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The Emerging Role of Polymeric Materials in Pharmaceutical Designs and Applications

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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 (20 January 2023) | Viewed by 19739

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Special Issue Editors

Dr. Silvia Vasiliu

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Guest Editor

“Petru Poni” Institute of Macromolecular Chemistry, Grigore Ghica Voda Alley, No. 41 A, 700487 Iasi, Romania
Interests: graft polymerization; n-vinylimidazole; gellan gum; betaine structure; nanoparticles; smart polymers; dental applications
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Dr. Marcela Mihai

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Guest Editor

Petru Poni Institute of Macromolecular Chemistry, 41A Grigore Ghica Voda Alley, 700487 Iasi, Romania
Interests: complex multicomponent systems; natural and synthetic polymers; functional polymers; functionalization of polymers; nanostructures; hybrids; electrostatic self-assembly
Special Issues, Collections and Topics in MDPI journals

Special Issue Information

Dear Colleagues,

Today, polymeric materials based on a wide range of natural and synthetic macromolecules occupy an essential role in every field of human activities. Pharmaceutically, polymeric materials represent an important tool in the development of packaging and drug delivery systems, as well as in the manufacture of disposable devices, such as syringes, bags, bottle, filters, membranes, inhalers, and tubes. Thus, several techniques have been developed to manufacture disposable devices: sintering, spinning, extrusion, and injection molding. At the same time, research in the field of drug delivery systems has been directed toward the development of new strategies to increase/optimize the release of drugs at the target site so as to obtain an increased/optimal bioavailability of the therapeutic agent. The role of polymeric material is to protect the bioactive principle from physiological environment, to control the release of drugs, to enhance drug stability, and to improve drug bioavailability, acting as a taste masking agent, binder in tablets, film-coating agent, protective and stabilizing agent, or rheological modifier. Additionally, the technologies offer the possibility to fabricate drug delivery systems in various forms that include tablets, pills, patches, tapes, films, injectable solutions, semisolids, and powders. This Special Issue is focused on the role of polymeric materials in pharmaceutical dosages as well as their applications in the pharmaceutical field. As the proposed topic is a remarkably interesting one, we invite you and your research team to submit research or review articles to the Special Issue entitled “The Emerging Role of Polymeric Materials in Pharmaceutical Designs and Applications” that will be published in the International Journal of Molecular Science.

Dr. Silvia Vasiliu
Dr. Marcela Mihai
Guest Editors

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Keywords

Taste masking
Excipients
Drug delivery systems
Rheological modifiers
Tablets
Patches
Films
Disposable devices

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Published Papers (9 papers)

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Research

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22 pages, 3666 KiB

Open AccessArticle

Design of Dyes Based on the Quinoline or Quinoxaline Skeleton towards Visible Light Photoinitiators

by Ilona Pyszka and Beata Jędrzejewska

Int. J. Mol. Sci. 2024, 25(8), 4289; https://doi.org/10.3390/ijms25084289 - 12 Apr 2024

Cited by 1 | Viewed by 868

Abstract

Dyes based on quinoline and quinoxaline skeletons were designed for application as visible light photoinitiators. The obtained compounds absorb electromagnetic radiation on the border between ultraviolet and visible light, which allows the use of dental lamps as light sources during the initiation of the photopolymerization reaction. Their another desirable feature is the ability to create a long-lived excited state, which enables the chain reaction to proceed through the mechanism of intermolecular electron transfer. In two-component photoinitiating systems, in the presence of an electron donor or a hydrogen atom donor, the synthesized compounds show excellent abilities to photoinitiate the polymerization of acrylates. In control tests, the efficiency of photopolymerization using modified quinoline and quinoxaline derivatives is comparable to that obtained using a typical, commercial photoinitiator for dentistry, camphorquinone. Moreover, the use of the tested compounds requires a small amount of photoinitiator (only 0.04% by weight) to initiate the reaction. The research also showed a significant acceleration of the photopolymerization process and shortening of the reaction time. In practice, this means that the new two-component initiating systems can be used in much lower concentrations without slowing down the speed of obtaining polymer materials. It is worth emphasizing that these two features of the new initiating system allow for cost reduction by reducing financial outlays on both materials (photoinitiators) and electricity. Full article

