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Polymers for Pharmaceutical Applications II
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Polymers for Pharmaceutical Applications II

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

Deadline for manuscript submissions: closed (31 December 2020) | Viewed by 31059

Special Issue Editor

Prof. Dr. Vitaliy V. Khutoryanskiy

E-Mail Website
Guest Editor
Reading School of Pharmacy, University of Reading, Reading RG6 6AD, UK
Interests: water-soluble polymers; hydrogels; polymer complexes; drug delivery; mucoadhesion; nanomaterials
Special Issues, Collections and Topics in MDPI journals

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 can be used as suspending, emulsifying, binding, and flocculating agents, and as adhesives, packaging, and coating materials. They can 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). There are also numerous applications of polymers in the design of advanced drug delivery systems. These include conjugates of drugs and other biopharmaceutical agents with polymers, in situ gelling systems, nano- and microparticles functionalized with various ligands to achieve drug targeting, multistage delivery systems, etc.

All these potential pharmaceutical applications of polymers will be covered in this Special Issue, which welcomes the 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
  • hydrogels
  • solid drug dispersions
  • dosage forms
  • coatings
  • nano- and microparticles
  • controlled release
  • in situ gelling systems
  • capsules

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Published Papers (6 papers)

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Research

11 pages, 824 KiB  
Communication
Determination of Temperature-Dependent Coefficients of Viscosity and Surface Tension of Tamarind Seeds (Tamarindus indica L.) Polymer
by Rishabha Malviya, Sheetal Jha, Neeraj Kumar Fuloria, Vetriselvan Subramaniyan, Srikumar Chakravarthi, Kathiresan Sathasivam, Usha Kumari, Dhanalekshmi Unnikrishnan Meenakshi, Omji Porwal, Akanksha Sharma, Darnal Hari Kumar and Shivkanya Fuloria
Polymers 2021, 13(4), 610; https://doi.org/10.3390/polym13040610 - 18 Feb 2021
Cited by 10 | Viewed by 3854
Abstract
The rheological properties of tamarind seed polymer are characterized for its possible commercialization in the food and pharmaceutical industry. Seed polymer was extracted using water as a solvent and ethyl alcohol as a precipitating agent. The temperature’s effect on the rheological behavior of [...] Read more.
The rheological properties of tamarind seed polymer are characterized for its possible commercialization in the food and pharmaceutical industry. Seed polymer was extracted using water as a solvent and ethyl alcohol as a precipitating agent. The temperature’s effect on the rheological behavior of the polymeric solution was studied. In addition to this, the temperature coefficient, viscosity, surface tension, activation energy, Gibbs free energy, Reynolds number, and entropy of fusion were calculated by using the Arrhenius, Gibbs–Helmholtz, Frenkel–Eyring, and Eotvos equations, respectively. The activation energy of the gum was found to be 20.46 ± 1.06 kJ/mol. Changes in entropy and enthalpy were found to be 23.66 ± 0.97 and −0.10 ± 0.01 kJ/mol, respectively. The calculated amount of entropy of fusion was found to be 0.88 kJ/mol. A considerable decrease in apparent viscosity and surface tension was produced when the temperature was raised. The present study concludes that the tamarind seed polymer solution is less sensitive to temperature change in comparison to Albzia lebbac gum, Ficus glumosa gum and A. marcocarpa gum. This study also concludes that the attainment of the transition state of viscous flow for tamarind seed gum is accompanied by bond breaking. The excellent physicochemical properties of tamarind seed polymers make them promising excipients for future drug formulation and make their application in the food and cosmetics industry possible. Full article
(This article belongs to the Special Issue Polymers for Pharmaceutical Applications II)
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19 pages, 6731 KiB  
Article
Influence of Drug Incorporation on the Physico-Chemical Properties of Poly(l-Lactide) Implant Coating Matrices—A Systematic Study
by Daniela Arbeiter, Thomas Reske, Michael Teske, Dalibor Bajer, Volkmar Senz, Klaus-Peter Schmitz, Niels Grabow and Stefan Oschatz
Polymers 2021, 13(2), 292; https://doi.org/10.3390/polym13020292 - 18 Jan 2021
Cited by 18 | Viewed by 3617
Abstract
Local drug delivery has become indispensable in biomedical engineering with stents being ideal carrier platforms. While local drug release is superior to systemic administration in many fields, the incorporation of drugs into polymers may influence the physico-chemical properties of said matrix. This is [...] Read more.
