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Polymeric Carrier Systems Enabling Transdermal Drug Delivery

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A special issue of Polymers (ISSN 2073-4360). This special issue belongs to the section "Biomacromolecules, Biobased and Biodegradable Polymers".

Deadline for manuscript submissions: closed (31 October 2021) | Viewed by 17917

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Special Issue Editors

Dr. Christian Wiraja

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Guest Editor

School of Physical and Mathematical Sciences, Nanyang Technological University, Singapore 639798, Singapore
Interests: drug delivery; polymeric and DNA-based nanocarriers; regenerative medicine; tissue engineering; cell imaging

Dr. Chenjie Xu

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Guest Editor

Department of Biomedical Engineering, City University of Hong Kong, 83 Tat Chee Avenue, Kowloon, Hong Kong, China
Interests: transdermal drug delivery; translational medicine; cellular therapy; microneedles patches; drug nanocarriers

Special Issue Information

Dear Colleagues,

In recent years, transdermal drug delivery (TDD) has been highly sought after to enable both localized and systemic therapy. Bypassing the gastro-intestinal and hepatic first-pass metabolism, TDD promises significant drug bioavailability with reduced risks of immune rejection. Moreover, TDD is non/minimally invasive, ensuring great patient compliance alongside the possibility of self-application. To this end, polymeric carrier systems (e.g., nanocarriers and microneedles) are widely explored to facilitate safe, efficacious, and well-controlled TDD. Facile preparation, flexibility in cargo moieties, tuneable release profile, and great biocompatibility are some advantages of polymer-based TDD carriers.

In this Special Issue, current efforts to develop and employ such polymeric TDD carriers are highlighted. The scope of this Special Issue will include techniques utilized to fabricate polymeric TDD carriers, methods to characterize and optimize drug loading and release profile (i.e., sustained-release, stimuli-responsiveness) as well as disease-specific adaptations for localized skin pathology and systemic diseases (e.g., diabetes mellitus).

Dr. Christian Wiraja
Dr. Chenjie Xu
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

Polymeric nanocarrier
polymeric microneedles
transdermal
drug delivery
non-invasive
localized therapy
skin diseases

Published Papers (5 papers)

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Research

15 pages, 2681 KiB

Open AccessArticle

Thermosensitive Gels Used to Improve Microneedle-Assisted Transdermal Delivery of Naltrexone

by Kevin V. Tobin, Jennifer Fiegel and Nicole K. Brogden

Polymers 2021, 13(6), 933; https://0-doi-org.brum.beds.ac.uk/10.3390/polym13060933 - 18 Mar 2021

Cited by 16 | Viewed by 3188

Abstract

Transdermal delivery of naltrexone (NTX) can be enhanced using microneedles, although micropores generated this way can reseal by 48 h in humans, which prevents further drug delivery from a formulation. Poloxamer 407 (P407) is a thermosensitive polymer that may extend microneedle-assisted NTX delivery time by creating an in situ gel depot in the skin. We characterized gelation temperature, drug release, and permeation of P407 gels containing 7% NTX-HCl. To investigate microneedle effects on NTX-HCl permeation, porcine skin was treated with microneedles (600 or 750 μm length), creating 50 or 100 micropores. The formulations were removed from the skin at 48 h to simulate the effect of micropores resealing in vivo, when drug delivery is blunted. Gelation temperature increased slightly with addition of NTX-HCl. In vitro NTX-HCl release from P407 formulations demonstrated first order release kinetics. Microneedle treatment enhanced NTX-HCl permeation both from aqueous solution controls and P407 gels. Steady-state flux was overall lower in the P407 conditions compared to the aqueous solution, though ratios of AUCs before and after gel removal demonstrate that P407 gels provide more sustained release even after gel removal. This may be beneficial for reducing the required application frequency of microneedles for ongoing treatment. Full article

(This article belongs to the Special Issue Polymeric Carrier Systems Enabling Transdermal Drug Delivery)

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19 pages, 20516 KiB

Open AccessArticle

Plumbagin-Loaded Glycerosome Gel as Topical Delivery System for Skin Cancer Therapy

by Shadab Md, Nabil A. Alhakamy, Hibah M. Aldawsari, Mohammad Husain, Nazia Khan, Mohamed A. Alfaleh, Hani Z. Asfour, Yassine Riadi, Anwar L. Bilgrami and Md Habban Akhter

