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Polymer-Based Systems for Controlled Release and Targeting of Drugs

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

Deadline for manuscript submissions: closed (31 July 2019) | Viewed by 67537

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Prof. Dr. Gaetano Giammona

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Laboratory of Biocompatible Polymers, Department of “Scienze e Tecnologie Biologiche, Chimiche e Farmaceutiche” (STEBICEF), University of Palermo, Via Archirafi, 32, 90123 Palermo, Italy
Interests: synthesis and physicochemical characterization of biocompatible polymers; innovative drug delivery systems; drug and gene delivery; hydrogels; three-dimensional scaffolds; tissue engineering; regenerative medicine; targeted release; lipid-based drug delivery systems; theranostic systems
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Prof. Dr. Emanuela Fabiola Craparo

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Guest Editor

Laboratory of Biocompatible Polymers, Department of “Scienze e Tecnologie Biologiche, Chimiche e Farmaceutiche” (STEBICEF), University of Palermo, Via Archirafi 32, 90123 Palermo, Italy
Interests: functionalization and purification of biopolymers; controlled drug release; active targeting; micro- and nanoparticles; polymeric micelles; lipid-based nanostructured systems; polycations; gene therapy; imaging
Special Issues, Collections and Topics in MDPI journals

Special Issue Information

Dear Colleagues,

The need to find new advanced approaches of care for the most serious pathologies that affect humans, from the possibility of dissolving biologically-active substances (conventional organic drugs, peptides, proteins, such as antibodies, nucleic acid-based drugs (NABDs), such as siRNA, miRNA) in body fluids, to targeted therapies and personalized ones, continues, hand-in-hand, with research on new performing materials to better achieve these goals through the realization of appropriate vectors for the delivery of these bioactive molecules.

Polymeric materials can be designed and manufactured for obtaining delivery systems with appropriate characteristics in terms of drug release and performance. To be used for human applications, a polymer must be primarily biocompatible and non-toxic, and also functionalizable to give appropriate structural and functional characteristics, such as to make it easily workable,

This Special Issue aims to attract researchers who are currently working on the design and production of polymeric materials, as well as work on the search for strategies to modify existing ones for making innovative systems for drug delivery and/or regenerative medicine. In particular, we expect to receive original papers or reviews on polymeric systems, ranging from nano- to macro-structures, for drug and/or cell delivery.

Prof. Gaetano Giammona
Prof. Emanuela Fabiola Craparo
Guest Editors

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

Biocompatible polymers
Drug delivery systems
Gene therapy
Tissue engineering
Targeted drug release
Personalized medicine
Nanoparticles
Microparticles
Polyplexes

Published Papers (11 papers)

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Editorial

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3 pages, 164 KiB

Open AccessEditorial

Polymer-Based Systems for Controlled Release and Targeting of Drugs

by Gaetano Giammona and Emanuela Fabiola Craparo

Polymers 2019, 11(12), 2066; https://doi.org/10.3390/polym11122066 - 11 Dec 2019

Cited by 3 | Viewed by 1889

Abstract

The current need to find new advanced approaches to carry biologically active substances (conventional organic drugs, peptides, proteins (such as antibodies), and nucleic acid-based drugs (NABDs such as siRNA and miRNA)) in the body fluids, to realize targeted therapies and even personalized ones, [...] Read more.

(This article belongs to the Special Issue Polymer-Based Systems for Controlled Release and Targeting of Drugs)

Research

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10 pages, 2131 KiB

Open AccessArticle

Investigation of Mucoadhesion and Degradation of PCL and PLGA Microcontainers for Oral Drug Delivery

by Zarmeena Abid, Mette Dalskov Mosgaard, Giorgio Manfroni, Ritika Singh Petersen, Line Hagner Nielsen, Anette Müllertz, Anja Boisen and Stephan Sylvest Keller

