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Polymers for Pharmaceutical Applications

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

Deadline for manuscript submissions: closed (29 February 2020) | Viewed by 25931

Special Issue Editor


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Guest Editor

Special Issue Information

Dear Colleagues,

Polymers are widely used in pharmaceutical applications. It is difficult to imagine a modern dosage form which could be prepared completely without the use of polymers. Polymers could play different roles in the design of pharmaceutical dosage forms. They could be used as suspending, emulsifying, binding, and flocculating agents, adhesives, packaging, and coating materials. They could also be used to make gels, nanoparticles, microparticles, and various capsules. Some functional polymers also exhibit intrinsic biological activity, e.g., materials with antimicrobial or anticoagulant properties. Additionally, drugs and other biopharmaceutical agents could be covalently linked to some polymers to modify their properties.

All these potential pharmaceutical applications of polymers will be covered in this Special Issue, which welcomes submission of both reviews and original research articles in this area.

Prof. Vitaliy Khutoryanskiy
Guest Editor

Manuscript Submission Information

Manuscripts should be submitted online at www.mdpi.com by registering and logging in to this website. Once you are registered, click here to go to the submission form. Manuscripts can be submitted until the deadline. All submissions that pass pre-check are peer-reviewed. Accepted papers will be published continuously in the journal (as soon as accepted) and will be listed together on the special issue website. Research articles, review articles as well as short communications are invited. For planned papers, a title and short abstract (about 100 words) can be sent to the Editorial Office for announcement on this website.

Submitted manuscripts should not have been published previously, nor be under consideration for publication elsewhere (except conference proceedings papers). All manuscripts are thoroughly refereed through a single-blind peer-review process. A guide for authors and other relevant information for submission of manuscripts is available on the Instructions for Authors page. Polymers is an international peer-reviewed open access semimonthly journal published by MDPI.

Please visit the Instructions for Authors page before submitting a manuscript. The Article Processing Charge (APC) for publication in this open access journal is 2700 CHF (Swiss Francs). Submitted papers should be well formatted and use good English. Authors may use MDPI's English editing service prior to publication or during author revisions.

Keywords

  • pharmaceutical polymers
  • drug delivery
  • polyelectrolytes
  • polysaccharides
  • gels
  • solid dosage forms
  • semi-solid dosage forms
  • liquid dosage forms
  • adhesives
  • coatings
  • particles
  • controlled release

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Published Papers (5 papers)