Local drug delivery has become indispensable in biomedical engineering with stents being ideal carrier platforms. While local drug release is superior to systemic administration in many fields, the incorporation of drugs into polymers may influence the physico-chemical properties of said matrix. This is of particular relevance as minimally invasive implantation is frequently accompanied by mechanical stresses on the implant and coating. Thus, drug incorporation into polymers may result in a susceptibility to potentially life-threatening implant failure. We investigated spray-coated poly-l-lactide (PLLA)/drug blends using thermal measurements (DSC) and tensile tests to determine the influence of selected drugs, namely sirolimus, paclitaxel, dexamethasone, and cyclosporine A, on the physico-chemical properties of the polymer. For all drugs and PLLA/drug ratios, an increase in tensile strength was observed. As for sirolimus and dexamethasone, PLLA/drug mixed phase systems were identified by shifted drug melting peaks at 200 °C and 240 °C, respectively, whereas paclitaxel and dexamethasone led to cold crystallization. Cyclosporine A did not affect matrix thermal properties. Altogether, our data provide a contribution towards an understanding of the complex interaction between PLLA and different drugs. Our results hold implications regarding the necessity of target-oriented thermal treatment to ensure the shelf life and performance of stent coatings. Full article
(This article belongs to the Special Issue Polymers for Pharmaceutical Applications II)
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16 pages, 2795 KiB  
Article
Hybrid Acrylated Chitosan and Thiolated Pectin Cross-Linked Hydrogels with Tunable Properties
by Shaked Eliyahu, Alexandra Galitsky, Esther Ritov and Havazelet Bianco-Peled
Polymers 2021, 13(2), 266; https://doi.org/10.3390/polym13020266 - 14 Jan 2021
Cited by 25 | Viewed by 3903
Abstract
We developed and characterized a new hydrogel system based on the physical and chemical interactions of pectin partially modified with thiol groups and chitosan modified with acrylate end groups. Gelation occurred at high pectin thiol ratios, indicating that a low acrylated chitosan concentration [...] Read more.
We developed and characterized a new hydrogel system based on the physical and chemical interactions of pectin partially modified with thiol groups and chitosan modified with acrylate end groups. Gelation occurred at high pectin thiol ratios, indicating that a low acrylated chitosan concentration in the hydrogel had a profound effect on the cross-linking. Turbidity, Fourier transform infrared spectroscopy, and free thiol determination analyses were performed to determine the relationships of the different bonds inside the gel. At low pH values below the pKa of chitosan, more electrostatic interactions were formed between opposite charges, but at high pH values, the Michael-type addition reaction between acrylate and thiol took place, creating harder hydrogels. Swelling experiments and Young’s modulus measurements were performed to study the structure and properties of the resultant hydrogels. The nanostructure was examined using small-angle X-ray scattering. The texture profile analysis showed a unique property of hydrogel adhesiveness. By implementing changes in the preparation procedure, we controlled the hydrogel properties. This hybrid hydrogel system can be a good candidate for a wide range of biomedical applications, such as a mucosal biomimetic surface for mucoadhesive testing. Full article
(This article belongs to the Special Issue Polymers for Pharmaceutical Applications II)
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17 pages, 4131 KiB  
Article
Interpolymer Complexes of Eudragit® Copolymers as Novel Carriers for Colon-Specific Drug Delivery
by Aleksandra V. Bukhovets, Nikoletta Fotaki, Vitaliy V. Khutoryanskiy and Rouslan I. Moustafine
Polymers 2020, 12(7), 1459; https://doi.org/10.3390/polym12071459 - 30 Jun 2020
Cited by 18 | Viewed by 4509
Abstract
Interpolymer complexes (IPC) based on Eudragit® EPO and Eudragit® S100 were investigated as potential carriers for oral controlled drug delivery to the colon. IPC samples were prepared by mixing copolymer solutions in organic solvents (ethanol, isopropanol:acetone mixture (60:40, % v/ [...] Read more.