Polymers 2019, 11(11), 1828; https://doi.org/10.3390/polym11111828 - 07 Nov 2019

Cited by 25 | Viewed by 3300

Abstract

Microfabricated devices have been introduced as a promising approach to overcome some of the challenges related to oral administration of drugs and, thereby, improve their oral bioavailability. In this study, we fabricate biodegradable microcontainers with different polymers, namely poly-ɛ-caprolactone (PCL), poly(lactic-co-glycolic acid) (PLGA) 50:50 and PLGA 75:25 by hot punching. The mucoadhesion of the microcontainers is assessed with an ex vivo retention model on porcine intestinal tissue. Finally, in vitro degradation studies of the biodegradable microcontainers are completed for six weeks in simulated intestinal medium with the addition of pancreatic enzymes. Through SEM inspection, the PLGA 50:50 microcontainers show the first signs of degradation already after two weeks and complete degradation within four weeks, while the other polymers slowly degrade in the medium over several weeks. Full article

(This article belongs to the Special Issue Polymer-Based Systems for Controlled Release and Targeting of Drugs)

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22 pages, 4439 KiB

Open AccessArticle

Combining Inulin Multifunctional Polycation and Magnetic Nanoparticles: Redox-Responsive siRNA-Loaded Systems for Magnetofection

by Carla Sardo, Emanuela Fabiola Craparo, Barbara Porsio, Gaetano Giammona and Gennara Cavallaro

Polymers 2019, 11(5), 889; https://doi.org/10.3390/polym11050889 - 15 May 2019

Cited by 7 | Viewed by 3245

Abstract

Superparamagnetic Iron Oxide Nanoparticles (SPIONs) are recognized as one of the most promising agents for theranostic applications. Among methods designed for siRNA delivery, magnetofection, that is, nucleic acid cell uptake under the influence of a magnetic field acting on magnetic nucleic acid vectors, is emerging as a unique approach to combining advantages such as strong improvement of the kinetics of the delivery process and the possibility of localizing nucleic acid delivery to an area where the magnetic field is applied. This paper reports on the preparation of siRNA loaded magnetoplexes—named ICD@SS@SPIONs/siRNA—by controlled crosslinking, in the presence of SPIONs, of the polycation INU-C-DETA, synthesized starting from the polysaccharide inulin by grafting diethylenetriamine and cystamine molecules. The obtained ICD@SS@SPIONs/siRNA have suitable chemical-physical characteristics to be employed for iv administration and are also able to release siRNA in a redox-triggered manner thanks to intracellular glutathione (GSH) mediated reduction of disulphide bridges formed during the crosslinking process. Moreover, ICD@SS@SPIONs/siRNA are able to produce magnetic targeting in vitro on breast cancer cells, without appreciable cyto- and hemo-toxic effects, in a wide range of concentrations. Finally, protein binding to nanoparticles revealed that obtained systems are potentially longer circulating and applicable as a smart multifunctional agents for cancer therapy. Full article

(This article belongs to the Special Issue Polymer-Based Systems for Controlled Release and Targeting of Drugs)

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16 pages, 3149 KiB

Open AccessArticle

Characterization and Optimization of PLA Stereocomplexed Hydrogels for Local Gene Delivery Systems

by Kwei-Yu Liu, Daniel G. Abebe, Elizabeth Rachel Wiley and Tomoko Fujiwara

Polymers 2019, 11(5), 796; https://doi.org/10.3390/polym11050796 - 03 May 2019

Cited by 7 | Viewed by 3650

Abstract

Localized gene delivery still remains as a challenging therapeutic method due to the multiple hurdles to overcome. One of the significant factors is a development of a matrix to carry and safely deliver genes at the local site in a controlled manner and then exit and disintegrate harmlessly. This report describes the structural and mechanistic studies on the in-situ forming hydrogels composed of the PEI/DNA multi-layered micelles to apply for gene therapy. The stereocomplexation-driven hydrogel systems from the DNA-loaded and DNA-free PLA-PEG-PLA triblock copolymer micelles that include enantiomeric polylactide blocks exhibited a sol-to-gel transitions between room and body temperatures. These hydrogels have well-described structure and compositions, and improved mechanical properties. Furthermore, the investigation of their degradation profiles and chemical analysis indicated the faster acidic degradation and stepwise degradation process of these micelle–hydrogel systems. Full article

