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Polymers
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Macromolecular Designing for Drug Delivery Systems
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Macromolecular Designing for Drug Delivery Systems

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

Deadline for manuscript submissions: closed (31 December 2021) | Viewed by 19826

Special Issue Editor

Prof. Dr. Dorota Neugebauer

E-Mail Website
Guest Editor
Department of Physical Chemistry and Technology of Polymers, Faculty of Chemistry, Silesian University of Technology, 44-100 Gliwice, Poland
Interests: amphiphilic polymers; graft copolymers; molecular brushes; micellization; drug delivery systems
Special Issues, Collections and Topics in MDPI journals

Special Issue Information

Dear Colleagues,

Studies on well-defined polymers with extraordinary architecture and characteristics have been used to develop macromolecular designing. The (pseudo)living and controlled character of polymerizations leads to the control of basic parameters of polymers, i.e., molecular weights with narrow distribution. Precisely synthesized macromolecules with chain uniformity, composition, topology, and functionality are treated as tailor-made polymers with extremely high performance. The advantageous biocompatibility of functional materials is particularly important for biomedical applications, including tissue engineering, scaffolds, diagnostics, and drug-delivery systems (DDS). The latter require the design of polymeric carriers responsible for drug transport efficiency and its controlled release profile, which is adjusted by controlled particle sizes, hydrophilic/hydrophobic balance, and topology (linear vs. star, brush, and hiperbranched). One of the functions of carriers, based on liposomes, nanospheres, hydrogels, and self-assembling micellar structures with suitable stabilities, is to extend the circulation time in the blood, which increases the effectiveness of the target action. The biological activity of the polymeric system can be increased by the addition of a second bioactive substance, leading to a system with potential application in combined therapy, which enhances treatment efficacy and allows for the restoration of a patient's health or the reduction of the risk of complications.

Prof. Dorota Neugebauer
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

  • structure design
  • polymer carriers
  • nonlinear polymers
  • amphiphilics
  • micellar systems
  • loading and release

Published Papers (5 papers)