(This article belongs to the Special Issue The Emerging Role of Polymeric Materials in Pharmaceutical Designs and Applications)

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21 pages, 2964 KiB

Open AccessArticle

Antitumor Activity of PEGylated and TEGylated Phenothiazine Derivatives: Structure–Activity Relationship

by Sandu Cibotaru, Andreea-Isabela Sandu, Alina Nicolescu and Luminita Marin

Int. J. Mol. Sci. 2023, 24(6), 5449; https://doi.org/10.3390/ijms24065449 - 13 Mar 2023

Cited by 3 | Viewed by 1805

Abstract

The paper aims to investigate the antitumor activity of a series of phenothiazine derivatives in order to establish a structure–antitumor activity relationship. To this end, PEGylated and TEGylated phenothiazine have been functionalized with formyl units and further with sulfonamide units via dynamic imine bonds. Their antitumor activity was monitored in vitro against seven human tumors cell lines and a mouse one compared to a human normal cell line by MTS assay. In order to find the potential influence of different building blocks on antitumor activity, the antioxidant activity, the ability to inhibit farnesyltransferase and the capacity to bind amino acids relevant for tumor cell growth were investigated as well. It was established that different building blocks conferred different functionalities, inducing specific antitumor activity against the tumor cells. Full article

(This article belongs to the Special Issue The Emerging Role of Polymeric Materials in Pharmaceutical Designs and Applications)

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15 pages, 2771 KiB

Open AccessArticle

Effect of Chitosan-Diosgenin Combination on Wound Healing

by Lubomir Petrov, Olya Stoilova, Georgi Pramatarov, Hristiyana Kanzova, Elina Tsvetanova, Madlena Andreeva, Almira Georgieva, Dimitrinka Atanasova, Stanislav Philipov and Albena Alexandrova

Int. J. Mol. Sci. 2023, 24(5), 5049; https://doi.org/10.3390/ijms24055049 - 6 Mar 2023

Cited by 5 | Viewed by 2199

Abstract

The difficult-to-heal wounds continue to be a problem for modern medicine. Chitosan and diosgenin possess anti-inflammatory and antioxidant effects making them relevant substances for wound treatment. That is why this work aimed to study the effect of the combined application of chitosan and diosgenin on a mouse skin wound model. For the purpose, wounds (6 mm diameter) were made on mice’s backs and were treated for 9 days with one of the following: 50% ethanol (control), polyethylene glycol (PEG) in 50% ethanol, chitosan and PEG in 50% ethanol (Chs), diosgenin and PEG in 50% ethanol (Dg) and chitosan, diosgenin and PEG in 50% ethanol (ChsDg). Before the first treatment and on the 3rd, 6th and 9th days, the wounds were photographed and their area was determined. On the 9th day, animals were euthanized and wounds’ tissues were excised for histological analysis. In addition, the lipid peroxidation (LPO), protein oxidation (POx) and total glutathione (tGSH) levels were measured. The results showed that ChsDg had the most pronounced overall effect on wound area reduction, followed by Chs and PEG. Moreover, the application of ChsDg maintained high levels of tGSH in wound tissues, compared to other substances. It was shown that all tested substances, except ethanol, reduced POx comparable to intact skin levels. Therefore, the combined application of chitosan and diosgenin is a very promising and effective medication for wound healing. Full article

(This article belongs to the Special Issue The Emerging Role of Polymeric Materials in Pharmaceutical Designs and Applications)