(This article belongs to the Special Issue Polymer-Based Systems for Controlled Release and Targeting of Drugs)

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14 pages, 6716 KiB

Open AccessEditor’s ChoiceArticle

Microfluidic Based Fabrication and Characterization of Highly Porous Polymeric Microspheres

by Benzion Amoyav and Ofra Benny

Polymers 2019, 11(3), 419; https://doi.org/10.3390/polym11030419 - 05 Mar 2019

Cited by 63 | Viewed by 9529

Abstract

Polymeric porous particles are currently used for various applications in biotechnology, tissue engineering and pharmaceutical science, e.g., floating drug delivery systems and inhaled formulations. Particle shape and size depend on variable parameters; among them, polymer type and concentration, stirring speed, pH and type of solvent. In this study, porous poly(lactic-co-glycolic) acid (PLGA) and poly(d,l-lactide) (PLA) microspheres (MPs), with varying sizes and morphologies, were synthesized and optimized using both batch formulation and a flow-focusing microfluidic device. A well-established method of preparation utilizing solvent evaporation and the double emulsion technique was performed. Similar to other batch encapsulation methods, this technique is time and reagent consuming and consists of several steps. Hence, although porous structures provide tremendous opportunity in the design of new applications for tissue engineering and as improved controlled-release carriers, the synthesis of these particles with predefined properties remains challenging. We demonstrated the fabrication of porous MPs using a simple microfluidic device, compared to batch synthesis fabrication; and the effect of solvent, polymer concentration and type, post-hydrolysis treatment, on porosity degree. Moreover, a kinetic release study of fluorescent molecule was conducted for non-porous in comparison to porous particles. An overview of future prospects and the potential of these porous beads in this scientific area are discussed. Full article

(This article belongs to the Special Issue Polymer-Based Systems for Controlled Release and Targeting of Drugs)

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14 pages, 1987 KiB

Open AccessArticle

Temperature Responsive Nanoparticles Based on PEGylated Polyaspartamide Derivatives for Drug Delivery

by Guangyan Zhang and Xulin Jiang

Polymers 2019, 11(2), 316; https://doi.org/10.3390/polym11020316 - 13 Feb 2019

Cited by 14 | Viewed by 3489

Abstract

The temperature responsive PEGylated polyaspartamide derivative, denoted as mPEG-PAAHP, was synthesized by the click reaction. FTIR and ¹H NMR were adopted to characterize and confirm the chemical structures of the obtained mPEG-PAAHPs. The temperature responsive behavior investigated by transmittance and dynamic light scattering showed that some of the obtained mPEG-PAAHPs exhibited obvious temperature responsiveness and could be used to prepare nanoparticles by quickly heating. Drug paclitaxel can be encapsulated into mPEG-PAAHP based nanoparticles with a high encapsulation efficiency up to 99% (corresponding to a drug loading content of around 9.9%). Dynamic light scattering results showed that the PTX-loaded nanoparticles had a mean size around 80 nm (PDI<0.2) and good stability in PBS with 150 mM ionic strength. In vitro cytotoxicity results showed that mPEG-PAAHP did not show any toxicity to HeLa cells, but the PTX-loaded nanoparticles based on mPEG-PAAHP exhibited obvious anti-cancer activity. Thus, the temperature responsive PEGylated polyaspartamide derivative mPEG-PAAHP may be a promising drug delivery system. Full article

(This article belongs to the Special Issue Polymer-Based Systems for Controlled Release and Targeting of Drugs)

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16 pages, 3028 KiB

Open AccessArticle

Facile Preparation of Reduction-Responsive Micelles Based on Biodegradable Amphiphilic Polyurethane with Disulfide Bonds in the Backbone

by Peng Zhang, Jiaying Hu, Leran Bu, Hena Zhang, Baixiang Du, Caihong Zhu and Yuling Li

