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Design of Novel Polymeric Systems for Controlled Drug Delivery

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A special issue of Pharmaceutics (ISSN 1999-4923). This special issue belongs to the section "Drug Delivery and Controlled Release".

Deadline for manuscript submissions: closed (30 September 2021) | Viewed by 25154

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Prof. Dr. Janusz Kasperczyk

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1. Faculty of Pharmaceutical Sciences, Medical University of Silesia, Katowice, Poland
2. Centre of Polymer and Carbon Materials, Polish Academy of Sciences, Zabrze, Poland
Interests: polymeric drug delivery systems; influence of polymer chain structure for drug release; NMR spectroscopy for medical applications; polymer medical devices; resorbable implants containing drugs
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Special Issue Information

Dear Colleagues,

Over the past decades, controlled drug delivery systems has become one of the most progressive scientific fields. The ability to control the structure of polymer chains in the process of polymer synthesis allows for the obtaining of polymeric drug carriers with strictly programmed physical and mechanical properties. The appropriate selection of such materials makes it possible to control the kinetics of drug release.

This Special Issue is dedicated to recent advances in the design and construction of DDS for the controlled release of pharmaceutically active substances using both biodegradable and stable polymer materials. It is dedicated to all types of drug forms for the construction of which polymers were used: micro and nanospheres, polymer micelles, targeted therapy systems, resorbable implants containing pharmaceutically active substances, coatings for stable implants releasing drugs including stents, implants in the form of microfibers or nano-nonwovens obtained by electrospinning including multidrug therapy, conjugates, nanotubes, polymerosomes, nanoparticles, etc. The discussion of the manufacturing of the advanced novel polymeric systems and their application in the pharmaceutical field is also welcome.

It is our pleasure to invite you to contribute a manuscript to this Special Issue. Full research papers, short communications, and reviews are all welcome.

The list of keywords below is not exhaustive, but it may help in preparing your submission. Please do not hesitate to go beyond it or to submit a paper whose topic is not explicitly mentioned in this list.

Best regards

Prof. Dr. Janusz Kasperczyk
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. Pharmaceutics is an international peer-reviewed open access monthly 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 2900 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

Drug delivery
Degradable polymers
Smart polymers
Controlled release
Pharmacokinetics
Structure–property relationship
NMR
Chain microstructure
Nonwovens
Self-assembly
Shape memory polymers
Electrospinning
Nanotubes
Conjugates
Polymerosomes
Microspheres
Micelles
Polymer nanoparticles
Thermoresponsive nanogels
Microcarrier
Drug delivery
Sensors
Stimuli responding hydrogels
Targeted therapy
Coatings
DDS

Published Papers (9 papers)

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Research

15 pages, 40523 KiB

Open AccessArticle

Electrospun Nanofiber and Cryogel of Polyvinyl Alcohol Transdermal Patch Containing Diclofenac Sodium: Preparation, Characterization and In Vitro Release Studies

by Shafizah Sa’adon, Mohamed Nainar Mohamed Ansari, Saiful Izwan Abd Razak, Abdul Halim Mohd Yusof, Ahmad Athif Mohd Faudzi, Suresh Sagadevan, Nadirul Hasraf Mat Nayan, Joseph Sahaya Anand and Khairul Anuar Mat Amin

Pharmaceutics 2021, 13(11), 1900; https://doi.org/10.3390/pharmaceutics13111900 - 09 Nov 2021

