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Polymers in Pharmaceutical Technology
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Polymers in Pharmaceutical Technology

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

Deadline for manuscript submissions: closed (25 July 2023) | Viewed by 30042

Special Issue Editor

Dr. Natassa Pippa

E-Mail Website
Guest Editor
Department of Pharmacy, National & Kapodistrian University of Athens, Athens, Greece
Interests: drug delivery systems; liposomes; polymers; nanotechnology; fractals
Special Issues, Collections and Topics in MDPI journals

Special Issue Information

Dear Colleagues,

The advances in materials science have been greatly beneficial to pharmaceutical technology with regard to the preparation of innovative delivery platforms of active pharmaceutical ingredients (APIs). Polymers are considered as the best materials with properties making them ideal candidates as innovative excipients of the design and development of delivery platforms. Polymer therapeutics attracts the interest of the scientific community due to its numerous advantages, i.e., biocompatibility, stealth, controlled release properties, etc. Polymers are included in marketed medicinal products, medicines and medical devices, acting as solubilizers, permeation enhancers, and helping toward the specific targeting of the drugs to the site of actions.

This Special Issue is concerned with the applications of polymers in pharmaceutics, including polymeric pharmaceutical excipients in solid oral dosage forms, controlled release matrix systems, and amorphous solid dispersions. Topics may include the synthesis of novel polymers, physicochemical characterizations, self-assembly behavior, interactions of polymers with active pharmaceutical ingredients and/or other excipients, as well as the impact of polymers into the drug release mechanism. Special attention will be given to applications of polymers in pharmaceutical nanotechnology. The formation, preparation, and drug loading/release of polymer micelles, polyelectrolyte complexes, polymersomes, polymeric nanoparticles, and nanogels are hot topics in current literature, too. Both original manuscripts and reviews are welcome.

Dr. Natassa Pippa
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 excipients
  • Solubilizers
  • Permeation enhancers
  • Polymer coating
  • Capsule shells
  • Osmotic pumps
  • Solid dosage forms
  • Matrix systems
  • Controlled release
  • Polymer dispersions
  • Micelles
  • polymeric nanoparticles
  • Polymersomes
  • Polyplex
  • Polyelectrolyte
  • Biopolymer
  • Hydrogels

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Related Special Issue

Published Papers (7 papers)