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21 pages, 13895 KiB

Open AccessArticle

Curcumin-Loaded PnBA-b-POEGA Nanoformulations: A Study of Drug-Polymer Interactions and Release Behavior

by Angeliki Chroni, Thomas Mavromoustakos and Stergios Pispas

Int. J. Mol. Sci. 2023, 24(5), 4621; https://doi.org/10.3390/ijms24054621 - 27 Feb 2023

Cited by 4 | Viewed by 2048

Abstract

The current study focuses on the development of innovative and highly-stable curcumin (CUR)-based therapeutics by encapsulating CUR in biocompatible poly(n-butyl acrylate)-block-poly(oligo(ethylene glycol) methyl ether acrylate) (PnBA-b-POEGA) micelles. State-of-the-art methods were used to investigate the encapsulation of CUR in PnBA-b-POEGA micelles and the potential of ultrasound to enhance the release of encapsulated CUR. Dynamic light scattering (DLS), attenuated total reflection Fourier transform infrared (ATR-FTIR), and ultraviolet-visible (UV-Vis) spectroscopies confirmed the successful encapsulation of CUR within the hydrophobic domains of the copolymers, resulting in the formation of distinct and robust drug/polymer nanostructures. The exceptional stability of the CUR-loaded PnBA-b-POEGA nanocarriers over a period of 210 days was also demonstrated by proton nuclear magnetic resonance (¹H-NMR) spectroscopy studies. A comprehensive 2D NMR characterization of the CUR-loaded nanocarriers authenticated the presence of CUR within the micelles, and unveiled the intricate nature of the drug-polymer intermolecular interactions. The UV-Vis results also indicated high encapsulation efficiency values for the CUR-loaded nanocarriers and revealed a significant influence of ultrasound on the release profile of CUR. The present research provides new understanding of the encapsulation and release mechanisms of CUR within biocompatible diblock copolymers and has significant implications for the advancement of safe and effective CUR-based therapeutics. Full article

(This article belongs to the Special Issue The Emerging Role of Polymeric Materials in Pharmaceutical Designs and Applications)

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24 pages, 8633 KiB

Open AccessArticle

Chitosan Sponges with Instantaneous Shape Recovery and Multistrain Antibacterial Activity for Controlled Release of Plant-Derived Polyphenols

by Ioana-Victoria Platon, Claudiu-Augustin Ghiorghita, Maria Marinela Lazar, Irina Elena Raschip and Maria Valentina Dinu

Int. J. Mol. Sci. 2023, 24(5), 4452; https://doi.org/10.3390/ijms24054452 - 23 Feb 2023

Cited by 15 | Viewed by 2289

Abstract

Biomass-derived materials with multiple features are seldom reported so far. Herein, new chitosan (CS) sponges with complementary functions for point-of-use healthcare applications were prepared by glutaraldehyde (GA) cross-linking and tested for antibacterial activity, antioxidant properties, and controlled delivery of plant-derived polyphenols. Their structural, morphological, and mechanical properties were thoroughly assessed by Fourier-transform infrared (FTIR) spectroscopy, scanning electron microscopy (SEM), and uniaxial compression measurements, respectively. The main features of sponges were modulated by varying the CS concentration, cross-linking ratio, and gelation conditions (either cryogelation or room-temperature gelation). They exhibited complete water-triggered shape recovery after compression, remarkable antibacterial properties against Gram-positive (Staphylococcus aureus (S. aureus), Listeria monocytogenes (L. monocytogenes)) and Gram-negative (Escherichia coli (E. coli), Salmonella typhimurium (S. typhimurium)) strains, as well as good radical scavenging activity. The release profile of a plant-derived polyphenol, namely curcumin (CCM), was investigated at 37 °C in simulated gastrointestinal media. It was found that CCM release was dependent on the composition and the preparation strategy of sponges. By linearly fitting the CCM kinetic release data from the CS sponges with the Korsmeyer–Peppas kinetic models, a pseudo-Fickian diffusion release mechanism was predicted. Full article