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Research

19 pages, 5028 KiB  
Article
Development and Evaluation of a Polyvinylalcohol -Cellulose Derivative-Based Film with Povidone-Iodine Predicted for Wound Treatment
by Dorota Kida, Olimpia Gładysz, Małgorzata Szulc, Jacek Zborowski, Adam Junka, Maciej Janeczek, Anna Lipińska, Aleksandra Skalec and Bożena Karolewicz
Polymers 2020, 12(6), 1271; https://doi.org/10.3390/polym12061271 - 2 Jun 2020
Cited by 18 | Viewed by 5550
Abstract
The aim of this study was to develop and assess a polyvinyl alcohol-cellulose derivatives-based film with incorporated povidone-iodine (PVP-I) predicted for applications in the treatment of periodontitis. Films were fabricated by solvent-casting, and their physical characteristics, such as their surface and structure morphology, [...] Read more.
The aim of this study was to develop and assess a polyvinyl alcohol-cellulose derivatives-based film with incorporated povidone-iodine (PVP-I) predicted for applications in the treatment of periodontitis. Films were fabricated by solvent-casting, and their physical characteristics, such as their surface and structure morphology, mechanical properties, and disintegrating time, were evaluated. For in vitro iodine release studies and evaluation, the antimicrobial activity was tested using a modified disc diffusion method against five microbial strains. For further use, we selected the film with polyvinyl alcohol-hydroxypropyl methylcellulose (PVA/HPMC_B) based on acceptable physicochemical properties. To assess the subacute toxicity of the film composition, the tissue regeneration process was tested in rats and compared to a conventional dressing commonly used in wound healing (Spongostan). Seven days after implantation, dorsal skin sections and blood samples (n = 10, in total n = 30) were examined. The wound area, epithelium, and dermis were evaluated microscopically, while the blood collected from the rats underwent biochemical analysis. The blood biochemistry results were comparable in all three groups. No significant histological differences between the Spongostan and the placebo film developed after subcutaneous implantation were observed. In contrast, the inflammation stage was reduced and the “scar” in the dermis was smaller when PVP-I and PVA/HPMC_B films were used. A smaller local inflammatory response inflicted less tissue damage, leading to the activation of subsequent regeneration phases and restoration of the area to its original state. The results obtained confirmed that PVP-I incorporated into PVA-hydroxypropyl methylcellulose film is a promising drug carrier, working faster and more effectively than the other two dressing materials evaluated. These developments provide a promising alternative in tissue regeneration and the wound healing process. Full article
(This article belongs to the Special Issue Polymers for Pharmaceutical Applications)
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21 pages, 5071 KiB  
Article
Photosensitive Poly-l-lysine/Heparin Interpolyelectrolyte Complexes for Delivery of Genetic Drugs
by Viktor Korzhikov-Vlakh, Iuliia Katernuk, Iuliia Pilipenko, Antonina Lavrentieva, Ivan Guryanov, Vladimir Sharoyko, Alina A. Manshina and Tatiana B. Tennikova
Polymers 2020, 12(5), 1077; https://doi.org/10.3390/polym12051077 - 8 May 2020
Cited by 7 | Viewed by 4419
Abstract
Photo-triggered release of biopharmaceutical drugs inside the cells is a challenging direction of modern science, which requires obtaining new polymeric systems. The interpolyelectrolyte complexes (IPECs) of poly-l-lysine with heparin capable of encapsulation of genetic constructions—such as model oligonucleotide, siRNA, and pDNA—were [...] Read more.
Photo-triggered release of biopharmaceutical drugs inside the cells is a challenging direction of modern science, which requires obtaining new polymeric systems. The interpolyelectrolyte complexes (IPECs) of poly-l-lysine with heparin capable of encapsulation of genetic constructions—such as model oligonucleotide, siRNA, and pDNA—were obtained. Poly-l-lysine to heparin ratios were optimized to provide the appropriate release kinetics of genetic material from the polyplex. In order to impart the obtained IPEC with photosensitive properties, the linker was synthesized as based on 4-brommethyl-3-nitrobenzoic acid. The conditions and kinetics of photosensitive linker destruction were carefully studied. The colloid particles of IPEC were modified with Cy3 probe and their cellular internalization was investigated by flow cytometry method. The efficacy of photosensitive IPECs as siRNA and pDNA delivery system was evaluated. Full article
(This article belongs to the Special Issue Polymers for Pharmaceutical Applications)
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18 pages, 2489 KiB  
Article
Solubility Improvement of Progesterone from Solid Dispersions Prepared by Solvent Evaporation and Co-milling
by Xing Chen, Ioannis Partheniadis, Ioannis Nikolakakis and Hisham Al-Obaidi
Polymers 2020, 12(4), 854; https://doi.org/10.3390/polym12040854 - 7 Apr 2020
Cited by 29 | Viewed by 5015
Abstract
The aim of this contribution was to evaluate the impact of processing methods and polymeric carriers on the physicochemical properties of solid dispersions of the poorly soluble drug progesterone (PG). Five polymers: hydroxypropyl methylcellulose (HPMC), hydroxypropyl methylcellulose acetate succinate (HPMCAS), microcrystalline cellulose (MCC), [...] Read more.
