Pharmaceutical Polymers

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

Deadline for manuscript submissions: closed (30 September 2019) | Viewed by 29687

Special Issue Editor

Special Issue Information

Dear Colleagues,

Polymers play essential roles in the pharmaceutical field, thanks to the matching of their chemical-physical features with the needs of medicinal manufacturing processes, as well as in biopharmaceutic aspects. In recent years, the incoming of personalized therapeutic treatments and the spreading of biological therapeutics have further encouraged the development of pharmaceutical polymers thus bringing more opportunities for formulators to achieve efficacious pharmaceutical dosage forms, drug delivery systems, and diagnostics.

This Special Issue is focused on the application of either naturally derived or synthetic biocompatible polymers in the pharmaceutical field, especially dedicated to research aimed at associating specific polymer chemical-physical features with biopharmaceutic and pharmacokinetic improvements, benefits that support active stability, eased processing (eg., printing, electrospinning, nanoparticle technology, etc.), and inherent/adjutant bioactivity.

Dr. Anna Maria Piras
Guest Editor

Manuscript Submission Information

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Keywords

  • Biopolymers
  • Pharmaceutical dosage forms
  • Diagnostics
  • Macromolecular complex
  • Nanomedicine
  • Functional polymers
  • 3D Processing

Published Papers (7 papers)