Polymers 2021, 13(6), 923; https://0-doi-org.brum.beds.ac.uk/10.3390/polym13060923 - 17 Mar 2021

Cited by 27 | Viewed by 3517

Abstract

Plumbagin (PLM) is a phytochemical which has shown cytotoxicity against of cancer cells both in vitro and in vivo. However, the clinical application of PLM has been hindered due to poor aqueous solubility and low bioavailability. The aim of the present study was to develop, optimize and evaluate PLM-loaded glycerosome (GM) gel and compare with conventional liposome (CL) for therapeutic efficacy against skin cancer. The GM formulations were optimized by employing design expert software by 3-level 3-factor design. The prepared GMs were characterized in vitro for vesicle size, size distribution, zeta potential, vesicle deformability, drug release, skin permeation, retention, texture, antioxidant and cytotoxicity activities. The optimized formulation showed a vesicle size of 119.20 ± 15.67 nm with a polydispersity index (PDI) of 0.145 ± 0.02, the zeta potential of −27 ± 5.12 mV and entrapment efficiency of 76.42 ± 9.98%. The optimized PLM-loaded GM formulation was transformed into a pre-formed gel which was prepared using Carbopol 934 polymer. The drug diffusion fluxes of CL gel and GM-loaded gel were 23.31 ± 6.0 and 79.43 ± 12.43 µg/cm²/h, respectively. The result of texture analysis revealed the adequate hardness, cohesiveness, consistency, and viscosity of the developed GM-loaded gel compared to CL gel. The confocal images showed that glycerosomal gel has deeper skin layer penetration as compared to the control solution. GM-loaded gel treated rat skin showed significantly (p < 0.05) higher drug accumulation in the dermis, higher cytotoxicity and higher antioxidant activity as compared to CL gel and PLM suspension. Thus, findings revealed that novel GM-loaded gel could be potential carriers for therapeutic intervention in skin cancer. Full article

(This article belongs to the Special Issue Polymeric Carrier Systems Enabling Transdermal Drug Delivery)

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14 pages, 2433 KiB

Open AccessArticle

Curcumin Niosomes Prepared from Proniosomal Gels: In Vitro Skin Permeability, Kinetic and In Vivo Studies

by Tamer M. Shehata, Mahmoud M. Ibrahim and Heba S. Elsewedy

Polymers 2021, 13(5), 791; https://0-doi-org.brum.beds.ac.uk/10.3390/polym13050791 - 04 Mar 2021

Cited by 36 | Viewed by 3490

Abstract

Curcumin is a poorly water-soluble drug that is used for the treatment of inflammations, tumors, wound healing antioxidant and other diseases. In the current manuscript, it is successfully formulated into proniosome gels. The proniosomes are readily hydrated into niosomal formulations using warm water. Proniosomes were prepared using nonionic surfactants (tween 80, span 60) either solely or in combinations with cholesterol. The produced niosomal formulations were homogenous in size with vesicular sizes >343 and <1800 nm. The encapsulation efficiency percentage “EE%” of curcumin in niosomal formulations was different according to niosomal composition. It increased up to 99.74% in formulations of tween 80/Chol of 200 μmole/mL lipid concentration. Span 60/chol niosomes showed decreased curcumin EE%. Niosomal formulations showed increased SSTF and PC with enhancement ratios of more than 20-fold compared with curcumin suspension form. Kinetically, niosomes fitted to the Korsemeyer-Peppas model with non-Fickian transport according to their calculated n-values where curcumin suspension form showed Korsemeyer-Peppas kinetics with Fickian transport. Niosomal formulations deposited higher curcumin amounts in the skin compared with the suspension form. The best niosomal formulation (F9) was used for niosomal gel and emulgel fabrication. Finally, the anti-inflammatory activity of curcumin in various formulations was evaluated using a rat hind paw edema method and the % of swelling was 17.5% following 24 h in group treated with curcumin niosomal emulgel. In conclusion, this study suggests that the developed niosomal emulgel could significantly enhance the anti-inflammatory effect of curcumin and be an efficient carrier for the transdermal delivery of the drug. Full article

