °C for 1, 1.5–2, 2.5–3, or 3.5–4 h. Fluidised lactose was chosen since it is an excipient in the manufacture of drugs based on diluted antibodies to IFNγ. After incubation, spectra were recorded within a wavenumber range of 10 to 110 cm⁻¹ with a resolution of 4 cm⁻¹. Lactose saturated with dilutions of antibodies to IFNγ (incubated for more than 2.5 h) changed the structural properties of an IFNγ aqueous solution without direct contact compared to the control. Terahertz spectra revealed stronger intermolecular hydrogen bonds and an increase in the relaxation time of free and weakly bound water molecules. The methodology developed on the basis of THz-TDS could potentially be applied to quality control of pharmaceuticals based on extremely diluted antibodies. Full article

(This article belongs to the Special Issue New Properties of Supramolecular Complexes and Drug Nanoparticles)

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Review

Jump to: Research

16 pages, 5202 KiB

Open AccessReview

Recent Update Roles of Magnetic Nanoparticles in Circulating Tumor Cell (CTC)/Non-CTC Separation

by Chawapon Pipatwatcharadate, Poornima Ramesh Iyer and Dakrong Pissuwan

Pharmaceutics 2023, 15(10), 2482; https://doi.org/10.3390/pharmaceutics15102482 - 17 Oct 2023

Cited by 6 | Viewed by 2324

Abstract

Metastasis of cancer is a major cause of death worldwide. Circulating tumor cells (CTCs) are important in the metastatic process of cancer. CTCs are able to circulate in the bloodstream. Therefore, they can be used as biomarkers of metastasis. However, CTCs are rare [...] Read more.

Metastasis of cancer is a major cause of death worldwide. Circulating tumor cells (CTCs) are important in the metastatic process of cancer. CTCs are able to circulate in the bloodstream. Therefore, they can be used as biomarkers of metastasis. However, CTCs are rare when compared to a large number of blood cells in the blood. Many CTC detection methods have been developed to increase CTC detection efficiency. Magnetic nanoparticles (MNPs) have attracted immense attention owing to their potential medical applications. They are particularly appealing as a tool for cell separation. Because of their unique properties, MNPs are of considerable interest for the enrichment of CTCs through CTC or non-CTC separation. Herein, we review recent developments in the application of MNPs to separate CTCs or non-CTCs in samples containing CTCs. This review provides information on new approaches that can be used to detect CTCs in blood samples. The combination of MNPs with other particles for magnetic-based cell separation for CTC detection is discussed. Furthermore, different approaches for synthesizing MNPs are included in this review. Full article

(This article belongs to the Special Issue New Properties of Supramolecular Complexes and Drug Nanoparticles)

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14 pages, 1637 KiB

Open AccessReview

Lipophosphonoxins—A Novel Group of Broad Spectrum Antibacterial Compounds

by Viktor Šebek, Pavel Anzenbacher, Dominik Rejman, Alena Špičáková and Milan Kolář

Pharmaceutics 2023, 15(10), 2395; https://doi.org/10.3390/pharmaceutics15102395 - 28 Sep 2023

Viewed by 1551

Abstract

Lipophosphonoxins (LPPOs) represent a new group of membrane-targeting antibiotics. Three generations of LPPOs have been described: First-generation LPPOs, second-generation LPPOs, and LEGO-LPPOs. All three generations have a similar mode of bactericidal action of targeting and disrupting the bacterial cytoplasmic membrane of prokaryotic cells, [...] Read more.

Lipophosphonoxins (LPPOs) represent a new group of membrane-targeting antibiotics. Three generations of LPPOs have been described: First-generation LPPOs, second-generation LPPOs, and LEGO-LPPOs. All three generations have a similar mode of bactericidal action of targeting and disrupting the bacterial cytoplasmic membrane of prokaryotic cells, with limited effect on eukaryotic cells. First-generation LPPOs showed excellent bactericidal activity against Gram-positive species, including multiresistant strains. Second-generation LPPOs broaden the antibiotic effect also against Gram-negative bacteria. However, both first- and second-generation LPPOs lose their antibacterial activity in the presence of serum albumin. LEGO-LPPOs were found to be active against both Gram-positive and Gram-negative bacteria, have better selectivity as compared to first- and second-generation resistance to LEGO-LPPOs was also not observed, and are active even in the presence of serum albumin. Second-generation LPPOs have been studied as antimicrobial additives in bone cement and as nanofiber dressing components in the treatment of wound infections in mice. Second-generation LPPOs and LEGO-LPPOs were also tested to treat ex vivo simulated endodontic infections in dental root canals. The results of all these studies were encouraging and suggested further investigation of LPPOs in these indications. This paper aims to review and compile published data on LPPOs. Full article

(This article belongs to the Special Issue New Properties of Supramolecular Complexes and Drug Nanoparticles)

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28 pages, 9979 KiB

Open AccessReview

Advancements in the Application of the Fenton Reaction in the Cancer Microenvironment

by Rile Ou, Gerile Aodeng and Jun Ai

Pharmaceutics 2023, 15(9), 2337; https://doi.org/10.3390/pharmaceutics15092337 - 18 Sep 2023

Cited by 6 | Viewed by 2306

Abstract

Cancer is a complex and multifaceted disease that continues to be a global health challenge. It exerts a tremendous burden on individuals, families, healthcare systems, and society as a whole. To mitigate the impact of cancer, concerted efforts and collaboration on a global [...] Read more.