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Research

11 pages, 1896 KiB  
Article
Polycaprolactone-Based Mimetic Antimicrobial Peptide Copolymers Vesicles as an Effective Drug-Carrier for Cancer Therapy
by Yusheng Qian, Xinyu Zhou, Jing He and Chuncai Zhou
Polymers 2019, 11(11), 1783; https://doi.org/10.3390/polym11111783 - 31 Oct 2019
Cited by 6 | Viewed by 2973
Abstract
A novel series of amphiphilic mimicking antimicrobial peptide copolymers PCL16-b-Kn can assemble in water to form uniform vesicles. Transmission electron microscopy was used to observe the vesicular structure of the nanoparticles, and dynamic light scattering revealed their uniform [...] Read more.
A novel series of amphiphilic mimicking antimicrobial peptide copolymers PCL16-b-Kn can assemble in water to form uniform vesicles. Transmission electron microscopy was used to observe the vesicular structure of the nanoparticles, and dynamic light scattering revealed their uniform size and narrow dispersion. Critical vesiculation concentrations were also tested, revealing that these vesicles can exist at low concentrations. Furthermore, in vitro and intracellular drug release of doxorubicin(DOX)-vesicles were conducted. These vesicles could encapsulate DOX and achieve efficient intracellular drug release. Overall, these copolymer vesicles exhibit potential application value as multifunctional drug-carrier systems with antibacterial capability in cancer therapy. Full article
(This article belongs to the Special Issue Pharmaceutical Polymers)
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17 pages, 3020 KiB  
Article
Gellan Gum-Based Hydrogel for the Transdermal Delivery of Nebivolol: Optimization and Evaluation
by Anroop B. Nair, Jigar Shah, Bader M. Aljaeid, Bandar E. Al-Dhubiab and Shery Jacob
Polymers 2019, 11(10), 1699; https://doi.org/10.3390/polym11101699 - 16 Oct 2019
Cited by 23 | Viewed by 4105
Abstract
Poor solubility and appreciable first-pass metabolism have limited the oral bioavailability of nebivolol. The objective of the current investigation was to design, formulate, and optimize a hydrogel-based transdermal system for nebivolol using factorial design and compare its pharmacokinetics with oral suspension. Hydrogel formulations [...] Read more.
Poor solubility and appreciable first-pass metabolism have limited the oral bioavailability of nebivolol. The objective of the current investigation was to design, formulate, and optimize a hydrogel-based transdermal system for nebivolol using factorial design and compare its pharmacokinetics with oral suspension. Hydrogel formulations (F1–F8) were prepared by varying the amounts of gellan gum, carbopol, and polyethylene glycol. A 23 full factorial design was used to assess the effect of independent variables such as gellan gum, carbopol, and polyethylene glycol 400 on dependent variables like viscosity, in vitro release, and ex vivo permeation after 2 h at two levels. Optimized gel (F7), containing nebivolol hydrochloride (75 mg), gellan gum (300 mg), carbopol (150 mg), polyethylene glycol 400 (20 µL), tween 80 (1 mL), ethanol (10 mL), and water (up to 30 mL) was selected and evaluated in albino rats. The physicochemical properties of F7 (pH: 7.1 ± 0.15, viscosity: 8943 ± 116 centipoise, drug content: 98.81% ± 2.16%) seem ideal for transdermal application. It was noticed that the concentration of carbopol has a more significant role than gellan gum in gel viscosity. A biphasic release pattern was exhibited by gels, and the release rate was mainly influenced by the concentration of gellan gum. Greater transdermal flux (30.86 ± 4.08 µg/cm2/h) was observed in F7 as compared with other prepared gels. Noticeable enhancement in AUC0-α value (986.52 ± 382.63 ng.h/mL; p < 0.01) of transdermal therapy (~2-fold higher compared with oral administration) established the potential of F7 to improve the rate and extent of nebivolol delivery. The overall results demonstrated here signify that F7 could be a feasible alternative to oral therapy of nebivolol. Full article
(This article belongs to the Special Issue Pharmaceutical Polymers)
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16 pages, 4834 KiB  
Article
pH-Responsive Carboxymethylcellulose Nanoparticles for 68Ga-WBC Labeling in PET Imaging
by Anna Maria Piras, Angela Fabiano, Stefania Sartini, Ylenia Zambito, Simona Braccini, Federica Chiellini, Angela G. Cataldi, Francesco Bartoli, Ana de la Fuente and Paola Anna Erba
Polymers 2019, 11(10), 1615; https://doi.org/10.3390/polym11101615 - 5 Oct 2019
Cited by 9 | Viewed by 2811
Abstract
Carboxymethylcellulose (CMC) is a well-known pharmaceutical polymer, recently gaining attention in the field of nanomedicine, especially as a polyelectrolyte agent for the formation of complexes with oppositely charged macromolecules. Here, we report on the application of pH-sensitive pharmaceutical grade CMC-based nanoparticles (NP) for [...] Read more.