Polymers 2019, 11(2), 262; https://doi.org/10.3390/polym11020262 - 04 Feb 2019

Cited by 7 | Viewed by 3080

Abstract

In this paper, we synthesized a biodegradable amphiphilic polymer of polyurethane-polyethylene glycol with disulfide bonds in the main chain (PEG-PU(SS)-PEG). DLS and SEM showed that the polymer could self-assemble into micelles in aqueous solution and could be used to load the hydrophobic anticancer drug DOX. Intriguingly, drug release in vitro indicated that DOX-loaded PEG-PU(SS)-PEG micelles had good stability under the extracellular physiological environment, but the disulfide bonds broke rapidly and DOX was released quickly under the intracellular reducing conditions. CCK-8 assays showed that DOX-loaded PEG-PU(SS)-PEG micelles had a high in vitro antitumor activity in C6 cells, whereas blank PEG-PU(SS)-PEG micelles were nontoxic to C6 cells. It was also found that there was strong and persistent accumulation of DOX-loaded PEG-PU(SS)-PEG as compared with PEG-PU-PEG both by the cell internalization tests and the flow cytometry measurements. Hence, PEG-PU(SS)-PEG micelles will have a potential use for clinical treatment of cancer in the future. Full article

(This article belongs to the Special Issue Polymer-Based Systems for Controlled Release and Targeting of Drugs)

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16 pages, 2557 KiB

Open AccessArticle

Starch-Based Pickering Emulsions as Platforms for Topical Antibiotic Delivery: In Vitro and In Vivo Studies

by Joana Marto, Aida Duarte, Sandra Simões, Lídia Maria Gonçalves, Luís Filipe Gouveia, António José Almeida and Helena Margarida Ribeiro

Polymers 2019, 11(1), 108; https://doi.org/10.3390/polym11010108 - 10 Jan 2019

Cited by 27 | Viewed by 4944

Abstract

The present study investigated a new approach to treat superficial skin infections by topical application of minocycline hydrochloride (MH) formulated in a novel starch-based Pickering emulsion (ASt-emulsions). The emulsions were fully characterized in terms of efficacy, as well as in vitro release and permeation studies. The emulsions provided a prolonged MH release, always above its minimum inhibitory concentration against Staphylococcus aureus, although the drug did not permeate through the entire skin layer. The in vitro antibacterial activity of MHASt-emulsions against S. aureus was confirmed and their therapeutic efficacy was assessed using an in vitro skin-adapted agar diffusion test. In vivo antibacterial activity, evaluated using the tape-stripping infection model in mice, showed the topical administration of MH was effective against superficial infections caused by S. aureus. This study supports the potential of ASt-emulsions as promising platforms for topical antibiotic delivery, contributing to a new perspective on the treatment of superficial bacterial infections. Full article

(This article belongs to the Special Issue Polymer-Based Systems for Controlled Release and Targeting of Drugs)

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12 pages, 3102 KiB

Open AccessArticle

Design, Synthesis, and Characterization of Schiff Base Bond-Linked pH-Responsive Doxorubicin Prodrug Based on Functionalized mPEG-PCL for Targeted Cancer Therapy

by Yinglei Zhai, Xing Zhou, Zhiqiang Zhang, Lei Zhang, Dianyu Wang, Xinhui Wang and Wei Sun

Polymers 2018, 10(10), 1127; https://doi.org/10.3390/polym10101127 - 11 Oct 2018

Cited by 25 | Viewed by 4863

Abstract

The side effects of doxorubicin (DOX) extremely limit its application in the treatment of malignant tumors. Nano-sized polymeric drugs based on the acidic microenvironment of tissular- or intra- tumor have attracted ample attention because of their potential in reducing side effects. In this research, an amphiphilic diblock copolymer based on poly (ethylene glycol) (PEG) and functionalized polycaprolactone (PCL) was synthesized and utilized as the drug carrier. DOX was chemically conjugated with the polymer via acid-cleavable imine bonds to obtain a novel pH-sensitive DOX prodrug (mPEG-PCL-Imi-DOX). mPEG-PCL-Imi-DOX (24.2 wt % DOX content) formed micelles with an average diameter of 125 nm through a simple solvent evaporation method. The in vitro release profile demonstrated that DOX release of the prodrug micelles was pH-responsive and able to be accelerated with the decrease of pH. In vitro cytotoxicity assay tests revealed that the pH-sensitive DOX prodrug micelles exhibited relatively lower toxicity and similar antitumor efficacy towards MCF-7 cells compared with free DOX. Hence, the DOX prodrug micelles with imine bonds can offer a carrier with great potential for chemo-therapeutics. Full article