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Research

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14 pages, 12324 KiB  
Article
Drug-Polymers Composite Matrix Tablets: Effect of Hydroxypropyl Methylcellulose (HPMC) K-Series on Porosity, Compatibility, and Release Behavior of the Tablet Containing a BCS Class I Drug
by Namon Hirun and Pakorn Kraisit
Polymers 2022, 14(16), 3406; https://doi.org/10.3390/polym14163406 - 19 Aug 2022
Cited by 16 | Viewed by 5083
Abstract
The purpose of this research was to see how the physicochemical properties and porosity of matrix tablets containing various types of hydroxypropyl methylcellulose (HPMC) K series affected the release of propranolol hydrochloride (PNL). PNL is a class I drug (high solubility and permeability) [...] Read more.
The purpose of this research was to see how the physicochemical properties and porosity of matrix tablets containing various types of hydroxypropyl methylcellulose (HPMC) K series affected the release of propranolol hydrochloride (PNL). PNL is a class I drug (high solubility and permeability) according to the Biopharmaceutics Classification System (BCS), making it an excellent model drug used for studying extended-release drug products. The direct compression method was used to prepare the HPMC-based matrix tablets. PNL and the excipients were found to be compatible using Fourier transform infrared spectroscopy (FTIR), powder X-ray diffraction (PXRD), and differential scanning calorimetry (DSC). The surfaces of all the compressed HPMC-based matrix tablets were rough, with accumulated particles and small holes. The compressed HPMC-based matrix tablet porosity was also determined by using mercury porosimetry. The compressed HPMC-based matrix tablets made of low viscosity HPMC had tiny pores (diameter < 0.01 μm). The shorter polymeric chains are more prone to deformation, resulting in a small pore proportion. The compressed HPMC-based matrix tablets sustained the release of PNL for over 12 h. The release exponent values (n), which reflect the release mechanism of the drug from the tablets, ranged from 0.476 to 0.497. These values indicated that the release was governed by anomalous transport. The compressed HPMC-based matrix tablets have the potential for a sustained release of PNL. Full article
(This article belongs to the Special Issue Polymers in Pharmaceutical Technology)
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14 pages, 1553 KiB  
Article
Modified Release of the Pineal Hormone Melatonin from Matrix Tablets Containing Poly(L-lactic Acid) and Its PLA-co-PEAd and PLA-co-PBAd Copolymers
by Marilena Vlachou, Angeliki Siamidi, Dionysia Anagnostopoulou, Evi Christodoulou and Nikolaos D. Bikiaris
Polymers 2022, 14(8), 1504; https://doi.org/10.3390/polym14081504 - 7 Apr 2022
Cited by 5 | Viewed by 2674
Abstract
In terms of drug delivery, the attractive properties of poly(L-lactic acid) (PLA) and its aliphatic polyesters, poly(ethylene adipate) (PEAd) and poly(butylene adipate) (PBAd), render them ideal co-formulants for the preparation of modified-release pharmaceutical formulations. Furthermore, we have previously demonstrated that by [...] Read more.
In terms of drug delivery, the attractive properties of poly(L-lactic acid) (PLA) and its aliphatic polyesters, poly(ethylene adipate) (PEAd) and poly(butylene adipate) (PBAd), render them ideal co-formulants for the preparation of modified-release pharmaceutical formulations. Furthermore, we have previously demonstrated that by adding a “softer” aliphatic polyester onto the macromolecular chain of PLA, i.e., PEAd or PBAd, resulting in the formation of the PLA’s copolymers (PLA-co-PEAd and PLA-co-PBAd, in 95/5, 90/10, 75/25 and 50/50 weight ratios), the hydrolysis rate is also severely affected, leading to improved dissolution rates of the active pharmaceutical ingredients (API). In the present report, we communicate our findings on the in vitro modified release of the chronobiotic hormone melatonin (MLT), in aqueous media (pH 1.2 and 6.8), from poly(L-lactic acid) and the aforementioned copolymer matrix tablets, enriched with commonly used biopolymers, such as hydroxypropylmethylcellulose (HPMC K15), lactose monohydrate, and sodium alginate. It was found that, depending on the composition and the relevant content of these excipients in the matrix tablets, the release of MLT satisfied the sought targets for fast sleep onset and sleep maintenance. These findings constitute a useful background for pursuing relevant in vivo studies on melatonin in the future. Full article
(This article belongs to the Special Issue Polymers in Pharmaceutical Technology)
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17 pages, 3426 KiB  
Article
Evaluation and Characterization of Curcumin-β-Cyclodextrin and Cyclodextrin-Based Nanosponge Inclusion Complexation
by Hadeia Mashaqbeh, Rana Obaidat and Nizar Al-Shar’i
Polymers 2021, 13(23), 4073; https://doi.org/10.3390/polym13234073 - 24 Nov 2021
Cited by 48 | Viewed by 5445
Abstract
Cyclodextrin polymers and cyclodextrin-based nanosponges have been widely investigated for increasing drug bioavailability. This study examined curcumin’s complexation stability and solubilization with β-cyclodextrin and β-cyclodextrin-based nanosponge. Nanosponges were prepared through the cross-linking of β-cyclodextrin with different molar ratios of diphenyl carbonate. Phase solubility [...] Read more.