Cancer is a complex and multifaceted disease that continues to be a global health challenge. It exerts a tremendous burden on individuals, families, healthcare systems, and society as a whole. To mitigate the impact of cancer, concerted efforts and collaboration on a global scale are essential. This includes strengthening preventive measures, promoting early detection, and advancing effective treatment strategies. In the field of cancer treatment, researchers and clinicians are constantly seeking new approaches and technologies to improve therapeutic outcomes and minimize adverse effects. One promising avenue of investigation is the utilization of the Fenton reaction, a chemical process that involves the generation of highly reactive hydroxyl radicals (·OH) through the interaction of hydrogen peroxide (H₂O₂) with ferrous ions (Fe²⁺). The generated ·OH radicals possess strong oxidative properties, which can lead to the selective destruction of cancer cells. In recent years, researchers have successfully introduced the Fenton reaction into the cancer microenvironment through the application of nanotechnology, such as polymer nanoparticles and light-responsive nanoparticles. This article reviews the progress of the application of the Fenton reaction, catalyzed by polymer nanoparticles and light-responsive nanoparticles, in the cancer microenvironment, as well as the potential applications and future development directions of the Fenton reaction in the field of tumor treatment. Full article

(This article belongs to the Special Issue New Properties of Supramolecular Complexes and Drug Nanoparticles)

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103 pages, 45843 KiB

Open AccessReview

Comprehensive Insights into Medicinal Research on Imidazole-Based Supramolecular Complexes

by Shu-Rui Li, Yi-Min Tan, Ling Zhang and Cheng-He Zhou

Pharmaceutics 2023, 15(5), 1348; https://doi.org/10.3390/pharmaceutics15051348 - 27 Apr 2023

Cited by 30 | Viewed by 3773

Abstract

The electron-rich five-membered aromatic aza-heterocyclic imidazole, which contains two nitrogen atoms, is an important functional fragment widely present in a large number of biomolecules and medicinal drugs; its unique structure is beneficial to easily bind with various inorganic or organic ions and molecules [...] Read more.

The electron-rich five-membered aromatic aza-heterocyclic imidazole, which contains two nitrogen atoms, is an important functional fragment widely present in a large number of biomolecules and medicinal drugs; its unique structure is beneficial to easily bind with various inorganic or organic ions and molecules through noncovalent interactions to form a variety of supramolecular complexes with broad medicinal potential, which is being paid an increasing amount of attention regarding more and more contributions to imidazole-based supramolecular complexes for possible medicinal application. This work gives systematical and comprehensive insights into medicinal research on imidazole-based supramolecular complexes, including anticancer, antibacterial, antifungal, antiparasitic, antidiabetic, antihypertensive, and anti-inflammatory aspects as well as ion receptors, imaging agents, and pathologic probes. The new trend of the foreseeable research in the near future toward imidazole-based supramolecular medicinal chemistry is also prospected. It is hoped that this work provides beneficial help for the rational design of imidazole-based drug molecules and supramolecular medicinal agents and more effective diagnostic agents and pathological probes. Full article

(This article belongs to the Special Issue New Properties of Supramolecular Complexes and Drug Nanoparticles)

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60 pages, 7335 KiB

Open AccessReview

Dual-Drug Delivery by Anisotropic and Uniform Hybrid Nanostructures: A Comparative Study of the Function and Substrate–Drug Interaction Properties

by Delaram Kargari Aghmiouni and Sepideh Khoee

Pharmaceutics 2023, 15(4), 1214; https://doi.org/10.3390/pharmaceutics15041214 - 11 Apr 2023

Cited by 8 | Viewed by 2645

Abstract

By utilizing nanoparticles to upload and interact with several pharmaceuticals in varying methods, the primary obstacles associated with loading two or more medications or cargos with different characteristics may be addressed. Therefore, it is feasible to evaluate the benefits provided by co-delivery systems [...] Read more.

By utilizing nanoparticles to upload and interact with several pharmaceuticals in varying methods, the primary obstacles associated with loading two or more medications or cargos with different characteristics may be addressed. Therefore, it is feasible to evaluate the benefits provided by co-delivery systems utilizing nanoparticles by investigating the properties and functions of the commonly used structures, such as multi- or simultaneous-stage controlled release, synergic effect, enhanced targetability, and internalization. However, due to the unique surface or core features of each hybrid design, the eventual drug–carrier interactions, release, and penetration processes may vary. Our review article focused on the drug’s loading, binding interactions, release, physiochemical, and surface functionalization features, as well as the varying internalization and cytotoxicity of each structure that may aid in the selection of an appropriate design. This was achieved by comparing the actions of uniform-surfaced hybrid particles (such as core–shell particles) to those of anisotropic, asymmetrical hybrid particles (such as Janus, multicompartment, or patchy particles). Information is provided on the use of homogeneous or heterogeneous particles with specified characteristics for the simultaneous delivery of various cargos, possibly enhancing the efficacy of treatment techniques for illnesses such as cancer. Full article

(This article belongs to the Special Issue New Properties of Supramolecular Complexes and Drug Nanoparticles)

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