Interpolymer complexes (IPC) based on Eudragit® EPO and Eudragit® S100 were investigated as potential carriers for oral controlled drug delivery to the colon. IPC samples were prepared by mixing copolymer solutions in organic solvents (ethanol, isopropanol:acetone mixture (60:40, % v/v) and tetrahydrofuran). According to the data of elemental analysis, FTIR-spectroscopy, X-ray photoelectron spectroscopy and thermal analysis these IPCs have excess of anionic copolymer (Eudragit® S100) in their structure; they are stabilized by hydrogen and ionic intermacromolecular bonds and do not include free copolymer domains. IPC have pH-independent swelling properties in the media mimicking gastrointestinal tract (GIT) conditions and provide colon-specific delivery of indomethacin in buffer solutions (pH 1.2; 5.8; 6.8; 7.4) and in biorelevant media (fasted state simulated gastric fluid, fasted state simulated intestinal fluid—version 2 and fasted stated simulated colonic fluid). Full article
(This article belongs to the Special Issue Polymers for Pharmaceutical Applications II)
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13 pages, 3911 KiB  
Article
Synthesis and Comparative Study of Nanoparticles Derived from Bovine and Human Serum Albumins
by Yerkeblan Tazhbayev, Olzhas Mukashev, Meiram Burkeyev and Vladimir I. Lozinsky
Polymers 2020, 12(6), 1301; https://doi.org/10.3390/polym12061301 - 6 Jun 2020
Cited by 13 | Viewed by 5049
Abstract
This study describes the preparation of nanoparticles derived from bovine serum albumin (BSA) in comparison with the formation of nanoparticles composed of human serum albumin (HSA), when the same preparation procedure was used in both cases. To obtain protein nanoparticles, the method of [...] Read more.
This study describes the preparation of nanoparticles derived from bovine serum albumin (BSA) in comparison with the formation of nanoparticles composed of human serum albumin (HSA), when the same preparation procedure was used in both cases. To obtain protein nanoparticles, the method of desolvation with ethanol was employed, followed by the stabilization with urea and cysteine. It was shown that, upon transition from HSA to BSA, the particles with smaller sizes and with a narrower polydispersity were formed. The possibility of the immobilization of the antitumor drug hydroxyurea in such protein nanoparticles by adsorption and inclusion methods has been shown. The drug release profile from the polymer matrix was established. Full article
(This article belongs to the Special Issue Polymers for Pharmaceutical Applications II)
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18 pages, 3966 KiB  
Article
Less Reactive Thiol Ligands: Key towards Highly Mucoadhesive Drug Delivery Systems
by Iram Shahzadi, Andrea Fürst, Zeynep Burcu Akkus-Dagdeviren, Shumaila Arshad, Markus Kurpiers, Barbara Matuszczak and Andreas Bernkop-Schnürch
Polymers 2020, 12(6), 1259; https://doi.org/10.3390/polym12061259 - 30 May 2020
Cited by 19 | Viewed by 4277
Abstract
As less reactive s-protected thiomers can likely interpenetrate the mucus gel layer to a higher extent before getting immobilized via disulfide bond formation with mucins, it was the aim of this study to develop a novel type of s-protected thiomer based [...] Read more.
As less reactive s-protected thiomers can likely interpenetrate the mucus gel layer to a higher extent before getting immobilized via disulfide bond formation with mucins, it was the aim of this study to develop a novel type of s-protected thiomer based on the less reactive substructure cysteine-N-acetyl cysteine (Cys-NAC) in order to obtain improved mucoadhesive properties. For this purpose, two types of s-protected thiomers, polyacrylic acid-cysteine-mercaptonicotinic acid (PAA-Cys-MNA) and polyacrylic acid-cysteine-N-acetyl cysteine (PAA-Cys-NAC), were synthesized and characterized by Fourier-transform infrared spectroscopy (FT-IR) and the quantification of attached disulfide ligands. The viscosity of both products was measured in the presence of NAC and mucus. Both thiomers were also evaluated regarding swelling behavior, tensile studies and retention time on the porcine intestinal mucosa. The FT-IR spectra confirmed the successful attachment of Cys-MNA and Cys-NAC ligands to PAA. The number of attached sulfhydryl groups was in the range of 660–683 µmol/g. The viscosity of both s-protected thiomers increased due to the addition of increasing amounts of NAC. The viscosity of the mucus increased in the presence of 1% PAA-Cys-MNA and PAA-Cys-NAC 5.6- and 10.9-fold, respectively, in comparison to only 1% PAA. Both s-protected thiomers showed higher water uptake than unmodified PAA. The maximum detachment force (MDF) and the total work of adhesion (TWA) increased in the case of PAA-Cys-MNA up to 1.4- and 1.6-fold and up to 2.4- and 2.8-fold in the case of PAA-Cys-NAC. The retention of PAA, PAA-Cys-MNA, and PAA-Cys-NAC on porcine intestinal mucosa was 25%, 49%, and 76% within 3 h, respectively. The results of this study provide evidence that less reactive s-protected thiomers exhibit higher mucoadhesive properties than highly reactive s-protected thiomers. Full article
(This article belongs to the Special Issue Polymers for Pharmaceutical Applications II)
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