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Innovative Polymers 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 (31 May 2022) | Viewed by 23043

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Special Issue Editor

Dr. Vanessa Andrés-Guerrero

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Guest Editor

Innovation, Therapy and Pharmaceutical Development in Ophthalmology (InnOftal) Research Group, UCM 920415, Department of Pharmaceutics and Food Technology, Faculty of Pharmacy, Complutense University of Madrid, Plaza Ramón y Cajal s/n, 28040 Madrid, Spain
Interests: drug delivery; controlled release; ophthalmology; pharmaceutics; biopharmaceutics; microtechnology; nanotechnology; in situ gelling systems; biomaterials; biodegradable polymers; pharmaceutical technology; ocular drug delivery

Special Issue Information

Dear Colleagues,

The development of drug delivery systems is among the most active areas of pharmaceutical research. The search for new drug delivery systems to improve the efficacy of specific drugs, such as peptides, proteins, nucleic acid-based drugs, or even conventional organic drugs, is one of the frontier research areas. The materials used must be non-toxic and give appropriate structural and functional characteristics, such as being easily workable, processed, and engineered in order to obtain the desired system, so as to be applied in drug delivery and targeting. In addition, they have to be able to provide the appropriate characteristics in terms of drug release, performance, and tolerance, according to the selected route of administration.

This Special Issue is addressed to those authors who are currently engaged in the development and evaluation of innovative polymers that play an important role in controlled release applications.

Dr. Vanessa Andrés-Guerrero
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.

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Keywords

controlled release
polymers
drug delivery
intracellular delivery
polymer therapeutics
polymer innovation
microsystems
nanosystems
pharmaceutical technology

Published Papers (6 papers)

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Research

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15 pages, 3361 KiB

Open AccessArticle

Integrating Inflammation-Responsive Prodrug with Electrospun Nanofibers for Anti-Inflammation Application

by Jingjing Ye, Min Gong, Jian Song, Shu Chen, Qinghan Meng, Rui Shi, Liqun Zhang and Jiajia Xue

Pharmaceutics 2022, 14(6), 1273; https://0-doi-org.brum.beds.ac.uk/10.3390/pharmaceutics14061273 - 15 Jun 2022

Cited by 10 | Viewed by 2049

Abstract

Chronic inflammation plays a side effect on tissue regeneration, greatly inhibiting the repair or regeneration of tissues. Conventional local delivery of anti-inflammation drugs through physical encapsulation into carriers face the challenges of uncontrolled release. The construction of an inflammation-responsive prodrug to release anti-inflammation drugs depending on the occurrence of inflammation to regulate chronic inflammation is of high need. Here, we construct nanofiber-based scaffolds to regulate the inflammation response of chronic inflammation during tissue regeneration. An inflammation-sensitive prodrug is synthesized by free radical polymerization of the indomethacin-containing precursor, which is prepared by the esterification of N-(2-hydroxyethyl) acrylamide with the anti-inflammation drug indomethacin. Then, anti-inflammation scaffolds are constructed by loading the prodrug in poly(ε-caprolactone)/gelatin electrospun nanofibers. Cholesterol esterase, mimicking the inflammation environment, is adopted to catalyze the hydrolysis of the ester bonds, both in the prodrug and the nanofibers matrix, leading to the generation of indomethacin and the subsequent release to the surrounding. In contrast, only a minor amount of the drug is released from the scaffold, just based on the mechanism of hydrolysis in the absence of cholesterol esterase. Furthermore, the inflammation-responsive nanofiber scaffold can effectively inhibit the cytokines secreted from RAW264.7 macrophage cells induced by lipopolysaccharide in vitro studies, highlighting the great potential of these electrospun nanofiber scaffolds to be applied for regulating the chronic inflammation in tissue regeneration. Full article

(This article belongs to the Special Issue Innovative Polymers for Controlled Drug Delivery)

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13 pages, 3186 KiB

Open AccessArticle

Coupling of Fused Deposition Modeling and Inkjet Printing to Produce Drug Loaded 3D Printed Tablets

by Laura Andrade Junqueira, Atabak Ghanizadeh Tabriz, Francisco José Raposo, Luana Rocha Carobini, Urias Pardócimo Vaz, Marcos Antônio Fernandes Brandão, Dennis Douroumis and Nádia Rezende Barbosa Raposo

Pharmaceutics 2022, 14(1), 159; https://0-doi-org.brum.beds.ac.uk/10.3390/pharmaceutics14010159 - 10 Jan 2022