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Research

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15 pages, 3011 KiB  
Article
Synthesis of Retinol-Loaded Lipid Nanocarrier via Vacuum Emulsification to Improve Topical Skin Delivery
by Seung-Hyun Jun, Hanul Kim, HyeJin Lee, Ji Eun Song, Sun Gyoo Park and Nea-Gyu Kang
Polymers 2021, 13(5), 826; https://doi.org/10.3390/polym13050826 - 08 Mar 2021
Cited by 14 | Viewed by 4882
Abstract
Retinol has been widely used as an anti-wrinkle active ingredient in cosmetic fields. However, the oxidation of retinol by air was one of the critical problems for application in the skincare field. In this study, Retinol-loaded lipid nanocarriers were prepared via the vacuum [...] Read more.
Retinol has been widely used as an anti-wrinkle active ingredient in cosmetic fields. However, the oxidation of retinol by air was one of the critical problems for application in the skincare field. In this study, Retinol-loaded lipid nanocarriers were prepared via the vacuum emulsification method to increase the stability of retinol vulnerable to air and optimized encapsulation conditions and to increase the penetration efficiency into skin. Optimizing the components of lipid nanocarriers, gradients of carbon chain C8-22 using various lipid species which made the amorphous structure and enough spaces to load retinol inside the capsules were estimated from the lower enthalpy change and peak shift in DSC analysis. The vacuum-assisted lipid nanocarriers (VLN) could help suppress oxidation, which could have advantages to increase the thermal stability of retinol. The retinol-loaded VLN (VLN-ROL) had narrow size distribution under 0.3 PDI value, under 200 nm scaled particle size, and fully negative surface charge of about -50 mV for the electrostatic repulsion to avoid aggregation phenomenon among the lipid nanoparticles. It maintained 90% or more retinol concentration after 4 weeks of storage at 25, 40 and 50 °C and kept stable. The VLN-ROL-containing cream showed improved penetration efficiency applied to porcine skins compared to the commercial retinol 10S from BASF. The total amount of retinol into the skin of VLN-ROL (0.1% of retinol) was enhanced by about 2.2-fold (2.86 ± 0.23 μg) higher than that in 0.1% of bare retinol (about 1.29 ± 0.09 μg). In addition, applied on a 3D Human skin model, the epidermal thickness and the relative percentage of dermal collagen area effectively increased compared to the control and retinol, respectively. Additionally, the level of secreted IL-1α was lower and epidermal damage was weaker than commercial product A. This retinol-loaded lipid nanocarrier could be a potentially superior material for cosmetics and biomedical research. Full article
(This article belongs to the Special Issue Macromolecular Designing for Drug Delivery Systems)
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16 pages, 3619 KiB  
Article
Coumarin-Containing Light-Responsive Carboxymethyl Chitosan Micelles as Nanocarriers for Controlled Release of Pesticide
by Song Feng, Junqin Wang, Lihua Zhang, Qin Chen, Wang Yue, Ni Ke and Haibo Xie
Polymers 2020, 12(10), 2268; https://doi.org/10.3390/polym12102268 - 01 Oct 2020
Cited by 34 | Viewed by 3506
Abstract
Currently, controlled release formulations (CRFs) of pesticides in response to biotic and/or abiotic stimuli have shown great potential for providing “on-demand” smart release of loaded active ingredients. In this study, amphiphilic biopolymers were prepared by introducing hydrophobic (7-diethylaminocoumarin-4-yl)methyl succinate (DEACMS) onto the main [...] Read more.
Currently, controlled release formulations (CRFs) of pesticides in response to biotic and/or abiotic stimuli have shown great potential for providing “on-demand” smart release of loaded active ingredients. In this study, amphiphilic biopolymers were prepared by introducing hydrophobic (7-diethylaminocoumarin-4-yl)methyl succinate (DEACMS) onto the main chain of hydrophilic carboxymethylchitosan (CMCS) via the formation of amide bonds which were able to self-assemble into spherical micelles in aqueous media and were utilized as light-responsive nanocarriers for the controlled release of pesticides. FTIR and NMR characterizations confirmed the successful synthesis of the CMCS-DEACMS conjugate. The critical micelle concentration (CMC) decreased with the increase in the substitution of DEACMS on CMCS, which ranged from 0.013 to 0.042 mg/mL. Upon irradiation under simulated sunlight, the hydrodynamic diameter, morphology, photophysical properties and photolysis were researched by means of dynamic light scattering (DLS), transmission electron microscopy (TEM), UV-vis absorption spectroscopy and fluorescence spectroscopy. Moreover, 2,4-dichlorophenoxyacetic acid (2,4-D) was used as a model pesticide and encapsulated into the CMCS-DEACMS micelles. In these micelle formulations, the release of 2,4-D was promoted upon simulated sunlight irradiation, during which the coumarin moieties were cleaved from the CMCS backbone, resulting in a shift of the hydrophilic–hydrophobic balance and destabilization of the micelles. Additionally, bioassay studies suggested that this 2,4-D contained which micelles showed good bioactivity on the target plant without harming the nontarget plant. Thereby, the light-responsive CMCS-DEACMS micelles bearing photocleavable coumarin moieties provide a smart delivery platform for agrochemicals. Full article
(This article belongs to the Special Issue Macromolecular Designing for Drug Delivery Systems)
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14 pages, 1981 KiB  
Article
