Research

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25 pages, 3388 KiB

Open AccessArticle

Development and Characterisation of a Topical Methyl Salicylate Patch: Effect of Solvents on Adhesion and Skin Permeation

by Soo Chin Yeoh, Poh Lee Loh, Vikneswaran Murugaiyah and Choon Fu Goh

Pharmaceutics 2022, 14(11), 2491; https://doi.org/10.3390/pharmaceutics14112491 - 17 Nov 2022

Cited by 2 | Viewed by 2539

Abstract

The advent of skin patch formulation design and technology has enabled the commercialisation of methyl salicylate (MS) as a topical patch. However, the most fundamental aspect of skin permeation is unknown at present. The study aims to investigate the effect of solvent choice [...] Read more.

The advent of skin patch formulation design and technology has enabled the commercialisation of methyl salicylate (MS) as a topical patch. However, the most fundamental aspect of skin permeation is unknown at present. The study aims to investigate the effect of solvent choice on the skin permeation of MS in a neat solvent system and patch formulation with an emphasis on patch adhesion. MS in six selected solvents (propylene glycol (PG), Transcutol^®, isopropyl myristate, Labrasol^®, Plurol^® oleique CC 497 and Maisine^® CC) was characterised and in vitro permeation studies were also performed. An ATR-FTIR analysis on solvent-treated skin was conudcted. Patch formulation was prepared and characterised for adhesion, in vitro drug release and skin permeation studies. The highest MS permeation was found in neat PG over 24 h (~90 μg/cm²) due to its strong skin protein conformation effect. Transcutol^® and isopropyl myristate showed better skin deposition and formulation retention, respectively. Nevertheless, PG enhanced the patch adhesion despite having a lower cumulative amount of MS permeated (~80 μg/cm²) as compared with Transcutol^® and Maisine^® (~110–150 μg/cm²). These two solvents, however, demonstrated better skin deposition and formulation retention but a lower patch adhesion. The unpredictable influence of the solvent on patch adhesion highlights the importance of the trade-off between patch adhesion and skin permeation during formulation design. Full article

(This article belongs to the Special Issue Drug Delivery and Penetration through Skin and Its Formulations)

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13 pages, 1625 KiB

Open AccessArticle

Dermal Delivery of Diclofenac Sodium—In Vitro and In Vivo Studies

by Fotis Iliopoulos, Choon Fu Goh, Tasnuva Haque, Annisa Rahma and Majella E. Lane

Pharmaceutics 2022, 14(10), 2106; https://doi.org/10.3390/pharmaceutics14102106 - 01 Oct 2022

Cited by 6 | Viewed by 2554

Abstract

Previously, we reported the use of confocal Raman spectroscopy (CRS) as a novel non-invasive approach to determine drug disposition in the skin in vivo. Results obtained by CRS were found to correlate with data from the well-established in vitro permeation test (IVPT) model [...] Read more.

Previously, we reported the use of confocal Raman spectroscopy (CRS) as a novel non-invasive approach to determine drug disposition in the skin in vivo. Results obtained by CRS were found to correlate with data from the well-established in vitro permeation test (IVPT) model using human epidermis. However, these studies used simple vehicles comprising single solvents and binary or ternary solvent mixtures; to date, the utility of CRS for monitoring dermal absorption following application of complex marketed formulations has not been examined. In the present work, skin delivery of diclofenac sodium (DFNa) from two topical dermatological drug products, namely Diclac^® Lipogel 10 mg/g and Primofenac^® Emulsion gel 1%, was determined by IVPT and in vivo by both CRS and tape stripping (TS) methodologies under similar experimental conditions. The in vivo data were evaluated against the in vitro findings, and a direct comparison between CRS and TS was performed. Results from all methodologies showed that Diclac promoted significantly greater DFNa delivery to the skin (p < 0.05). The cumulative amounts of DFNa which permeated at 24 h in vitro for Diclac (86.5 ± 9.4 µg/cm²) were 3.6-fold greater than the corresponding amounts found for Primofenac (24.4 ± 2.7 µg/cm²). Additionally, total skin uptake of DFNa in vivo, estimated by the area under the depth profiles curves (AUC), or the signal intensity of the drug detected in the upper stratum corneum (SC) (4 µm) ranged from 3.5 to 3.6-fold greater for Diclac than for Primofenac. The shape of the distribution profiles and the depth of DFNa penetration to the SC estimated by CRS and TS were similar for the two methods. However, TS data indicated a 4.7-fold greater efficacy of Diclac relative to Primofenac, with corresponding total amounts of drug penetrated, 94.1 ± 22.6 µg and 20.2 ± 7.0 µg. The findings demonstrate that CRS is a methodology that is capable of distinguishing skin delivery of DFNa from different formulations. The results support the use of this approach for non-invasive evaluation of topical products in vivo. Future studies will examine additional formulations with more complex compositions and will use a wider range of drugs with different physicochemical properties. The non-invasive nature of CRS coupled with the ability to monitor drug permeation in real time offer significant advantages for testing and development of topical dermatological products. Full article

