Polymers for Controlled/Targeted Drug and Gene Delivery

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

Deadline for manuscript submissions: closed (31 July 2023) | Viewed by 4240

Special Issue Editors


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Guest Editor
1. Department of Pharmaceutical Sciences, Medical University of Plovdiv, Plovdiv, Bulgaria
2. Research Institute at Medical University of Plovdiv (RIMU), Plovdiv, Bulgaria
Interests: polymer drug carriers; micro- and nanoparticles;controlled drug release

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Guest Editor
Department of Bioorganic Chemistry, Faculty of Pharmacy, Medical University of Plovdiv, 4002 Plovdiv, Bulgaria
Interests: biopolymers; chitosan; casein; micro gels; targeted drug delivery
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Special Issue Information

Dear Colleagues,

In recent decades, polymers are widely used as biomaterials due to their favorable properties, such as good biocompatibility, biodegradability, simple design and preparation of a variety of structures with tunable characteristics. The development of drug delivery systems based on natural and synthetic polymers is rapidly emerging in the pharmaceutical field. Polymers play a significant role as drug and gene carriers because they can deliver therapeutic agents directly into the intended site of action at a controlled rate with superior efficacy. Thus, the formulation of polymer carriers with improved characteristics can provide better control of the pharmacokinetic and pharmacodynamic drug behavior and ensure more effective and safe therapy. In this context, developments in recent years have focused on various types of polymer micro- and nano-sized drug and gene delivery systems:  micro- and nanospheres, micro- and nanocapsules, microbeads, microfilms, microneedles, microsponges, nanogels, nanofibers, nanotubes and others, as well as exploring the possibilities for alternative routes of administration, such as pulmonary, transdermal, ocular, nasal, including nose-to-brain administration.

This Special Issue will collect studies concerning the current and emerging research on the design and development of advanced polymer drug/gene delivery systems and their application. Special attention will be given to research articles focused on major conceptual and technological challenges to the successful formulation of polymer-based systems for controlled/targeted delivery with improved therapeutical properties.

Dr. Plamen Katsarov
Dr. Bissera Pilicheva
Dr. Cédric Delattre
Guest Editors

Manuscript Submission Information

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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

  • polymer drug carriers
  • drug delivery systems
  • polymer gene carriers
  • micro- and nanoparticles
  • targeted drug delivery
  • controlled drug release
  • alternative routes of administration

Published Papers (3 papers)

