Advanced Polymeric Materials for Pharmaceutical Applications IV

A special issue of Polymers (ISSN 2073-4360). This special issue belongs to the section "Polymer Applications".

Deadline for manuscript submissions: 15 June 2024 | Viewed by 7210

Special Issue Editors


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Guest Editor
School of Pharmacy, Aristotle University of Thessaloniki, 54124 Thessaloniki, Greece
Interests: drug delivery systems; polyesters; controlled drug release; polymeric solid dispersions
Special Issues, Collections and Topics in MDPI journals

E-Mail Website
Guest Editor
Laboratory of Organic Chemistry, School of Chemical Engineering, Aristotle University of Thessaloniki, 54124 Thessaloniki, Greece
Interests: nanotechnology; natural products; drug delivery systems; pharmaceutical technology
Special Issues, Collections and Topics in MDPI journals

Special Issue Information

Dear Colleagues,

Polymers, whether synthetic or of natural origin, have played an important role in the development and advancement of pharmaceutical and biomedical applications. In this context, efforts are constantly being made to develop new polymeric materials having exceptional properties for use in medical applications (low toxicity, good biocompatibility, etc.). Within this framework, the current Special Issue (SI) aims to explore the various aspects related to the development and pharmaceutical/biomedical applications of modern advanced polymeric materials. The authors will cover all relevant sections, including immediate and controlled drug release, implants, patches, medical devices, dental composites, diagnostics, etc. The scope of this SI is to provide an expert panel with a primary emphasis on addressing the needs and interests of both academic and industrial readers.

Dr. Panagiotis Barmpalexis
Dr. Konstantinos N. Kontogiannopoulos
Guest Editors

Manuscript Submission Information

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Published Papers (6 papers)