Cited by 12 | Viewed by 3245

Abstract

Transdermal drug delivery systems (TDDS) have drawn more interest from pharmaceutical scientists because they could provide steady blood levels and prevent the first-pass metabolism over a longer period. Polyvinyl alcohol (PVA) has been widely used in this application due to its biocompatibility, non-toxicity, nanofiber and hydrogel-forming ability. Despite those benefits, their morphology would easily be destroyed by continuous water absorption and contribute to burst drug release due to its hydrophilicity. The aim of this study was to prepare the diclofenac sodium (DS)-medicated dual layer PVA patch using a combination of electrospinning and cryogelation (freeze–thaw) methods to improve the physicochemical properties and drug compatibility and investigate the release of the DS-medicated dual layer PVA patch. Morphological observations using scanning electron microscopy (SEM) verified the polymer−polymer interaction between both layers, whereas Fourier transform infrared (FTIR) spectroscopy has demonstrated the compatibility of DS in PVA matrix up to 2% w/v of PVA volume. The DS loads were found amorphously distributed efficaciously in PVA matrix as no visible spectra of DS–PVA interaction were detected. The DS-medicated dual layer PVA patch with a thicker nanofiber layer (3-milliliter running volume), three freeze–thaw cycles and 2% DS loading labeled as 2%DL_B3C show the lowest swelling capacity (18.47%). The in vitro assessment using Franz diffusion cells showed that the 2%DL_B3C indicates a better sustained release of DS, with 53.26% of the DS being released after 12 h. The 2%DL_B3C owned a flux (J_ss) of 0.256 mg/cm²/h and a permeability coefficient (K_p) value of 0.020 cm/h. Thus, the results demonstrate that DS-medicated dual layer PVA patches prepared via a combination of electrospinning and cryogelation are capable of releasing drugs for up to 24 h and can serve as a drug reservoir in the skin, thereby extending the pharmacologic effects of DS. Full article

(This article belongs to the Special Issue Design of Novel Polymeric Systems for Controlled Drug Delivery)

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17 pages, 3007 KiB

Open AccessArticle

Comparison of PLA-Based Micelles and Microspheres as Carriers of Epothilone B and Rapamycin. The Effect of Delivery System and Polymer Composition on Drug Release and Cytotoxicity against MDA-MB-231 Breast Cancer Cells

by Katarzyna Jelonek, Alicja Zajdel, Adam Wilczok, Bożena Kaczmarczyk, Monika Musiał-Kulik, Anna Hercog, Aleksander Foryś, Małgorzata Pastusiak and Janusz Kasperczyk

Pharmaceutics 2021, 13(11), 1881; https://doi.org/10.3390/pharmaceutics13111881 - 05 Nov 2021

Cited by 9 | Viewed by 1996

Abstract

Co-delivery of epothilone B (EpoB) and rapamycin (Rap) increases cytotoxicity against various kinds of cancers. However, the current challenge is to develop a drug delivery system (DDS) for the simultaneous delivery and release of these two drugs. Additionally, it is important to understand the release mechanism, as well as the factors that affect drug release, in order to tailor this process. The aim of this study was to analyze PLA–PEG micelles along with several types of microspheres obtained from PLA or a mixture of PLA and PLA–PEG as carriers of EpoB and Rap for their drug release properties and cytotoxicity against breast cancer cells. The study showed that the release process of EpoB and Rap from a PLA-based injectable delivery systems depends on the type of DDS, morphology, and polymeric composition (PLA to PLA–PEG ratio). These factors also affect the biological activity of the DDS, because the cytotoxic effect of the drugs against MDA-MB-231 cells depends on the release rate. The release process from all kinds of DDS was well-characterized by the Peppas–Sahlin model and was mainly controlled by Fickian diffusion. The conducted analysis allowed also for the selection of PLA 50/PLA–PEG 50 microspheres and PLA–PEG micelles as a promising co-delivery system of EpoB and Rap. Full article

(This article belongs to the Special Issue Design of Novel Polymeric Systems for Controlled Drug Delivery)

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20 pages, 5240 KiB

Open AccessArticle

Hyaluronic Acid Hydrogels for Controlled Pulmonary Drug Delivery—A Particle Engineering Approach

by Dariush Nikjoo, Irès van der Zwaan, Mikael Brülls, Ulrika Tehler and Göran Frenning

Pharmaceutics 2021, 13(11), 1878; https://doi.org/10.3390/pharmaceutics13111878 - 05 Nov 2021