(This article belongs to the Special Issue Drug Delivery and Penetration through Skin and Its Formulations)

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18 pages, 4060 KiB

Open AccessArticle

Formulation and Evaluation of the In Vitro Performance of Topical Dermatological Products Containing Diclofenac Sodium

by Mahima Manian, Piyush Jain, Deepal Vora and Ajay K. Banga

Pharmaceutics 2022, 14(9), 1892; https://doi.org/10.3390/pharmaceutics14091892 - 07 Sep 2022

Cited by 6 | Viewed by 3913

Abstract

The selection of an appropriate vehicle in a semi-solid topical product is of utmost importance since the vehicle composition and microstructure can potentially cause changes in drug–vehicle or vehicle–skin interactions and affect drug release and subsequent permeation into and across skin. Hence, the [...] Read more.

The selection of an appropriate vehicle in a semi-solid topical product is of utmost importance since the vehicle composition and microstructure can potentially cause changes in drug–vehicle or vehicle–skin interactions and affect drug release and subsequent permeation into and across skin. Hence, the aim of this study was to evaluate different semi-solid formulations containing diclofenac sodium for the physicochemical and structural performance of excipients used and various physiological factors governing permeation of drugs applied to skin. The formulations (emulsion, emulgel, gel, and ointment) were prepared using conventional excipients and were found to be homogenous and stable. Rheological analysis demonstrated characteristic shear-thinning and viscoelastic behavior of formulations. The mean release rate of the gel formulation (380.42 ± 3.05 µg/cm²/h^0.5) was statistically higher compared to all other formulations. In vitro permeation using human skin showed a significantly greater extent of drug permeation and retention for the emulgel formulation (23.61 ± 1.03 µg/cm² and 47.95 ± 2.47 µg/cm², respectively). The results demonstrated that the different formulations influenced product performance due to their inherent properties. The findings of this study demonstrated that a comprehensive physicochemical and structural evaluation is required to optimize the in vitro performance for dermatological formulations depending on the intended therapeutic effect. Full article

(This article belongs to the Special Issue Drug Delivery and Penetration through Skin and Its Formulations)

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17 pages, 22637 KiB

Open AccessArticle

Structural and Functional Analysis of Excised Skins and Human Reconstructed Epidermis with Confocal Raman Spectroscopy and in Microfluidic Diffusion Chambers

by Dorottya Kocsis, Hichem Kichou, Katalin Döme, Zsófia Varga-Medveczky, Zsolt Révész, Istvan Antal and Franciska Erdő

Pharmaceutics 2022, 14(8), 1689; https://doi.org/10.3390/pharmaceutics14081689 - 13 Aug 2022

Cited by 10 | Viewed by 2271

Abstract

Several ex vivo and in vitro skin models are available in the toolbox of dermatological and cosmetic research. Some of them are widely used in drug penetration testing. The excised skins show higher variability, while the in vitro skins provide more reproducible data. [...] Read more.

Several ex vivo and in vitro skin models are available in the toolbox of dermatological and cosmetic research. Some of them are widely used in drug penetration testing. The excised skins show higher variability, while the in vitro skins provide more reproducible data. The aim of the current study was to compare the chemical composition of different skin models (excised rat skin, excised human skin and human-reconstructed epidermis) by measurement of ceramides, cholesterol, lactate, urea, protein and water at different depths of the tissues. The second goal was to compile a testing system, which includes a skin-on-a-chip diffusion setup and a confocal Raman spectroscopy for testing drug diffusion across the skin barrier and accumulation in the tissue models. A hydrophilic drug caffeine and the P-glycoprotein substrate quinidine were used in the study as topical cream formulations. The results indicate that although the transdermal diffusion of quinidine is lower, the skin accumulation was comparable for the two drugs. The various skin models showed different chemical compositions. The human skin was abundant in ceramides and cholesterol, while the reconstructed skin contained less water and more urea and protein. Based on these results, it can be concluded that skin-on-a-chip and confocal Raman microspectroscopy are suitable for testing drug penetration and distribution at different skin layers within an exposition window. Furthermore, obese human skin should be treated with caution for skin absorption testing due to its unbalanced composition. Full article

(This article belongs to the Special Issue Drug Delivery and Penetration through Skin and Its Formulations)

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21 pages, 4108 KiB

Open AccessArticle

AKVANO^®: A Novel Lipid Formulation System for Topical Drug Delivery—In Vitro Studies

by Jan Holmbäck, Vibhu Rinwa, Tobias Halthur, Puneet Rinwa, Anders Carlsson and Bengt Herslöf

Pharmaceutics 2022, 14(4), 794; https://doi.org/10.3390/pharmaceutics14040794 - 05 Apr 2022

Cited by 3 | Viewed by 2446

Abstract

A novel formulation technology called AKVANO^® has been developed with the aim to provide a tuneable and versatile drug delivery system for topical administration. The vehicle is based on a water-free lipid formulation where selected lipids, mainly phospholipids rich in phosphatidylcholine, are [...] Read more.