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Research

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26 pages, 26654 KiB  
Article
Nitrocellulose for Prolonged Permeation of Levofloxacin HCl-Salicylic Acid In Situ Gel
by Ei Mon Khaing, Kritamorn Jitrangsri, Parichart Chomto and Thawatchai Phaechamud
Polymers 2024, 16(7), 989; https://doi.org/10.3390/polym16070989 - 04 Apr 2024
Viewed by 476
Abstract
Currently, the application of solvent exchange-induced in situ gel is underway for drug delivery to the body target site. Nitrocellulose was attempted in this research as the matrix-forming agent in solvent exchange-induced in situ gel for acne and periodontitis treatments. The gel incorporated [...] Read more.
Currently, the application of solvent exchange-induced in situ gel is underway for drug delivery to the body target site. Nitrocellulose was attempted in this research as the matrix-forming agent in solvent exchange-induced in situ gel for acne and periodontitis treatments. The gel incorporated a combination of 1% w/w levofloxacin HCl and 2% w/w salicylic acid as the active compounds. In order to facilitate formulation development, the study explored the matrix-forming behavior of different concentrations of nitrocellulose in N-methyl pyrrolidone (NMP). Consequently, their physicochemical properties and matrix-forming behavior, as well as antimicrobial and anti-inflammatory activities, were evaluated using the agar cup diffusion method and thermal inhibition of protein denaturation in the egg albumin technique, respectively. All prepared formulations presented as clear solutions with Newtonian flow. Their contact angles on agarose gel were higher than on a glass slide due to matrix formation upon exposure to the aqueous phase of agarose, with an angle of less than 60° indicating good spreadability. Nitrocellulose concentrations exceeding 20% initiated stable opaque matrix formation upon contact with phosphate buffer pH 6.8. The high hardness and remaining force of the transformed gel indicated their robustness after solvent exchange. Fluorescence tracking using sodium fluorescein and Nile red confirmed the retardation of NMP and water diffusion by the nitrocellulose matrix. From the Franz cell permeation study, these drugs could permeate through neonate porcine skin and tissue of porcine buccal from the nitrocellulose in situ forming gel. Their accumulation in these tissues might enable the inhibition of the invading bacterial pathogens. The developed in situ gels effectively inhibited Staphylococcus aureus, Staphylococcus epidermidis, Propionibacterium acnes, and Porphyromonas gingivalis. Furthermore, the formulations demonstrated an anti-inflammatory effect. The low viscosity of LvSa25Nc makes it appropriate for injectable treatments targeting periodontitis, while the higher viscosity of LvSa40Nc renders it appropriate for topical applications in acne treatment. Therefore, the nitrocellulose in situ gel loaded with combined levofloxacin HCl and salicylic acid emerges as a promising dosage form for treating acne and periodontitis. Full article
(This article belongs to the Special Issue Advanced Polymeric Materials for Pharmaceutical Applications IV)
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19 pages, 4678 KiB  
Article
Utilizing Drug Amorphous Solid Dispersions for the Preparation of Dronedarone per os Formulations
by Afroditi Kapourani, Alexandra-Eleftheria Manioudaki, Konstantinos N. Kontogiannopoulos and Panagiotis Barmpalexis
Polymers 2023, 15(21), 4292; https://doi.org/10.3390/polym15214292 - 01 Nov 2023
Cited by 1 | Viewed by 743
Abstract
Dronedarone (DRN), an antiarrhythmic drug, exhibits potent pharmacological effects in the management of cardiac arrhythmias. Despite its therapeutic potential, DRN faces formulation challenges due to its low aqueous solubility. Hence, the present study is dedicated to the examination of amorphous solid dispersions (ASDs) [...] Read more.
Dronedarone (DRN), an antiarrhythmic drug, exhibits potent pharmacological effects in the management of cardiac arrhythmias. Despite its therapeutic potential, DRN faces formulation challenges due to its low aqueous solubility. Hence, the present study is dedicated to the examination of amorphous solid dispersions (ASDs) as a strategic approach for enhancing the solubility of DRN. Initially, the glass forming ability (GFA) of API was assessed alongside its thermal degradation profile, and it was revealed that DRN is a stable glass former (GFA III compound) that remains thermally stable up to approximately 200 °C. Subsequently, five commonly used ASD matrix/carriers, i.e., hydroxypropyl methylcellulose (HPMC), povidone (PVP), copovidone (PVP/VA), Soluplus® (SOL), and Eudragit® E PO (EPO), were screened for the formation of a DRN-based ASD using film casting and solvent shift methods, along with miscibility evaluation measurements. SOL proved to be the most promising matrix/carrier among the others, and, hence, was used to prepare DRN ASDs via the melt-quench method. The physicochemical characterization of the prepared systems (via pXRD) revealed the complete amorphization of the API within the matrix/carrier, while the system was physically stable for at least three months after its preparation. In vitro release studies for the ASDs, conducted under non-sink conditions, revealed the sustained supersaturation of the drug for at least 8 h. Finally, the use of attenuated total reflectance (ATR) FTIR spectroscopy showed the formation of a strong molecular interaction between the drug molecules and SOL. Full article
(This article belongs to the Special Issue Advanced Polymeric Materials for Pharmaceutical Applications IV)
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13 pages, 1242 KiB  
Article
An Evaluation of Parylene Thin Films to Prevent Encrustation for a Urinary Bladder Pressure MEMS Sensor System
by Sébastien Buchwalder, Mario Hersberger, Henrike Rebl, Susanne Seemann, Wolfgang Kram, Andreas Hogg, Lars G. W. Tvedt, Ingelin Clausen and Jürgen Burger
Polymers 2023, 15(17), 3559; https://doi.org/10.3390/polym15173559 - 27 Aug 2023
Viewed by 978
Abstract
Recent developments in urological implants have focused on preventive strategies to mitigate encrustation and biofilm formation. Parylene, a conformal, pinhole-free polymer coating, has gained attention due to its high biocompatibility and chemical resistance, excellent barrier properties, and low friction coefficient. This study aims [...] Read more.
Recent developments in urological implants have focused on preventive strategies to mitigate encrustation and biofilm formation. Parylene, a conformal, pinhole-free polymer coating, has gained attention due to its high biocompatibility and chemical resistance, excellent barrier properties, and low friction coefficient. This study aims to evaluate the effectiveness of parylene C in comparison to a parylene VT4 grade coating in preventing encrustation on a urinary bladder pressure MEMS sensor system. Additionally, silicon oxide (SiOx) applied as a finish coating was investigated for further improvements. An in vitro encrustation system mimicking natural urine flow was used to quantify the formation of urinary stones. These stones were subsequently analyzed using Fourier transform infrared spectrometry (FTIR). Encrustation results were then discussed in relation to coating surface chemical properties. Parylene C and VT4 grades demonstrated a very low encrustation mass, making them attractive options for encrustation prevention. The best performance was achieved after the addition of a hydrophilic SiOx finish coating on parylene VT4 grade. Parylene-based encapsulation proved to be an outstanding solution to prevent encrustation for urological implants. Full article
(This article belongs to the Special Issue Advanced Polymeric Materials for Pharmaceutical Applications IV)
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10 pages, 1581 KiB  
Article
Polyethylene Glycol-Mediated Directional Conjugation of Biological Molecules for Enhanced Immunoassays at the Point-of-Care
by Dheerendranath Battalapalli, Purbali Chakraborty, Disha Jain, Stephen K. Obaro, Umut A. Gurkan, Robert A. Bonomo and Mohamed S. Draz
Polymers 2023, 15(15), 3316; https://doi.org/10.3390/polym15153316 - 05 Aug 2023
Viewed by 1516
Abstract
Rapid and reliable point-of-care (POC) diagnostic tests can have a significant impact on global health. One of the most common approaches for developing POC systems is the use of target-specific biomolecules. However, the conjugation of biomolecules can result in decreased activity, which may [...] Read more.
Rapid and reliable point-of-care (POC) diagnostic tests can have a significant impact on global health. One of the most common approaches for developing POC systems is the use of target-specific biomolecules. However, the conjugation of biomolecules can result in decreased activity, which may compromise the analytical performance and accuracy of the developed systems. To overcome this challenge, we present a polymer-based cross-linking protocol for controlled and directed conjugation of biological molecules. Our protocol utilizes a bifunctional thiol-polyethylene glycol (PEG)-hydrazide polymer to enable site-directed conjugation of IgG antibodies to the surface of screen-printed metal electrodes. The metal surface of the electrodes is first modified with thiolated PEG molecules, leaving the hydrazide groups available to react with the aldehyde group in the Fc fragments of the oxidized IgG antibodies. Using anti-Klebsiella pneumoniae carbapenemase-2 (KPC-2) antibody as a model antibody used for antimicrobial resistance (AMR) testing, our results demonstrate a ~10-fold increase in antibody coupling compared with the standard N-hydroxysuccinimide (NHS)-based conjugation chemistry and effective capture (>94%) of the target KPC-2 enzyme antigen on the surface of modified electrodes. This straightforward and easy-to-perform strategy of site-directed antibody conjugation can be engineered for coupling other protein- and non-protein-based biological molecules commonly used in POC testing and development, thus enhancing the potential for improved diagnostic accuracy and performance. Full article
(This article belongs to the Special Issue Advanced Polymeric Materials for Pharmaceutical Applications IV)
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14 pages, 5055 KiB  
Article
Human Serum Albumin Nanoparticles: Synthesis, Optimization and Immobilization with Antituberculosis Drugs
by Aldana Galiyeva, Arailym Daribay, Tolkyn Zhumagaliyeva, Lyazzat Zhaparova, Daniyar Sadyrbekov and Yerkeblan Tazhbayev
Polymers 2023, 15(13), 2774; https://doi.org/10.3390/polym15132774 - 22 Jun 2023
Cited by 4 | Viewed by 1708
Abstract
The aim of this study was to create nanoparticles of human serum albumin immobilized with anti-TB drugs (rifampicin, isoniazid) using the desolvation method. Central Composite Design (CCD) was applied to study the effect of albumin, urea, L-cysteine, rifampicin and isoniazid concentration on particle [...] Read more.
The aim of this study was to create nanoparticles of human serum albumin immobilized with anti-TB drugs (rifampicin, isoniazid) using the desolvation method. Central Composite Design (CCD) was applied to study the effect of albumin, urea, L-cysteine, rifampicin and isoniazid concentration on particle size, polydispersity and loading degree of the drugs. The optimized nanoparticles were spherical in shape with an average particle size of 216.7 ± 3.7 nm and polydispersity of 0.286 ± 4.9. The loading degree of rifampicin and isoniazid in the optimized nanoparticles were 44% and 27%, respectively. The obtained nanoparticles were examined by Fourier-transform infrared spectroscopy (FTIR), thermogravimetric analysis (TGA) and differential scanning calorimetry (DSC); the results showed the absence of drug–polymer interactions. The drug release from the polymer matrix was studied using dialysis membranes. Full article
(This article belongs to the Special Issue Advanced Polymeric Materials for Pharmaceutical Applications IV)
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Review