Carboxymethylcellulose (CMC) is a well-known pharmaceutical polymer, recently gaining attention in the field of nanomedicine, especially as a polyelectrolyte agent for the formation of complexes with oppositely charged macromolecules. Here, we report on the application of pH-sensitive pharmaceutical grade CMC-based nanoparticles (NP) for white blood cells (WBC) PET imaging. In this context and as an alternative to 99mTc-HMPAO SPECT labeling, the use of 68Ga3+ as PET radionuclide was investigated since, at early time points, it could provide the greater spatial resolution and patient convenience of PET tomography over SPECT clinical practices. Two operator-friendly kit-type formulations were compared, with the intention of radiolabeling within a short time (10 min), under mild conditions (physiological pH, room temperature) and in agreement with the actual clinically applied guidelines. NP were labeled by directly using 68Ga3+ eluted in HCL 0.05 N, from hospital suited 68Ge/68Ga generator and in absence of chelator. The first kit type approach involved the application of 68Ga3+ as an ionotropic gelation agent for in-situ forming NP. The second kit type approach concerned the re-hydration of a proper freeze-dried injectable NP powder. pH-sensitive NP with 250 nm average diameter and 80% labeling efficacy were obtained. The NP dispersant medium, including a cryoprotective agent, was modulated in order to optimize the Zeta potential value (−18 mV), minimize the NP interaction with serum proteins and guarantee a physiological environment for WBC during NP incubation. Time-dependent WBC radiolabeling was correlated to NP uptake by using both confocal and FT-IR microscopies. The ready to use lyophilized NP formulation approach appears promising as a straightforward 68Ga-WBC labeling tool for PET imaging applications. Full article
(This article belongs to the Special Issue Pharmaceutical Polymers)
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11 pages, 2015 KiB  
Article
Polyelectrolyte Complexes between Polycarboxylates and BMP-2 for Enhancing Osteogenic Differentiation: Effect of Chemical Structure of Polycarboxylates
by Masahiko Terauchi, Atsushi Tamura, Asato Tonegawa, Satoshi Yamaguchi, Tetsuya Yoda and Nobuhiko Yui
Polymers 2019, 11(8), 1327; https://doi.org/10.3390/polym11081327 - 9 Aug 2019
Cited by 13 | Viewed by 3890
Abstract
Bone morphogenetic protein 2 (BMP-2) has received considerable attention because of its osteoinductivity, but its use is limited owing to its instability and adverse effects. To reduce the dose of BMP-2, complexation with heparin is a promising approach, because heparin enhances the osteoinductivity [...] Read more.
Bone morphogenetic protein 2 (BMP-2) has received considerable attention because of its osteoinductivity, but its use is limited owing to its instability and adverse effects. To reduce the dose of BMP-2, complexation with heparin is a promising approach, because heparin enhances the osteoinductivity of BMP-2. However, the clinical use of heparin is restricted because of its anticoagulant activity. Herein, to explore alternative polymers that show heparin-like activity, four polycarboxylates, poly(acrylic acid) (PAA), poly(methacrylic acid) (PMAA), poly(aspartic acid) (PAsp), and poly(glutamic acid) (PGlu), were selected and their capability to modulate the osteoinductivity of BMP-2 was evaluated. Dynamic light scattering indicated that these polycarboxylates formed polyelectrolyte complexes with BMP-2. The osteogenic differentiation efficiency of MC3T3-E1 cells treated with the polycarboxylate/BMP-2 complexes was investigated in comparison to that of the heparin/BMP-2 complex. As a result, PGlu/BMP-2 complex showed the highest activity of alkaline phosphatase, which is an early-stage marker of osteogenic differentiation, and rapid mineralization. Based on these observations, PGlu could serve as an alternative to heparin in the regenerative therapy of bone using BMP-2. Full article
(This article belongs to the Special Issue Pharmaceutical Polymers)
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18 pages, 4131 KiB  
Article
Relationship between Degree of Polymeric Ionisation and Hydrolytic Degradation of Eudragit® E Polymers under Extreme Acid Conditions
by Valentina Linares, Cristhian J. Yarce, Juan D. Echeverri, Elkin Galeano and Constain H. Salamanca
Polymers 2019, 11(6), 1010; https://doi.org/10.3390/polym11061010 - 7 Jun 2019
Cited by 30 | Viewed by 5986
Abstract
The commercial copolymers Eudragit® E 100 and Eudragit® PO are widely used materials in the pharmaceutical field as coating systems. Such materials derived from amino-methacrylate groups under acidulated conditions may acquire an ionisable fraction or undergo hydrolytic degradation of the polymeric [...] Read more.
The commercial copolymers Eudragit® E 100 and Eudragit® PO are widely used materials in the pharmaceutical field as coating systems. Such materials derived from amino-methacrylate groups under acidulated conditions may acquire an ionisable fraction or undergo hydrolytic degradation of the polymeric structure. This work focused on establishing the chemical, physical, and surface changes of two reprocessed polymeric materials, here named as EuCl-E-100 and EuCl-E-PO, which were obtained from the commercial Eudragit® E 100 and Eudragit® E PO, respectively. The commercial materials were exposed to extreme acid conditions, where the polymers were solubilised and subsequently dried by the refractance window method. The materials obtained were chemically characterised by potentiometric titration, nuclear magnetic resonance spectroscopy (1H NMR and 13C NMR) in one and two dimensions (COSY, HSQC, and HMBC), infrared spectroscopy, X-ray diffraction, and differential scanning calorimetry. Changes in the physical properties of the materials were evaluated through studies of flowability, compactability, and their ability to gain and lose humidity. Surface thermodynamic studies were carried out through contact angle measurements using the sessile drop method. The results showed that the processed polymeric materials acquired a substantial degree of ionisation without undergoing hydrolysis of the esterified groups. Furthermore, such changes improved the flow characteristics of the material and the solubility in aqueous media at pH > 5, while also maintaining the hydrophobicity degree of the polymeric surface. Full article