Cited by 20 | Viewed by 3181

Abstract

Hydrogels warrant attention as a potential material for use in sustained pulmonary drug delivery due to their swelling and mucoadhesive features. Herein, hyaluronic acid (HA) is considered a promising material due to its therapeutic potential, the effect on lung inflammation, and possible utility as an excipient or drug carrier. In this study, the feasibility of using HA hydrogels (without a model drug) to engineer inhalation powders for controlled pulmonary drug delivery was assessed. A combination of chemical crosslinking and spray-drying was proposed as a novel methodology for the preparation of inhalation powders. Different crosslinkers (urea; UR and glutaraldehyde; GA) were exploited in the hydrogel formulation and the obtained powders were subjected to extensive characterization. Compositional analysis of the powders indicated a crosslinked structure of the hydrogels with sufficient thermal stability to withstand spray drying. The obtained microparticles presented a spherical shape with mean diameter particle sizes from 2.3 ± 1.1 to 3.2 ± 2.9 μm. Microparticles formed from HA crosslinked with GA exhibited a reasonable aerosolization performance (fine particle fraction estimated as 28 ± 2%), whereas lower values were obtained for the UR-based formulation. Likewise, swelling and stability in water were larger for GA than for UR, for which the results were very similar to those obtained for native (not crosslinked) HA. In conclusion, microparticles could successfully be produced from crosslinked HA, and the ones crosslinked by GA exhibited superior performance in terms of aerosolization and swelling. Full article

(This article belongs to the Special Issue Design of Novel Polymeric Systems for Controlled Drug Delivery)

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12 pages, 2296 KiB

Open AccessArticle

L-Menthol-Loadable Electrospun Fibers of PMVEMA Anhydride for Topical Administration

by Amalia Mira, Marta Rubio-Camacho, David Alarcón, Enrique Rodríguez-Cañas, Asia Fernández-Carvajal, Alberto Falco and Ricardo Mallavia

Pharmaceutics 2021, 13(11), 1845; https://doi.org/10.3390/pharmaceutics13111845 - 03 Nov 2021

Cited by 4 | Viewed by 2108

Abstract

Poly(methyl vinyl ether-alt-maleic anhydride) (PMVEMA) of 119 and 139 molecular weights (P119 and P139, respectively) were electrospun to evaluate the resulting fibers as a topical delivery vehicle for (L-)menthol. Thus, electrospinning parameters were optimized for the production of uniform bead-free fibers from 12% w/w PMVEMA (±2.3% w/w menthol) solutions, and their morphology and size were characterized by field emission scanning electron microscopy (FESEM). The fibers of P119 (F₁₁₉s) and P139 (F₁₃₉s) showed average diameter sizes of approximately 534 and 664 nm, respectively, when unloaded, and 837 and 1369 nm when loaded with menthol. The morphology of all types of fibers was cylindrical except for F₁₃₉s, which mostly displayed a double-ribbon-like shape. Gas chromatography-mass spectrometry (GC-MS) analysis determined that not only was the menthol encapsulation efficiency higher in F₁₃₉s (92% versus 68% in F₁₁₉s) but also that its stability over time was higher, given that in contrast with F₁₁₉s, no significant losses in encapsulated menthol were detected in the F₁₃₉s after 10 days post-production. Finally, in vitro biological assays showed no significant induction of cytotoxicity for any of the experimental fibers or in the full functionality of the encapsulated menthol, as it achieved equivalent free-menthol levels of activation of its specific receptor, the (human) transient receptor potential cation channel subfamily M (melastatin) member 8 (TRPM8). Full article

(This article belongs to the Special Issue Design of Novel Polymeric Systems for Controlled Drug Delivery)

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23 pages, 3743 KiB

Open AccessArticle

Multilayer Films Based on Chitosan/Pectin Polyelectrolyte Complexes as Novel Platforms for Buccal Administration of Clotrimazole

by Joanna Potaś, Emilia Szymańska, Magdalena Wróblewska, Izabela Kurowska, Mateusz Maciejczyk, Anna Basa, Eliza Wolska, Agnieszka Zofia Wilczewska and Katarzyna Winnicka

Pharmaceutics 2021, 13(10), 1588; https://doi.org/10.3390/pharmaceutics13101588 - 30 Sep 2021