The aim of this contribution was to evaluate the impact of processing methods and polymeric carriers on the physicochemical properties of solid dispersions of the poorly soluble drug progesterone (PG). Five polymers: hydroxypropyl methylcellulose (HPMC), hydroxypropyl methylcellulose acetate succinate (HPMCAS), microcrystalline cellulose (MCC), polyvinylpyrrolidone (PVP) and silica (SiO2), and two processing methods: solvent evaporation (SE) and mechano-chemical activation by co-milling (BM) were applied. H-bonding was demonstrated by FTIR spectra as clear shifting of drug peaks at 1707 cm−1 (C20 carbonyl) and 1668 cm−1 (C3 carbonyl). Additionally, spectroscopic and thermal analysis revealed the presence of unstable PG II polymorphic form and a second heating DSC cycle, the presence of another polymorph possibly assigned to form III, but their influence on drug solubility was not apparent. Except for PG–MCC, solid dispersions improved drug solubility compared to physical mixtures. For SE dispersions, an inverse relationship was found between drug water solubility and drug–polymer Hansen solubility parameter difference (Δδt), whereas for BM dispersions, the solubility was influenced by both the intermolecular interactions and the polymer Tg. Solubility improvement with SE was demonstrated for all except PG–MCC dispersions, whereas improvement with BM was demonstrated by the PG–HPMC, PG–PVP and PG–HPMCAS dispersions, the last showing impressive increase from 34.21 to 82.13 μg/mL. The extensive H-bonding between PG and HPMCAS was proved by FTIR analysis of the dispersion in the liquid state. In conclusion, although SE improved drug solubility, BM gave more than twice greater improvement. This indicates that directly operating intermolecular forces are more efficient than the solvent mediated. Full article
(This article belongs to the Special Issue Polymers for Pharmaceutical Applications)
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21 pages, 3791 KiB  
Article
Different Types of Gel Carriers as Metronidazole Delivery Systems to the Oral Mucosa
by Magdalena Wróblewska, Emilia Szymańska, Marta Szekalska and Katarzyna Winnicka
Polymers 2020, 12(3), 680; https://doi.org/10.3390/polym12030680 - 19 Mar 2020
Cited by 47 | Viewed by 6347
Abstract
Periodontal diseases are some of the most widespread oral afflictions, and they are labeled as chronic infections caused by the accumulation of bacteria in dental plaque that produces localized inflammation of the periodontium. The use of local drug delivery systems to treat periodontal [...] Read more.
Periodontal diseases are some of the most widespread oral afflictions, and they are labeled as chronic infections caused by the accumulation of bacteria in dental plaque that produces localized inflammation of the periodontium. The use of local drug delivery systems to treat periodontal diseases has received greater attention, because the active substance is targeted directly to the affected area, which minimizes its systemic side effects. Therefore, the purpose of the investigation was to develop and characterize different types of gel formulations—bigel, hydrogel and oleogel—as local delivery systems containing metronidazole (MET), which can be applied to the oral mucosa. The influence of the formulation type on the mechanical, rheological and mucoadhesive properties were examined. Moreover, in vitro release of metronidazole, its ex vivo permeation through buccal porcine mucosa and antimicrobial activity measured by the plate diffusion method were estimated. It was found that the gel formulations obtained were non-Newtonian systems, showing a shear-thinning behavior and thixotropic properties with good textural features such as firmness, compressibility and adhesiveness. Moreover, the preparations designed possessed beneficial mucoadhesive properties. The formulated hydrogels and bigels containing micronized MET were considered as better formulations in terms of drug release and antimicrobial activity compared to commercially available metronidazole ointment. An ex vivo permeation study with the use of porcine buccal mucosa demonstrated that the bigel formulation was characterized by higher initial permeability rate providing a fast therapeutic effect with simultaneous moderate retention in mucosal tissue to decrease the risk of local cytotoxicity. Full article
(This article belongs to the Special Issue Polymers for Pharmaceutical Applications)
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18 pages, 3713 KiB  
Article
Development of Novel Galactosylated PLGA Nanoparticles for Hepatocyte Targeting Using Molecular Modelling
by Cláudia D. Raposo, Rita Costa, Krasimira T. Petrova, Catarina Brito, Marcus T. Scotti and M. Margarida Cardoso
Polymers 2020, 12(1), 94; https://doi.org/10.3390/polym12010094 - 4 Jan 2020
Cited by 12 | Viewed by 3606
Abstract
Doxorubicin-loaded PLGA nanoparticles conjugated with a new galactose-based ligand for the specific recognition by human hepatoma cellular carcinoma cells (Hep G2) were successfully produced. The new targeting compound was selected using molecular docking combined with quantum chemical calculations for modelling and comparing molecular [...] Read more.
Doxorubicin-loaded PLGA nanoparticles conjugated with a new galactose-based ligand for the specific recognition by human hepatoma cellular carcinoma cells (Hep G2) were successfully produced. The new targeting compound was selected using molecular docking combined with quantum chemical calculations for modelling and comparing molecular interactions among the H1 subunit of the asialoglycoprotein receptor containing the carbohydrate recognition domain and the ligand. The ligand, bis(1-O-ethyl-β-D-galactopyranosyl)amine, was synthetized, characterized, and subsequently linked to PLGA. Unloaded (PLGA-di-GAL NP) and doxorubicin-loaded (DOX-PLGA-di-GAL NP) nanoparticles were prepared using an emulsion method and characterized. The produced DOX-PLGA-di-GAL NP are spherical in shape with a size of 258 ± 47 nm, a zeta potential of −62.3 mV, and a drug encapsulation efficiency of 83%. The in vitro drug release results obtained show a three-phase release profile. In vitro cell studies confirmed the interaction between Hep G2 cells and PLGA-di-GAL NP. Cell cytotoxicity tests showed that unloaded NP are nontoxic and that DOX-PLGA-di-GAL NP caused a decrease of around 80% in cellular viability. The strategy used in this work to design new targeting compounds represents a promising tool to develop effective hepatocyte targeting drug delivery systems and can be applied to other tissues/organs. Full article
(This article belongs to the Special Issue Polymers for Pharmaceutical Applications)
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