Cyclodextrin polymers and cyclodextrin-based nanosponges have been widely investigated for increasing drug bioavailability. This study examined curcumin’s complexation stability and solubilization with β-cyclodextrin and β-cyclodextrin-based nanosponge. Nanosponges were prepared through the cross-linking of β-cyclodextrin with different molar ratios of diphenyl carbonate. Phase solubility experiments were conducted to evaluate the formed complexes and evaluate the potential of using β-cyclodextrin and nanosponge in pharmaceutical formulations. Furthermore, physicochemical characterizations of the prepared complexes included PXRD, FTIR, NMR, and DSC. In addition, in vitro release studies were performed for the prepared formulations. The formation of β-cyclodextrin complexes enhanced curcumin solubility up to 2.34-fold compared to the inherent solubility, compared to a 2.95-fold increment in curcumin solubility when loaded in β-cyclodextrin-based nanosponges. Interestingly, the stability constant for curcumin nanosponges was (4972.90 M−1), which was ten times higher than that for the β-cyclodextrin complex, where the value was 487.34 M−1. The study results indicated a decrease in the complexation efficiency and solubilization effect with the increased cross-linker amount. This study’s findings showed the potential of using cyclodextrin-based nanosponge and the importance of studying the effect of cross-linking density for the preparation of β-cyclodextrin-based nanosponges to be used for pharmaceutical formulations. Full article
(This article belongs to the Special Issue Polymers in Pharmaceutical Technology)
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18 pages, 4236 KiB  
Article
Probing the Release of Bupropion and Naltrexone Hydrochloride Salts from Biopolymeric Matrices of Diverse Chemical Structures
by Angeliki Siamidi, Aikaterini Dedeloudi and Marilena Vlachou
Polymers 2021, 13(9), 1456; https://doi.org/10.3390/polym13091456 - 30 Apr 2021
Cited by 3 | Viewed by 4458
Abstract
In the last decades, the notion of including excipients in the formulations, as inert substances aiding production processes, has changed and they are recently viewed as multifunctional discrete entities. It is now well documented that excipients serve several roles, spreading from the stabilization [...] Read more.
In the last decades, the notion of including excipients in the formulations, as inert substances aiding production processes, has changed and they are recently viewed as multifunctional discrete entities. It is now well documented that excipients serve several roles, spreading from the stabilization and modified release, to providing biocompatible properties and targeting moieties. The aim of this study was to develop matrix-based oral drug delivery systems of bupropion hydrochloride (BUP·HCl) and naltrexone hydrochloride (NTX·HCl), suitable for releasing these active substances in a modified manner, providing a stable level of drug release, which is simultaneously therapeutically effective and non-toxic, thus reducing side effects, after a single dose administration, throughout the gastrointestinal tract. The new formulations, employing hydroxypropylmethycellulose (HPMC K15M) (a cellulosic polymer, which, generally hydrates to form a gelatinous layer that is critical to prevent wetting and rapid drug release from the matrices), poly(methacylic acid-co-ethyl acrylate) 1:1 (Eudragit® L100-55: effective for site specific drug delivery in intestine), poly(ethylene oxide) (PEO) (7 × 106: a high molecular weight polymer, water-soluble, in micro-granular powder form), as the rate controlling polymers, were chosen to lead to a “soothing out” release pattern of these drugs, at 0 ≤ t ≤ 120 min. Moreover, the release of the two drugs from the ulvan-based tablets, was found to follow the desired profile, throughout the entire course of the dissolution experiments. Full article
(This article belongs to the Special Issue Polymers in Pharmaceutical Technology)
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19 pages, 4452 KiB  
Article
Formation of Uni-Lamellar Vesicles in Mixtures of DPPC with PEO-b-PCL Amphiphilic Diblock Copolymers
by Aristeidis Papagiannopoulos, Natassa Pippa, Costas Demetzos, Stergios Pispas and Aurel Radulescu
Polymers 2021, 13(1), 4; https://doi.org/10.3390/polym13010004 - 22 Dec 2020
Cited by 6 | Viewed by 2774
Abstract
The ability of mixtures of 1.2-dipalmitoyl-sn-glycero-3-phosphocholine (DPPC) and the amphiphilic diblock copolymers poly (ethylene oxide)-block-poly(ε-caprolactone) (PEO-b-PCL) to stabilize uni-lamellar nano-vesicles is reported. Small angle neutron scattering (SANS) is used to define their size distribution and bilayer structure and resolve the copresence of aggregates [...] Read more.
The ability of mixtures of 1.2-dipalmitoyl-sn-glycero-3-phosphocholine (DPPC) and the amphiphilic diblock copolymers poly (ethylene oxide)-block-poly(ε-caprolactone) (PEO-b-PCL) to stabilize uni-lamellar nano-vesicles is reported. Small angle neutron scattering (SANS) is used to define their size distribution and bilayer structure and resolve the copresence of aggregates and clusters in solution. The vesicles have a broad size distribution which is compatible with bilayer membranes of relatively low bending stiffness. Their mean diameter increases moderately with temperature and their number density and mass is higher in the case of the diblock copolymer with the larger hydrophobic block. Bayesian analysis is performed in order to justify the use of the particular SANS fitting model and confirm the reliability of the extracted parameters. This study shows that amphiphilic block copolymers can be effectively used to prepare mixed lipid-block copolymer vesicles with controlled lamellarity and a significant potential as nanocarriers for drug delivery. Full article
(This article belongs to the Special Issue Polymers in Pharmaceutical Technology)
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Review