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Research

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17 pages, 4927 KiB  
Article
Copolymeric Micelles of Poly(ε-caprolactone) and Poly(methacrylic acid) as Carriers for the Oral Delivery of Resveratrol
by Katya Kamenova, Lyubomira Radeva, Spiro Konstantinov, Petar D. Petrov and Krassimira Yoncheva
Polymers 2023, 15(18), 3769; https://doi.org/10.3390/polym15183769 - 14 Sep 2023
Cited by 2 | Viewed by 918
Abstract
In this study, we report the development of a micellar system based on a poly(methacrylic acid)-b-poly(ε-caprolactone)-b-poly(methacrylic acid) triblock copolymer (PMAA16-b-PCL35-b-PMAA16) for the oral delivery of resveratrol. The micellar nanocarriers were designed to comprise [...] Read more.
In this study, we report the development of a micellar system based on a poly(methacrylic acid)-b-poly(ε-caprolactone)-b-poly(methacrylic acid) triblock copolymer (PMAA16-b-PCL35-b-PMAA16) for the oral delivery of resveratrol. The micellar nanocarriers were designed to comprise a PCL core for solubilizing the poorly water-soluble drug and a hydrated PMAA corona with bioadhesive properties for providing better contact with the gastrointestinal mucosa. The micelles were first formed in an aqueous media via the solvent evaporation method and then loaded with resveratrol (72% encapsulation efficiency). Studies by transmission electron microscopy (TEM) and dynamic and electrophoretic light scattering (DLS and PALS) revealed a spherical shape, nanoscopic size (100 nm) and a negative surface charge (−30 mV) of the nanocarriers. Loading of the drug slightly decreased the hydrodynamic diameter (Dh) and increased the ƺ-potential of micelles. In vitro dissolution tests showed that 80% and 100% of resveratrol were released in 24 h in buffers with pH 1.2 and 6.8, respectively, whereas for the same time, not more than 10% of pure resveratrol was dissolved. A heat-induced albumin denaturation assay demonstrated the advantage of the aqueous micellar formulation of resveratrol, which possessed anti-inflammatory potential as high as that of the pure drug. Further, the micellar resveratrol (5 µM) exerted a strong protective effect and maintained viability of mucosa epithelial HT-29 cells in a co-cultural model, representing the production of inflammatory cytokines. For comparison, the pure resveratrol at the same concentration did not protect the damaged HT-29 cells at all. Thus, the present study revealed that the PMAA-b-PCL-b-PMAA copolymeric micelles might be considered appropriate nanocarriers for the oral delivery of resveratrol. Full article
(This article belongs to the Special Issue Polymers for Controlled/Targeted Drug and Gene Delivery)
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16 pages, 1803 KiB  
Article
Polymer Tablet Matrix Systems for the Controlled Release of Dry Betula pendula Leaf Extract
by Dimitar Penkov, Paolina Lukova, Hristo Manev, Stela Dimitrova and Margarita Kassarova
Polymers 2023, 15(17), 3558; https://doi.org/10.3390/polym15173558 - 26 Aug 2023
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Abstract
The aim of the study was to develop polymer matrix tablets with modified release of dry Betula pendula leaf extract and to investigate basic parameters influencing the drug release pattern. To fully assess the statistical significance of the influence of the individual factors [...] Read more.
The aim of the study was to develop polymer matrix tablets with modified release of dry Betula pendula leaf extract and to investigate basic parameters influencing the drug release pattern. To fully assess the statistical significance of the influence of the individual factors in the tablet formulation development as well as the combination of them, Tukey’s tests and a complete 33 factor analysis of variance (ANOVA) were applied. The following three factors were studied at three levels (low, medium and high): influence of the hydrophobic/hydrophilic polymer ratio Ethylcellulose (EC)/Hydroxypropyl methylcellulose (HPMC) (40/60, 25/75 and 10/90), influence of HPMC molecular weight (500 kDa, 750 kDa and 1150 kDa), and influence of the compression force applied (1 t, 1.5 t and 2 t). The effect of these varied parameters on the drug release parameter t80 was evaluated statistically. Twenty-seven tablet models were formulated, including all possible combinations of the variables. The obtained drug release profiles demonstrated that a 25/75 (EC/HPMC) ratio was the most suitable for prolonging the release process. Increasing the molecular weight of HMPC from 500 kDa to 750–1150 kDa and applying higher compression force significantly influenced the studied t80 values and caused sustained drug release (t80 up to 7.97 h). The combination of the hydrophilic HPMC polymer with the hydrophobic EC can result in the formation of a promising drug-carrying matrix, offering effective control of the drug release process. Full article
(This article belongs to the Special Issue Polymers for Controlled/Targeted Drug and Gene Delivery)
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Review

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25 pages, 2167 KiB  
Review
Novel Fucoidan Pharmaceutical Formulations and Their Potential Application in Oncology—A Review
by Nikolay Zahariev, Plamen Katsarov, Paolina Lukova and Bissera Pilicheva
Polymers 2023, 15(15), 3242; https://doi.org/10.3390/polym15153242 - 29 Jul 2023
Cited by 2 | Viewed by 1700
Abstract
Fucoidan belongs to the family of marine sulfated, L-fucose-rich polysaccharides found in the cell wall matrix of various brown algae species. In the last few years, sulfated polysaccharides have attracted the attention of researchers due to their broad biological activities such as anticoagulant, [...] Read more.
Fucoidan belongs to the family of marine sulfated, L-fucose-rich polysaccharides found in the cell wall matrix of various brown algae species. In the last few years, sulfated polysaccharides have attracted the attention of researchers due to their broad biological activities such as anticoagulant, antithrombotic, antidiabetic, immunomodulatory, anticancer and antiproliferative effects. Recently the application of fucoidan in the field of pharmaceutical technology has been widely investigated. Due to its low toxicity, biocompatibility and biodegradability, fucoidan plays an important role as a drug carrier for the formulation of various drug delivery systems, especially as a biopolymer with anticancer activity, used for targeted delivery of chemotherapeutics in oncology. Furthermore, the presence of sulfate residues with negative charge in its structure enables fucoidan to form ionic complexes with oppositely charged molecules, providing relatively easy structure-forming properties in combination with other polymers. The aim of the present study was to overview essential fucoidan characteristics, related to its application in the development of pharmaceutical formulations as a single drug carrier or in combinations with other polymers. Special focus was placed on micro- and nanosized drug delivery systems with polysaccharides and their application in the field of oncology. Full article
(This article belongs to the Special Issue Polymers for Controlled/Targeted Drug and Gene Delivery)
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