(This article belongs to the Special Issue Polymeric Carrier Systems Enabling Transdermal Drug Delivery)

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16 pages, 3127 KiB

Open AccessArticle

Enhancement of Curcumin Anti-Inflammatory Effect via Formulation into Myrrh Oil-Based Nanoemulgel

by Wafaa E. Soliman, Tamer M. Shehata, Maged E. Mohamed, Nancy S. Younis and Heba S. Elsewedy

Polymers 2021, 13(4), 577; https://0-doi-org.brum.beds.ac.uk/10.3390/polym13040577 - 14 Feb 2021

Cited by 31 | Viewed by 3505

Abstract

Background: Curcumin (Cur) possesses a variety of beneficial pharmacological properties including antioxidant, antimicrobial, anti-cancer and anti-inflammatory activities. Nevertheless, the low aqueous solubility and subsequent poor bioavailability greatly limits its effectiveness. Besides, the role of myrrh oil as an essential oil in treating inflammatory disorders has been recently demonstrated. The objective of the current investigation is to enhance Cur efficacy via developing Cur nanoemulgel, which helps to improve its solubility and permeability, for transdermal delivery. Methods: The formulated preparations (Cur gel, emulgel and nanoemulgel) were evaluated for their physical appearance, spreadability, viscosity, particle size, in vitro release and ex vivo drug permeation studies. The in vivo anti-inflammatory activity was estimated using the carrageenan-induced rat hind paw edema method. Results: The formulated Cur-loaded preparations exhibited good physical characteristics that were in the acceptable range of transdermal preparations. The release of Cur from gel, emulgel and nanoemulgel after 12 h was 72.17 ± 3.76, 51.93 ± 3.81 and 62.0 ± 3.9%, respectively. Skin permeation of Cur was significantly (p < 0.05) improved when formulated into nanoemulgel since it showed the best steady state transdermal flux (SSTF) value (108.6 ± 3.8 µg/cm²·h) with the highest enhancement ratio (ER) (7.1 ± 0.2). In vivo anti-inflammatory studies proved that Cur-loaded nanoemulgel displayed the lowest percent of swelling (26.6% after 12 h). Conclusions: The obtained data confirmed the potential of the nanoemulgel dosage form and established the synergism of myrrh oil and Cur as an advanced anti-inflammatory drug. Full article

(This article belongs to the Special Issue Polymeric Carrier Systems Enabling Transdermal Drug Delivery)

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19 pages, 9863 KiB

Open AccessArticle

Development of Stimuli-Responsive Chitosan/ZnO NPs Transdermal Systems for Controlled Cannabidiol Delivery

by Julia Radwan-Pragłowska, Łukasz Janus, Marek Piątkowski, Aleksandra Sierakowska, Ernest Szajna, Dalibor Matýsek and Dariusz Bogdał

Polymers 2021, 13(2), 211; https://0-doi-org.brum.beds.ac.uk/10.3390/polym13020211 - 08 Jan 2021

Cited by 12 | Viewed by 3378

Abstract

One of the most common neurological diseases is epilepsy, which not only negatively affects the quality of people’s life but also may lead to life-threatening situations when its symptoms such as seizures cannot be controlled medically. A very serious problem to be overcame is the untreatable form of this disease, which cannot be cured by any currently available medicines. Cannabidiol, which is a natural product obtained from Cannabis Sativa, brings a new hope to people suffering from drug-resistant epilepsy. However, the hydrophobic character of this compound significantly lowers its clinical efficiency. One of the promising methods of this substance bioactivity increase is delivery through the skin tissue. In this article, a new type of advanced transdermal systems based on chitosan and ZnO nanoparticles (NPs) has been developed according to Sustained Development principles. The chemical modification of the biopolymer confirmed by FT-IR method resulted in the preparation of the material with great swelling abilities and appropriate water vapor permeability. Obtained nanoparticles were investigated over their crystalline structure and morphology and their positive impact on drug loading capacity and cannabidiol controlled release was proved. The novel biomaterials were confirmed to have conductive properties and not be cytotoxic to L929 mouse fibroblasts. Full article

(This article belongs to the Special Issue Polymeric Carrier Systems Enabling Transdermal Drug Delivery)

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