Cited by 24 | Viewed by 2827

Abstract

Buccal films are recognized as easily applicable, microbiologically stable drug dosage forms with good retentivity at the mucosa intended for the therapy of oromucosal conditions, especially infectious diseases. Multilayer films composed of layers of oppositely charged polymers separated by ionically interacting polymeric chains creating polyelectrolyte complexes represent very interesting and relatively poorly explored area. We aimed to develop the antifungal multilayer systems composed of cationic chitosan and anionic pectin as potential platforms for controlled delivery of clotrimazole. The systems were pharmaceutically characterized with regard to inter alia their release kinetics under different pH conditions, physicomechanical, or mucoadhesion properties with using an animal model of the buccal mucosa. The antifungal activity against selected Candida sp. and potential cytotoxicity with regard to human gingival fibroblasts were also evaluated. Interactions between polyions were characterized with Fourier transform infrared spectroscopy. Different clotrimazole distribution in the films layers highly affected their in vitro dissolution profile. The designed films were recognized as intelligent pH-responsive systems with strong antifungal effect and satisfactory safety profile. As addition of chitosan resulted in the improved antifungal behavior of the drug, the potential utilization of the films in resistant cases of oral candidiasis might be worth of further exploration. Full article

(This article belongs to the Special Issue Design of Novel Polymeric Systems for Controlled Drug Delivery)

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14 pages, 4932 KiB

Open AccessArticle

Preparation of Electrospun Small Intestinal Submucosa/Poly(caprolactone-co-Lactide-co-glycolide) Nanofiber Sheet as a Potential Drug Carrier

by Nguyen Thi Thu Thao, Surha Lee, Gi Ru Shin, Youngji Kang, Sangdun Choi and Moon Suk Kim

Pharmaceutics 2021, 13(2), 253; https://doi.org/10.3390/pharmaceutics13020253 - 11 Feb 2021

Cited by 6 | Viewed by 2041

Abstract

In this work, we chose small intestine submucosa (SIS) as a drug carrier because SIS possesses good biocompatibility, non-immunogenic property and bio-resorbability, and performed electrospinning for preparation of nanofiber sheets (NS). For the preparation of drug-loaded electrospun SIS nanofiber sheets as a drug carrier, we used poly(ε-caprolactone-ran-l-lactide) (PCLA) copolymers to improve the electrospinning performance of SIS. The electrospinning of SIS and PCLA provided the electrospun SIS/PCLA (S/P)-nanofiber sheet (S/P-NS) with adjustable thickness and areas. The electrospun S/P-NS showed different porosities, pore sizes, diameters and tensile strengths depending on the ratios between SIS and PCLA. The electrospun S/P-NS was used as a drug carrier of the dexamethasone (Dex) and silver sulfadiazine (AgS) drug related to anti-inflammation. Dex-loaded S/P-NS and AgS-loaded S/P-NS was successfully fabricated by the electrospinning. In the in vitro and in vivo release, we successfully confirmed the possibility for the sustained release of Dex and AgS from the Dex-S/P-NS and AgS-S/P-NS for three weeks. In addition, the sustained Dex and AgS release suppressed the macrophage infiltration. Collectively, we achieved feasible development of SIS nanofiber sheets for a sustained Dex and AgS delivery system. Full article

(This article belongs to the Special Issue Design of Novel Polymeric Systems for Controlled Drug Delivery)

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15 pages, 2243 KiB

Open AccessArticle

Structure-to-Efficacy Relationship of HPMA-Based Nanomedicines: The Tumor Spheroid Penetration Study

by Júlia Kudláčová, Lenka Kotrchová, Libor Kostka, Eva Randárová, Marcela Filipová, Olga Janoušková, Jun Fang and Tomáš Etrych

Pharmaceutics 2020, 12(12), 1242; https://doi.org/10.3390/pharmaceutics12121242 - 20 Dec 2020

Cited by 5 | Viewed by 2238

Abstract

Nanomedicines are a novel class of therapeutics that benefit from the nano dimensions of the drug carrier. These nanosystems are highly advantageous mainly within cancer treatment due to their enhanced tumor accumulation. Monolayer tumor cells frequently used in routine preclinical assessment of nanotherapeutics do not have a spatial structural architecture that allows the investigation of the penetration of nanomedicines to predict their behavior in real tumor tissue. Therefore, tumor spheroids from colon carcinoma C26 cells and glioblastoma U87-MG cells were used as 3D in vitro models to analyze the effect of the inner structure, hydrodynamic size, dispersity, and biodegradability of N-(2-hydroxypropyl)methacrylamide (HPMA) copolymer-based nanomedicines carrying anticancer drug pirarubicin (THP) on the penetration within spheroids. While almost identical penetration through spheroids of linear and star-like copolymers and also their conjugates with THP was observed, THP penetration after nanomedicines application was considerably deeper than for the free THP, thus proving the benefit of polymer carriers. The cytotoxicity of THP-polymer nanomedicines against tumor cell spheroids was almost identical as for the free THP, whereas the 2D cell cytotoxicity of these nanomedicines is usually lower. The nanomedicines thus proved the enhanced efficacy within the more realistic 3D tumor cell spheroid system. Full article