(This article belongs to the Special Issue The Emerging Role of Polymeric Materials in Pharmaceutical Designs and Applications)

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16 pages, 5397 KiB

Open AccessArticle

Porous Crosslinked Zwitterionic Microparticles Based on Glycidyl Methacrylate and N-Vinylimidazole as Possible Drug Delivery Systems

by Marin-Aurel Trofin, Stefania Racovita, Silvia Vasiliu, Ana-Lavinia Vasiliu and Marcela Mihai

Int. J. Mol. Sci. 2022, 23(23), 14999; https://doi.org/10.3390/ijms232314999 - 30 Nov 2022

Cited by 2 | Viewed by 1715

Abstract

Crosslinked porous microparticles have received great attention as drug delivery systems lately due to their unique set of properties: the capability to form various polymer–drug combinations, low immunogenicity, patient compliance and ability to release drugs in a delayed or controlled manner. Moreover, polymers with betaine groups have shown some unique features such as antifouling, antimicrobial activity, biocompatibility and strong hydration properties. Herein, novel porous zwitterionic microparticles were prepared in two stages. The first step involves the synthesis of porous microparticles based on glycidyl methacrylate, N-vinylimidazole and triethyleneglycol dimethacrylate using the suspension polymerization technique, the second step being the synthesis of zwitterionic porous microparticles by polymer–analogous reaction in presence of sodium monochloroacetate as betainization agent. Both types of microparticles were characterized structurally and morphologically by FT-IR spectroscopy, energy dispersive X-ray analysis, scanning electron microscopy, dynamic vapors sorption and mercury porosimetry. The tetracycline loading into crosslinked and zwitterionic microparticles was also performed, the maximum tetracycline loading capacities being 87 mg/g and 135 mg/g, respectively. The drug release mechanism, elucidated by various mathematical models, is controlled by both diffusion and swelling processes as a function of the zwitterionic and/or porous microparticle structure. Both types of microparticles presented antibacterial activity against the two reference strains used in this study: Escherichia coli and Staphylococcus aureus. Full article

(This article belongs to the Special Issue The Emerging Role of Polymeric Materials in Pharmaceutical Designs and Applications)

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23 pages, 28094 KiB

Open AccessArticle

Evaluation of the Structural Modification of Ibuprofen on the Penetration Release of Ibuprofen from a Drug-in-Adhesive Matrix Type Transdermal Patch

by Paula Ossowicz-Rupniewska, Paulina Bednarczyk, Małgorzata Nowak, Anna Nowak, Wiktoria Duchnik, Łukasz Kucharski, Joanna Klebeko, Ewelina Świątek, Karolina Bilska, Joanna Rokicka, Ewa Janus, Adam Klimowicz and Zbigniew Czech

Int. J. Mol. Sci. 2022, 23(14), 7752; https://doi.org/10.3390/ijms23147752 - 13 Jul 2022

Cited by 10 | Viewed by 2704

Abstract

This study aimed to evaluate the effect of chemical modifications of the structure of active compounds on the skin permeation and accumulation of ibuprofen [IBU] from the acrylic pressure-sensitive adhesive used as a drug-in-adhesives matrix type transdermal patch. The active substances tested were ibuprofen salts obtained by pairing the ibuprofen anion with organic cations, such as amino acid isopropyl esters. The structural modification of ibuprofen tested were Ibuprofen sodium salt, [GlyOiPr][IBU], [AlaOiPr][IBU], [ValOiPr][IBU], [SerOiPr][IBU], [ThrOiPr][IBU], [(AspOiPr)₂][IBU], [LysOiPr][IBU], [LysOiPr][IBU]₂, [PheOiPr][IBU], and [ProOiPr][IBU]. For comparison, the penetration of unmodified ibuprofen and commercially available patches was also investigated. Thus, twelve transdermal patches with new drug modifications have been developed whose adhesive carrier is an acrylate copolymer. The obtained patches were characterized for their adhesive properties and tested for permeability of the active substance. Our results show that the obtained ibuprofen patches demonstrate similar permeability to commercial patches compared to those with structural modifications of ibuprofen. However, these modified patches show an increased drug permeability of 2.3 to even 6.4 times greater than unmodified ibuprofen. Increasing the permeability of the active substance and properties such as adhesion, cohesion, and tack make the obtained patches an excellent alternative to commercial patches containing ibuprofen. Full article