A novel formulation technology called AKVANO^® has been developed with the aim to provide a tuneable and versatile drug delivery system for topical administration. The vehicle is based on a water-free lipid formulation where selected lipids, mainly phospholipids rich in phosphatidylcholine, are dissolved in a volatile solvent, such as ethanol. With the aim of describing the basic properties of the system, the following physicochemical methods were used: viscometry, dynamic light scattering, NMR diffusometry, and atomic force microscopy. AKVANO formulations are non-viscous, with virtually no or very minute aggregates formed, and when applied to the skin, e.g., by spraying, a thin film consisting of lipid bilayer structures is formed. Standardized in vitro microbiological and irritation tests show that AKVANO formulations meet criteria for antibacterial, antifungal, and antiviral activities and, at the same time, are being investigated as a non-irritant to the skin and eye. The ethanol content in AKVANO facilitates incorporation of many active pharmaceutical ingredients (>80 successfully tested) and the phospholipids seem to act as a solubilizer in the formulation. In vitro skin permeation experiments using Strat-M^® membranes have shown that AKVANO formulations can be designed to alter the penetration of active ingredients by changing the lipid composition. Full article

(This article belongs to the Special Issue Drug Delivery and Penetration through Skin and Its Formulations)

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19 pages, 3083 KiB

Open AccessArticle

Polymeric Nanoparticles and Chitosan Gel Loading Ketorolac Tromethamine to Alleviate Pain Associated with Condyloma Acuminata during the Pre- and Post-Ablation

by Salima El Moussaoui, Ismael Abo-Horan, Lyda Halbaut, Cristina Alonso, Lluïsa Coderch, María Luisa Garduño-Ramírez, Beatriz Clares, José Luis Soriano, Ana Cristina Calpena, Francisco Fernández-Campos and Mireia Mallandrich

Pharmaceutics 2021, 13(11), 1784; https://doi.org/10.3390/pharmaceutics13111784 - 25 Oct 2021

Cited by 9 | Viewed by 2624

Abstract

This study describes the preparation and evaluation of two formulations, a hydrogel and a nanostructured system, containing ketorolac tromethamine as an anti-inflammatory agent for the local therapy against the inflammatory process derived from the surgical excision of Condyloma acuminata. Both formulations were physicochemically [...] Read more.

This study describes the preparation and evaluation of two formulations, a hydrogel and a nanostructured system, containing ketorolac tromethamine as an anti-inflammatory agent for the local therapy against the inflammatory process derived from the surgical excision of Condyloma acuminata. Both formulations were physicochemically characterized. In vitro release profiles show that the nanoparticles release 92% ± 2.3 of the total ketorolac tromethamine encapsulated, while the chitosan gel releases 18.6% ± 0.2. The ex vivo permeation and distribution through human skin were also assayed and was observed how the main amount of ketorolac tromethamine is retained in the epidermis. In vivo studies were accomplished to evaluate the anti-inflammatory efficacy in mice which also involved the histological analysis to confirm the in vivo results. The nanoparticles present a significantly higher anti-inflammatory efficacy than chitosan gel. The tolerability of developed formulations was assessed by monitoring the biomechanical properties of the skin before and after application of both formulations. No statistical differences in trans-epidermal water loss and skin hydration with respect to the basal values were observed and the formulations exhibited higher anti-inflammatory activity compared to a reference ketotorlac tromethamine solution. Therefore, it can be concluded that both formulations can be proposed as outstanding candidates for offering a local anti-inflammatory therapeutical tool with potential clinical application. Full article

(This article belongs to the Special Issue Drug Delivery and Penetration through Skin and Its Formulations)

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21 pages, 3343 KiB

Open AccessArticle

The Physicochemical, Biopharmaceutical, and In Vitro Efficacy Properties of Freeze-Dried Dexamethasone-Loaded Lipomers

by Eloy Pena-Rodríguez, Aida Mata-Ventosa, Laura Garcia-Vega, Sandra Pérez-Torras and Francisco Fernández-Campos

Pharmaceutics 2021, 13(8), 1322; https://doi.org/10.3390/pharmaceutics13081322 - 23 Aug 2021

Cited by 7 | Viewed by 3348

Abstract

Dexamethasone-loaded polymer hybrid nanoparticles were developed as a potential tool to treat alopecia areata due to their follicular targeting ability. Freeze drying (FD) is a common technique used to improve nanoparticle stability; however, there are few studies focused on its effect on ethyl [...] Read more.