Cited by 14 | Viewed by 3536

Abstract

In the current study, we have coupled Fused Deposition Modelling (FDM) for the fabrication of plain polyvinyl alcohol (PVA) tablets followed by dispensing of minoxidil ethanolic solutions using inkjet printing. The use of a drop-on-solid printing approach facilitates an accurate and reproducible process while it controls the deposition of the drug amounts. For the purpose of the study, the effect of the solvent was investigated and minoxidil ink solutions of ethanol 70% v/v (P70) or absolute ethanol (P100) were applied on the plain PVA tablets. Physicochemical characterization showed that solvent miscibility with the polymer substrate plays a key role and can lead to the formation of drug crystals on the surface or drug absorption in the polymer matrix. The produced minoxidil tablets showed sustained release profiles or initial bursts strongly affected by the solvent grade used for dispensing the required dose on drug loaded 3D printed tablets. This paradigm demonstrates that the coupling of FDM and inkjet printing technologies could be used for rapid development of personalized dosage forms. Full article

(This article belongs to the Special Issue Innovative Polymers for Controlled Drug Delivery)

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36 pages, 23914 KiB

Open AccessArticle

Sustained In Vitro and In Vivo Delivery of Metformin from Plant Pollen-Derived Composite Microcapsules

by Noha M. Meligi, Amro K. F. Dyab and Vesselin N. Paunov

Pharmaceutics 2021, 13(7), 1048; https://0-doi-org.brum.beds.ac.uk/10.3390/pharmaceutics13071048 - 09 Jul 2021

Cited by 11 | Viewed by 4191

Abstract

We developed a dual microencapsulation platform for the type 2 diabetes drug metformin (MTF), which is aimed to increase its bioavailability. We report the use of Lycopodium clavatum sporopollenin (LCS), derived from their natural spores, and raw Phoenix dactylifera L. (date palm) pollens (DPP) for MTF microencapsulation. MTF was loaded into LCS and DPP via a vacuum and a novel method of hydration-induced swelling. The loading capacity (LC) and encapsulation efficiency (EE) percentages for MTF-loaded LCS and MTF-loaded DPP microcapsules were 14.9% ± 0.7, 29.8 ± 0.8, and 15.2% ± 0.7, 30.3 ± 1.0, respectively. The release of MTF from MTF-loaded LCS microcapsules was additionally controlled by re-encapsulating the loaded microcapsules into calcium alginate (ALG) microbeads via ionotropic gelation, where the release of MTF was found to be significantly slower and pH-dependent. The pharmacokinetic parameters, obtained from the in vivo study, revealed that the relative bioavailability of the MTF-loaded LCS-ALG beads was 1.215 times higher compared to pure MTF, following oral administration of a single dose equivalent to 25 mg/kg body weight MTF to streptozotocin (STZ)-induced diabetic male Sprague-Dawley rats. Significant hypoglycemic effect was obtained for STZ-induced diabetic rats orally treated with MTF-loaded LCS-ALG beads compared to control diabetic rats. Over a period of 29 days, the STZ-induced diabetic rats treated with MTF-loaded LCS-ALG beads showed a decrease in the aspartate aminotransferase (AST), alanine aminotransferase (ALT), triglycerides, cholesterol, and low-density lipoprotein-cholesterol (LDL-C) levels, as well as an increase in glutathione peroxidase (GPx) and a recovery in the oxidative stress biomarker, lipid peroxidation (LPx). In addition, histopathological studies of liver, pancreas, kidney, and testes suggested that MTF-loaded LCS-ALG beads improved the degenerative changes in organs of diabetic rats. The LCS-ALG platform for dual encapsulation of MTF achieved sustained MTF delivery and enhancement of bioavailability, as well as the improved biochemical and histopathological characteristics in in vivo studies, opening many other intriguing applications in sustained drug delivery. Full article

(This article belongs to the Special Issue Innovative Polymers for Controlled Drug Delivery)

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15 pages, 30487 KiB

Open AccessArticle

The Effect of a Triple Combination of Bevacizumab, Sodium Hyaluronate and a Collagen Matrix Implant in a Trabeculectomy Animal Model

by Vanessa Andrés-Guerrero, Irene Camacho-Bosca, Liseth Salazar-Quiñones, Nestor Ventura-Abreu, Mercedes Molero-Senosiain, Samuel Hernández-Ruiz, Guillermo Bernal-Sancho, Rocío Herrero-Vanrell and Julián García-Feijóo

Pharmaceutics 2021, 13(6), 896; https://0-doi-org.brum.beds.ac.uk/10.3390/pharmaceutics13060896 - 17 Jun 2021