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15 pages, 1312 KiB  
Review
Molecularly Imprinted Polymers for Pharmaceutical Impurities: Design and Synthesis Methods
by Aliya Nur Hasanah and Ike Susanti
Polymers 2023, 15(16), 3401; https://doi.org/10.3390/polym15163401 - 14 Aug 2023
Cited by 4 | Viewed by 1225
Abstract
The safety of a medicinal product is determined by its pharmacological and toxicological profile, which depends not only on the active substance’s toxicological properties, but also on the impurities it contains. Because impurities are a problem that must be considered to ensure the [...] Read more.
The safety of a medicinal product is determined by its pharmacological and toxicological profile, which depends not only on the active substance’s toxicological properties, but also on the impurities it contains. Because impurities are a problem that must be considered to ensure the safety of a drug product, many studies have been conducted regarding the separation or purification of active pharmaceutical ingredients (APIs) and the determination of impurities in APIs and drug products. Several studies have applied molecularly imprinted polymers (MIPs) to separate impurities in active ingredients and as adsorbents in the sample preparation process. This review presents the design of MIPs and the methods used to synthesise MIPs to separate impurities in APIs and drug product samples, the application of MIPs to separate impurities, and a view of future studies involving MIPs to remove impurities from pharmaceutical products. Based on a comparison of the bulk and surface-imprinting polymerisation methods, the MIPs produced by the surface-imprinting polymerisation method have a higher adsorption capacity and faster adsorption kinetics than the MIPs produced by the bulk polymerisation method. However, the application of MIPs in the analysis of APIs and drug products are currently only related to organic compounds. Considering the advantages of MIPs to separate impurities, MIPs for other impurities still need to be developed, including multi-template MIPs for simultaneous separation of multiple impurities. Full article
(This article belongs to the Special Issue Advanced Polymeric Materials for Pharmaceutical Applications IV)
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