(This article belongs to the Special Issue The Emerging Role of Polymeric Materials in Pharmaceutical Designs and Applications)

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21 pages, 6965 KiB

Open AccessArticle

Does the Freeze–Thaw Technique Affect the Properties of the Alginate/Chitosan Glutamate Gels with Posaconazole as a Model Antifungal Drug?

by Marta Szekalska, Katarzyna Sosnowska, Magdalena Wróblewska, Anna Basa and Katarzyna Winnicka

Int. J. Mol. Sci. 2022, 23(12), 6775; https://doi.org/10.3390/ijms23126775 - 17 Jun 2022

Cited by 9 | Viewed by 2312

Abstract

Hydrogels are semi-solid systems with high flexibility, which, due to holding large amounts of water, are similar to natural tissues and are very useful in the field of biomedical applications. Despite the wide range of polymers available to form hydrogels, novel techniques utilized to obtain hydrogels with adequate properties are still being developed. The aim of this study was to evaluate the impact of the freeze–thaw technique on the properties of cryogels based on sodium alginate and chitosan glutamate with posaconazole as a model antifungal substance. The effect of the freezing and thawing process on the physicochemical, rheological, textural and bioadhesive properties of prepared cryogels was examined. Additionally, the antifungal activity against Candida albicans, Candida parapsilosis and Candida krusei of designed formulations was examined. It was shown that the freeze–thaw technique significantly improved viscosity, bioadhesiveness, textural properties and prolonged the in vitro posaconazole release. Moreover, alginate/chitosan glutamate cryogels exhibited higher values of inhibition zone in C. parapsilosis culture than traditional hydrogel formulations. Full article

(This article belongs to the Special Issue The Emerging Role of Polymeric Materials in Pharmaceutical Designs and Applications)

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Review

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24 pages, 1786 KiB

Open AccessReview

The Potential of Polyelectrolyte Multilayer Films as Drug Delivery Materials

by Joanna Potaś and Katarzyna Winnicka

Int. J. Mol. Sci. 2022, 23(7), 3496; https://doi.org/10.3390/ijms23073496 - 23 Mar 2022

Cited by 11 | Viewed by 2643

Abstract

Polyelectrolyte multilayers (PEMs) represent a group of polyelectrolyte complex (PEC)–based materials widely investigated in the biomedical and pharmaceutical sciences. Despite the unflagging popularity of the aforementioned systems in tissue engineering, only a few updated scientific reports concerning PEM potential in drug administration can be found. In fact, PEM coatings are currently recognized as important tools for functionalizing implantable scaffolds; however, only a small amount of attention has been given to PEMs as drug delivery materials. Scientific reports on PEMs reveal two dominant reasons for the limited usability of multilayers in pharmaceutical technology: complex and expensive preparation techniques as well as high sensitivity of interacting polyelectrolytes to the varieties of internal and external factors. The aim of this work was to analyze the latest approaches, concerning the potential of PEMs in pharmacy, chemical technology, and (primarily) tissue engineering, with special attention given to possible polymer combinations, technological parameters, and physicochemical characteristics, such as hydrophilicity, adhesive and swelling properties, and internal/external structures of the systems formed. Careful recognition of the above factors is crucial in the development of PEM-based drug delivery materials. Full article

(This article belongs to the Special Issue The Emerging Role of Polymeric Materials in Pharmaceutical Designs and Applications)

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