(This article belongs to the Special Issue Polymer-Based Systems for Controlled Release and Targeting of Drugs)

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12 pages, 1895 KiB

Open AccessArticle

Preparation and Evaluation of Metronidazole-Loaded Pectin Films for Potentially Targeting a Microbial Infection Associated with Periodontal Disease

by Taepin Junmahasathien, Pattaraporn Panraksa, Paytaai Protiarn, Doosadee Hormdee, Rajda Noisombut, Nutthapong Kantrong and Pensak Jantrawut

Polymers 2018, 10(9), 1021; https://doi.org/10.3390/polym10091021 - 13 Sep 2018

Cited by 28 | Viewed by 4170

Abstract

The objective of this study was to develop the metronidazole loaded high and low methoxyl pectin films (HM-G-MZ and LM-G-MZ) for the treatment of periodontal disease. The films were prepared by pectin 3% w/v, glycerin 40% w/v, and metronidazole 5% w/v. The developed films were characterized by scanning electron microscope and evaluated for thickness, weight variation, and elasticity. The developed films showing optimal mechanical properties were selected to evaluate radial swelling properties, in vitro release of metronidazole and the antimicrobial activity against Porphyromonas gingivalis and Aggregatibacter actinomycetemcomitans by the disc diffusion method. The results demonstrated that LM-MZ and HM-G-MZ films were colorless and yellowish color, respectively, with the film thickness around 0.36–0.38 mm. Furthermore, both films exhibited good elasticity with low puncture strength (1.63 ± 0.37 and 0.84 ± 0.03 N/mm², respectively) and also showed slight increase in radial swelling, so that they could be easily inserted and fitted into the periodontal pocket during a clinical use. However, HM-G-MZ showed a decrease in radial swelling after 1 h due to the film erosion. The in vitro release study of LM-G-MZ showed a burst release that was initially followed by a slow release rate profile, capable to maintain the therapeutic level in periodontal pocket for seven days, whereas HM-G-MZ showed an immediate release profile. The cumulative percentage of metronidazole release from HM-G-MZ was less than LM-G-MZ during the first 5 min as metronidazole was in a crystalline form inside HM-G-MZ film. For antimicrobial activity test, both films showed the inhibitory effect against P. gingivalis and A. actinomycetemcomitans, and there was no difference in the inhibition zone between LM-G-MZ and HM-G-MZ. The present study showed, for the first time, that low methoxyl pectin film containing glycerin and metronidazole could be potentially considered as a promising clinical tool for the drug delivery via intra-periodontal pocket to target an oral disease that is associated with polymicrobial infection. Full article

(This article belongs to the Special Issue Polymer-Based Systems for Controlled Release and Targeting of Drugs)

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Review

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24 pages, 2809 KiB

Open AccessReview

Implantable Polymeric Drug Delivery Devices: Classification, Manufacture, Materials, and Clinical Applications

by Sarah A. Stewart, Juan Domínguez-Robles, Ryan F. Donnelly and Eneko Larrañeta

Polymers 2018, 10(12), 1379; https://doi.org/10.3390/polym10121379 - 12 Dec 2018

Cited by 239 | Viewed by 24412

Abstract

The oral route is a popular and convenient means of drug delivery. However, despite its advantages, it also has challenges. Many drugs are not suitable for oral delivery due to: first pass metabolism; less than ideal properties; and side-effects of treatment. Additionally, oral delivery relies heavily on patient compliance. Implantable drug delivery devices are an alternative system that can achieve effective delivery with lower drug concentrations, and as a result, minimise side-effects whilst increasing patient compliance. This article gives an overview of classification of these drug delivery devices; the mechanism of drug release; the materials used for manufacture; the various methods of manufacture; and examples of clinical applications of implantable drug delivery devices. Full article

(This article belongs to the Special Issue Polymer-Based Systems for Controlled Release and Targeting of Drugs)

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