(This article belongs to the Special Issue Design of Novel Polymeric Systems for Controlled Drug Delivery)

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13 pages, 5868 KiB

Open AccessArticle

Controlled Drug Release from Biodegradable Polymer Matrix Loaded in Microcontainers Using Hot Punching

by Ritika Singh Petersen, Line Hagner Nielsen, Tomas Rindzevicius, Anja Boisen and Stephan Sylvest Keller

Pharmaceutics 2020, 12(11), 1050; https://doi.org/10.3390/pharmaceutics12111050 - 03 Nov 2020

Cited by 11 | Viewed by 2452

Abstract

Microcontainers are reservoir-based advanced drug delivery systems (DDS) that have proven to increase the bioavailibity of the small-molecule drugs, targeting of biomolecules, protection of vaccines and improved treatment of Pseudomonas aeruginosa. However, high-throughput loading of these micron-sized devices with drug has been challenging. Hot punching is a new technique that is a fast, simple and single-step process where the microdevices are themselves used as mold to punch biocompatible and biodegradable drug-polymer films, thereby loading the containers. Here, we investigate the effect of hot punching on the drug distribution as well as drug release from the loaded drug-polymer matrices. Zero-order sustained drug release is observed for the model drug Furosemide embedded in biodegradable polymer, Poly-ε-caprolactone, which is attributed to the unique spatial distribution of Furosemide during the loading process. Full article

(This article belongs to the Special Issue Design of Novel Polymeric Systems for Controlled Drug Delivery)

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18 pages, 16017 KiB

Open AccessArticle

Biodegradable Electrospun Nonwovens Releasing Propolis as a Promising Dressing Material for Burn Wound Treatment

by Mateusz Stojko, Jakub Włodarczyk, Michał Sobota, Paulina Karpeta-Jarząbek, Małgorzata Pastusiak, Henryk Janeczek, Piotr Dobrzyński, Gabriela Starczynowska, Arkadiusz Orchel, Jerzy Stojko, Olgierd Batoryna, Paweł Olczyk, Katarzyna Komosińska-Vassev, Krystyna Olczyk and Janusz Kasperczyk

Pharmaceutics 2020, 12(9), 883; https://doi.org/10.3390/pharmaceutics12090883 - 17 Sep 2020

Cited by 20 | Viewed by 3566

Abstract

The selection of dressing is crucial for the wound healing process. Traditional dressings protect against contamination and mechanical damage of an injured tissue. Alternatives for standard dressings are regenerating systems containing a polymer with an incorporated active compound. The aim of this research was to obtain a biodegradable wound dressing releasing propolis in a controlled manner throughout the healing process. Dressings were obtained by electrospinning a poly(lactide-co-glycolide) copolymer (PLGA) and propolis solution. The experiment consisted of in vitro drug release studies and in vivo macroscopic treatment evaluation. In in vitro studies released active compounds, the morphology of nonwovens, chemical composition changes of polymeric material during degradation process, weight loss and water absorption were determined. For in vivo research, four domestic pigs, were used. The 21-day experiment consisted of observation of healing third-degree burn wounds supplied with PLGA 85/15 nonwovens without active compound, with 5 wt % and 10 wt % of propolis, and wounds rinsed with NaCl. The in vitro experiment showed that controlling the molar ratio of lactidyl to glycolidyl units in the PLGA copolymer gives the opportunity to change the release profile of propolis from the nonwoven. The in vivo research showed that PLGA nonwovens with propolis may be a promising dressing material in the treatment of severe burn wounds. Full article

(This article belongs to the Special Issue Design of Novel Polymeric Systems for Controlled Drug Delivery)

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