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22 pages, 22086 KiB  
Review
Polymeric Nanostructures Containing Proteins and Peptides for Pharmaceutical Applications
by Antiopi Vardaxi, Martha Kafetzi and Stergios Pispas
Polymers 2022, 14(4), 777; https://doi.org/10.3390/polym14040777 - 16 Feb 2022
Cited by 13 | Viewed by 4203
Abstract
Over the last three decades, proteins and peptides have attracted great interest as drugs of choice for combating a broad spectrum of diseases, including diabetes mellitus, cancer, and infectious and neurological diseases. However, the delivery of therapeutic proteins to target sites should take [...] Read more.
Over the last three decades, proteins and peptides have attracted great interest as drugs of choice for combating a broad spectrum of diseases, including diabetes mellitus, cancer, and infectious and neurological diseases. However, the delivery of therapeutic proteins to target sites should take into account the obstacles and limitations related to their intrinsic sensitivity to different environmental conditions, fragile tertiary structures, and short half-life. Polymeric nanostructures have emerged as competent vehicles for protein delivery, as they are multifunctional and can be tailored according to their peculiarities. Thus, the enhanced bioavailability and biocompatibility, the adjustable control of physicochemical features, and the colloidal stability of polymer-based nanostructures further enable either the embedding or conjugation of hydrophobic or hydrophilic bioactive molecules, which are some of the features of paramount importance that they possess and which contribute to their selection as vehicles. The present review aims to discuss the prevalent nanostructures composed of block copolymers from the viewpoint of efficient protein hospitality and administration, as well as the up-to-date scientific publications and anticipated applications of polymeric nanovehicles containing proteins and peptides. Full article
(This article belongs to the Special Issue Polymers in Pharmaceutical Technology)
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21 pages, 4165 KiB  
Review
Progress in the Development of Chitosan Based Insulin Delivery Systems: A Systematic Literature Review
by Francivandi Coelho Barbosa, Milena Costa da Silva, Henrique Nunes da Silva, Danyllo Albuquerque, Allyson Antônio Ribeiro Gomes, Suédina Maria de Lima Silva and Marcus Vinícius Lia Fook
Polymers 2020, 12(11), 2499; https://doi.org/10.3390/polym12112499 - 27 Oct 2020
Cited by 20 | Viewed by 2962
Abstract
Diabetes mellitus is a chronic disease that is considered a worldwide epidemic, and its control is a constant challenge for health systems. Since insulin had its first successful use, scientists have researched to improve the desired effects and reduce side-effects. Over the years, [...] Read more.
Diabetes mellitus is a chronic disease that is considered a worldwide epidemic, and its control is a constant challenge for health systems. Since insulin had its first successful use, scientists have researched to improve the desired effects and reduce side-effects. Over the years, the challenge has been to increase adherence to treatment and improve the quality of life for diabetics by developing an insulin delivery system. This systematic review (SR) analyses experimental articles from 1998 to 2018 related to the development of the chitosan/insulin delivery system (CIDS). Automated support: Start tool was used to perform part of these activities. The search terms “insulin”, “delivery or release system”, and “chitosan” were used to retrieve articles in PubMed, Science Direct, Engineering Village, and HubMed. A total of 55 articles were selected. The overview, phase, model, way of administration, and the efficiency of CIDS were analyzed. According to SR results, most of the articles were published from 2010 onwards, representing 72.7% of the selected papers, and research groups from China publicized 23.6% of the selected articles. According to the SR, 51% of the studies were carried out in vivo and 45% in vitro. Most of the systems were nanoparticle based (54.8%), and oral administration was proposed by 60.0% of the selected articles. Only 36.4% performed loaded capacity and encapsulation efficiency assays, and 24 h (16.4%), 12 h (12.7%), and 6 h (11.0%) were the most frequent insulin release times. Chitosan’s intrinsic characteristics, which include biodegradability, biocompatibility, adhesiveness, the ability to open epithelial tight junctions to allow an increase in the paracellular transport of macromolecular drugs, such as insulin, and the fact that it does not result in allergic reactions in the human body after implantation, injection, topical application or ingestion, have contributed to the increase in research of CIDS over the years. However, the number of studies is still limited and the use of an alternative form of insulin administration is not yet possible. Thus, more studies in this area, aiming for the development of an insulin delivery system that can promote more adherence to the treatment and patient comfort, are required. Full article
(This article belongs to the Special Issue Polymers in Pharmaceutical Technology)
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