Cited by 2 | Viewed by 2023

Abstract

Currently available anti-scarring treatments for glaucoma filtration surgery (GFS) have potentially blinding complications, so there is a need for alternative and safer agents. The effects of the intrableb administration of a new combination of the anti-VEGF bevacizumab, sodium hyaluronate and a collagen matrix implant were investigated in a rabbit model of GFS, with the purpose of modulating inflammation, angiogenesis, fibroblast migration and fibrogenesis in the wound healing process. A comparative-effectiveness study was performed with twenty-four rabbits, randomly assigned to the following treatments: (a) biodegradable collagen matrix implant (Olo), (b) bevacizumab-loaded collagen matrix implant (Olo-BVZ), (c) bevacizumab-loaded collagen matrix implant combined with sodium hyaluronate (Olo-BVZ-H5) and (d) sham-operated animals (control). Rabbits underwent a conventional trabeculectomy and were studied over 30 days in terms of intraocular pressure and bleb characterization (height, area and vascularity in central, peripheral and non-bleb zones). Histologic differences among groups were further evaluated at day 30 (inflammation, total cellularity and degree of fibrosis in the area of surgery). Local delivery of bevacizumab (Olo-BVZ and Olo-BVZ-H5) increased the survival of the filtering bleb by 21% and 31%, respectively, and generated a significant decrease in inflammation and cell infiltration histologically 30 days after surgery, without exhibiting any local toxic effects. Olo-BVZ-H5 showed less lymphocyte infiltration and inflammation than the rest of the treatments. Intraoperative intrableb implantation of bevacizumab, sodium hyaluronate and a collagen matrix may provide an improved trabeculectomy outcome in this model of intense wound healing. This study showed an effective procedure with few surgical complications and a novel combination of active compounds that offer new possibilities to improve the efficacy of filtration surgery. Full article

(This article belongs to the Special Issue Innovative Polymers for Controlled Drug Delivery)

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Review

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37 pages, 5300 KiB

Open AccessReview

Polymeric Hydrogels for Controlled Drug Delivery to Treat Arthritis

by Anuradha Gupta, Jungmi Lee, Torsha Ghosh, Van Quy Nguyen, Anup Dey, Been Yoon, Wooram Um and Jae Hyung Park

Pharmaceutics 2022, 14(3), 540; https://0-doi-org.brum.beds.ac.uk/10.3390/pharmaceutics14030540 - 28 Feb 2022

Cited by 18 | Viewed by 5680

Abstract

Rheumatoid arthritis (RA) and osteoarthritis (OA) are disabling musculoskeletal disorders that affect joints and cartilage and may lead to bone degeneration. Conventional delivery of anti-arthritic agents is limited due to short intra-articular half-life and toxicities. Innovations in polymer chemistry have led to advancements in hydrogel technology, offering a versatile drug delivery platform exhibiting tissue-like properties with tunable drug loading and high residence time properties This review discusses the advantages and drawbacks of polymeric materials along with their modifications as well as their applications for fabricating hydrogels loaded with therapeutic agents (small molecule drugs, immunotherapeutic agents, and cells). Emphasis is given to the biological potentialities of hydrogel hybrid systems/micro-and nanotechnology-integrated hydrogels as promising tools. Applications for facile tuning of therapeutic drug loading, maintaining long-term release, and consequently improving therapeutic outcome and patient compliance in arthritis are detailed. This review also suggests the advantages, challenges, and future perspectives of hydrogels loaded with anti-arthritic agents with high therapeutic potential that may alter the landscape of currently available arthritis treatment modalities. Full article

(This article belongs to the Special Issue Innovative Polymers for Controlled Drug Delivery)

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30 pages, 1432 KiB

Open AccessReview

Stimuli-Responsive Polymers for Transdermal, Transmucosal and Ocular Drug Delivery

by Dmitriy Berillo, Zharylkasyn Zharkinbekov, Yevgeniy Kim, Kamila Raziyeva, Kamila Temirkhanova and Arman Saparov

Pharmaceutics 2021, 13(12), 2050; https://0-doi-org.brum.beds.ac.uk/10.3390/pharmaceutics13122050 - 01 Dec 2021

Cited by 16 | Viewed by 4101

Abstract

Despite their conventional and widespread use, oral and intravenous routes of drug administration face several limitations. In particular, orally administered drugs undergo enzymatic degradation in the gastrointestinal tract and first-pass metabolism in the liver, which tend to decrease their bioavailability. Intravenous infusions of medications are invasive, painful and stressful for patients and carry the risk of infections, tissue damage and other adverse reactions. In order to account for these disadvantages, alternative routes of drug delivery, such as transdermal, nasal, oromucosal, ocular and others, have been considered. Moreover, drug formulations have been modified in order to improve their storage stability, solubility, absorption and safety. Recently, stimuli-responsive polymers have been shown to achieve controlled release and enhance the bioavailability of multiple drugs. In this review, we discuss the most up-to-date use of stimuli-responsive materials in order to optimize the delivery of medications that are unstable to pH or undergo primary metabolism via transdermal, nasal, oromucosal and ocular routes. Release kinetics, diffusion parameters and permeation rate of the drug via the mucosa or skin are discussed as well. Full article

(This article belongs to the Special Issue Innovative Polymers for Controlled Drug Delivery)

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