Synthesis and Characterization of Ionic Graft Copolymers: Introduction and In Vitro Release of Antibacterial Drug by Anion Exchange
by Katarzyna Niesyto and Dorota Neugebauer
Polymers 2020, 12(9), 2159; https://doi.org/10.3390/polym12092159 - 22 Sep 2020
Cited by 14 | Viewed by 2788
Abstract
Amphiphilic graft copolymers based on [2-(methacryloyloxy)ethyl]trimethyl- ammonium chloride (TMAMA) were obtained for the delivery of pharmaceutical ionic drugs, such as p-aminosalicylate (PAS) and clavunate (CLV) anions. The side chains were attached by grafting from a multifunctional macroinitiator via atom transfer radical polymerization [...] Read more.
Amphiphilic graft copolymers based on [2-(methacryloyloxy)ethyl]trimethyl- ammonium chloride (TMAMA) were obtained for the delivery of pharmaceutical ionic drugs, such as p-aminosalicylate (PAS) and clavunate (CLV) anions. The side chains were attached by grafting from a multifunctional macroinitiator via atom transfer radical polymerization (ATRP) to get polymers with different grafting degrees and ionic content. The self-assembling ability, confirmed by determining the critical micelle concentration (CMC) through interfacial tension (IFT) with the use of goniometry, was reduced after ion exchange (CMC twice higher than for chloride anions contained copolymers 0.005–0.026 mg/mL). Similarly, the hydrophilicity level (adjusted by the content of ionic fraction) evaluated by the water contact angle (WCA) of the polymer film surfaces was decreased with the increase of trimethylammonium units (68°–44°) and after introduction of pharmaceutical anions. The exchange of Cl− onto PAS− and CLV− in the polymer matrix was yielded at 31%–64% and 79%–100%, respectively. The exchange onto phosphate anions to release the drug was carried out (PAS: 20%–42%, 3.1–8.8 μg/mL; CLV: 25%–73%, 11–31 μg/mL from 1 mg of drug conjugates). Because of the bacteriostatic activity of PAS and the support of the action of the antibiotics by CLV, the designed water-soluble systems could be alternatives for the treatment of bacterial infections, including pneumonia and tuberculosis. Full article
(This article belongs to the Special Issue Macromolecular Designing for Drug Delivery Systems)
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18 pages, 6415 KiB  
Article
4-n-Butylresorcinol-Based Linear and Graft Polymethacrylates for Arbutin and Vitamins Delivery by Micellar Systems
by Justyna Odrobińska, Łukasz Mielańczyk and Dorota Neugebauer
Polymers 2020, 12(2), 330; https://doi.org/10.3390/polym12020330 - 05 Feb 2020
Cited by 6 | Viewed by 3018
Abstract
A novel initiator, bromoester modified 4-n-butylresorcinol (4nBREBr2), was prepared and utilized in controlled atom transfer radical polymerization (ATRP) to obtain three series of amphiphilic copolymers. The V-shaped copolymers of methyl methacrylate (MMA), 2-hydroxyethyl methacrylate (HEMA), and poly(ethylene glycol) methyl [...] Read more.
A novel initiator, bromoester modified 4-n-butylresorcinol (4nBREBr2), was prepared and utilized in controlled atom transfer radical polymerization (ATRP) to obtain three series of amphiphilic copolymers. The V-shaped copolymers of methyl methacrylate (MMA), 2-hydroxyethyl methacrylate (HEMA), and poly(ethylene glycol) methyl ether methacrylate (MPEGMA), abbreviated to P(HEMA–co–MMA), P(HEMA–co–MPEGMA), and P(MMA–co–MPEGMA), were synthesized. Moreover, P((HEMA–graft–PEG)–co–MMA) graft copolymers were prepared by combining the pre-polymerization modification of HEMA and a “click” reaction using a “grafting onto” approach. All copolymers could form micelles with encapsulated active substances (vitamin C (VitC), vitamin E (VitE), arbutin (ARB)), which are used in cosmetology. In vitro studies carried out in a PBS solution (pH 7.4) demonstrates that in most cases the maximum release of active substance was after 1 h. The polymeric systems presenting satisfactory encapsulation characteristics and release profiles are attractive micellar carriers of cosmetic substances, which show a positive effect on the skin condition. Full article
(This article belongs to the Special Issue Macromolecular Designing for Drug Delivery Systems)
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Review

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36 pages, 4385 KiB  
Review
Polymeric Drug Delivery Systems Bearing Cholesterol Moieties: A Review
by Paweł Misiak, Karolina H. Markiewicz, Dawid Szymczuk and Agnieszka Z. Wilczewska
Polymers 2020, 12(11), 2620; https://doi.org/10.3390/polym12112620 - 06 Nov 2020
Cited by 15 | Viewed by 4691
Abstract
This review aims to provide an overview of polymers comprising cholesterol moiety/ies designed to be used in drug delivery. Over the last two decades, there have been many papers published in this field, which are summarized in this review. The primary focus of [...] Read more.
This review aims to provide an overview of polymers comprising cholesterol moiety/ies designed to be used in drug delivery. Over the last two decades, there have been many papers published in this field, which are summarized in this review. The primary focus of this article is on the methods of synthesis of polymers bearing cholesterol in the main chain or as side chains. The data related to the composition, molecular weight, and molecular weight distribution of polymers are presented. Moreover, other aspects, such as forms of carriers, types of encapsulated drugs, encapsulation efficiency and capacity, are also included. Full article
(This article belongs to the Special Issue Macromolecular Designing for Drug Delivery Systems)
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