(This article belongs to the Special Issue Pharmaceutical Polymers)
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12 pages, 2763 KiB  
Article
Butylglyceryl Pectin Nanoparticles: Synthesis, Formulation and Characterization
by Mohammad F. Bostanudin, Mosab Arafat, Muhammad Sarfraz, Dariusz C. Górecki and Eugen Barbu
Polymers 2019, 11(5), 789; https://doi.org/10.3390/polym11050789 - 2 May 2019
Cited by 24 | Viewed by 3724
Abstract
Pectin is a polysaccharide with very good gel forming properties that traditionally has found important applications in foods and pharmaceutical industries. Although less studied, chemical modifications of pectin leading to a decrease in its hydrophilicity can be useful for the development of novel [...] Read more.
Pectin is a polysaccharide with very good gel forming properties that traditionally has found important applications in foods and pharmaceutical industries. Although less studied, chemical modifications of pectin leading to a decrease in its hydrophilicity can be useful for the development of novel drug carriers. To this aim, butylglyceryl pectins (P-OX4) were synthesized via functionalization with n-butylglycidyl ether and subsequently formed into nanoparticles. Chromatographic, spectroscopic, and thermal analytical methods were employed to characterize the novel butylglyceryl pectins (P-OX4) obtained, prior to their formulation into nanoparticles via nanoprecipitation. Nuclear magnetic resonance (NMR) and Fourier transform infrared (FT-IR) spectroscopy confirmed a degree of modification in these materials in the range 10.4–13.6%, and thermal stability studies indicated an increase in both the thermal decomposition onset and glass transition temperature values (compared to those of the original pectin). An increase in the molecular weight and a decrease in the viscosity of P-OX4, when compared to the starting material, were also observed. The resulting nanoformulations were investigated in terms of particle morphology, size and stability, and it was found that particles were roughly spherical, with their size below 300 nm, and a negative zeta potential (−20 to −26 mV, indicating good stability). Having demonstrated the ability to load Doxorubicin at the level of 10%, their potential in drug delivery applications warrants further investigations. Full article
(This article belongs to the Special Issue Pharmaceutical Polymers)
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17 pages, 2345 KiB  
Article
Ethylcellulose in Organic Solution or Aqueous Dispersion Form in Designing Taste-Masked Microparticles by the Spray Drying Technique with a Model Bitter Drug: Rupatadine Fumarate
by Katarzyna Wasilewska, Marta Szekalska, Patrycja Ciosek-Skibinska, Joanna Lenik, Anna Basa, Julia Jacyna, Michal Markuszewski and Katarzyna Winnicka
Polymers 2019, 11(3), 522; https://doi.org/10.3390/polym11030522 - 20 Mar 2019
Cited by 16 | Viewed by 4944
Abstract
The taste of drugs is an important factor affecting pharmacotherapy effectiveness, and obtaining formulations with acceptable organoleptic properties is still an ongoing issue in pharmaceutical technology. One of the innovative methods of taste masking is preparation of microparticles by the spray drying technique, [...] Read more.
The taste of drugs is an important factor affecting pharmacotherapy effectiveness, and obtaining formulations with acceptable organoleptic properties is still an ongoing issue in pharmaceutical technology. One of the innovative methods of taste masking is preparation of microparticles by the spray drying technique, utilizing polymers with different physicochemical properties. Rupatadine fumarate (RUP) is one of the newest antihistamines, with an innovative and multidirectional mechanism of action, and an extremely bitter taste. The aim of this work was to investigate the feasibility of utilizing organic or aqueous forms of ethylcellulose (EC) for the preparation of microparticles with RUP by the spray drying technique. Spray dried samples at different drug:polymer ratios were prepared using organic solution (Ethocel®) or aqueous dispersions of EC (Surelease®, Aquacoat® ECD). Evaluation of the taste masking efficacy was performed in vivo in human taste panel, in vitro based on dissolution test, and by self-constructed electronic tongue. It was shown that microparticles obtained from aqueous dispersions of EC have superior pharmaceutical properties in terms of both morphology and taste masking efficacy in comparison to those obtained from organic solution. Full article
(This article belongs to the Special Issue Pharmaceutical Polymers)
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