Dexamethasone-loaded polymer hybrid nanoparticles were developed as a potential tool to treat alopecia areata due to their follicular targeting ability. Freeze drying (FD) is a common technique used to improve nanoparticle stability; however, there are few studies focused on its effect on ethyl cellulose lipid-core nanoparticles. Nanoparticles were lyophilized with different cryoprotectants. Sucrose was selected because it allowed for a good resuspension and provided acceptable physicochemical parameters (374.33 nm, +34.7 mV, polydispersion 0.229%, and 98.87% encapsulation efficiency). The nanoparticles obtained were loaded into a pleasant xanthan gum hydrogel, and the rheological, release, and skin permeation profiles of different formulations were studied. The FD formulation significantly modified the particle size, and the drug release and permeation properties were also altered. In addition, analyses of the cytotoxicity and anti-inflammatory efficacy of FD and non-FD particles on human keratinocytes indicated no differences. Full article

(This article belongs to the Special Issue Drug Delivery and Penetration through Skin and Its Formulations)

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19 pages, 1950 KiB

Open AccessArticle

“Plurethosome” as Vesicular System for Cutaneous Administration of Mangiferin: Formulative Study and 3D Skin Tissue Evaluation

by Maddalena Sguizzato, Francesca Ferrara, Paolo Mariani, Alessia Pepe, Rita Cortesi, Nicolas Huang, Fanny Simelière, Paola Boldrini, Anna Baldisserotto, Giuseppe Valacchi and Elisabetta Esposito

Pharmaceutics 2021, 13(8), 1124; https://doi.org/10.3390/pharmaceutics13081124 - 23 Jul 2021

Cited by 12 | Viewed by 2150

Abstract

Human skin is dramatically exposed to toxic pollutants such as ozone. To counteract the skin disorders induced by the air pollution, natural antioxidants such as mangiferin could be employed. A formulative study for the development of vesicular systems for mangiferin based on phosphatidylcholine [...] Read more.

Human skin is dramatically exposed to toxic pollutants such as ozone. To counteract the skin disorders induced by the air pollution, natural antioxidants such as mangiferin could be employed. A formulative study for the development of vesicular systems for mangiferin based on phosphatidylcholine and the block copolymer pluronic is described. Plurethosomes were designed for mangiferin transdermal administration and compared to ethosome and transethosome. Particularly, the effect of vesicle composition was investigated on size distribution, inner and outer morphology by photon correlation spectroscopy, small angle X-ray diffraction, and transmission electron microscopy. The potential of selected formulations as vehicles for mangiferin was studied, evaluating encapsulation efficiency and in vitro diffusion parameters by Franz cells. The mangiferin antioxidant capacity was verified by the 2,2-diphenyl-1-picrylhydrazyl assay. Vesicle size spanned between 200 and 550 nm, being influenced by phosphatidylcholine concentration and by the presence of polysorbate or pluronic. The vesicle supramolecular structure was multilamellar in the case of ethosome or plurethosome and unilamellar in the case of transethosome. A linear diffusion of mangiferin in the case of ethosome and transethosomes and a biphasic profile in the case of plurethosomes indicated the capability of multilamellar vesicles to retain the drug more efficaciously than the unilamellar ones. The antioxidant and anti-inflammatory potential effect of mangiferin against pollutants was evaluated on 3D human skin models exposed to O₃. The protective effect exerted by plurethosomes and transethosomes suggests their possible application to enhance the cutaneous antioxidant defense status. Full article

(This article belongs to the Special Issue Drug Delivery and Penetration through Skin and Its Formulations)

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10 pages, 3155 KiB

Open AccessArticle

Development and Evaluation of a Human Skin Equivalent in a Semiautomatic Microfluidic Diffusion Chamber

by Júlia Tárnoki-Zách, Elod Mehes, Zsófia Varga-Medveczky, Dona Greta Isai, Nandor Barany, Edina Bugyik, Zsolt Revesz, Sándor Paku, Franciska Erdo and Andras Czirok

Pharmaceutics 2021, 13(6), 910; https://doi.org/10.3390/pharmaceutics13060910 - 20 Jun 2021

Cited by 14 | Viewed by 2835

Abstract

There is an increasing demand for transdermal transport measurements to optimize topical drug formulations and to achieve proper penetration profile of cosmetic ingredients. Reflecting ethical concerns the use of both human and animal tissues is becoming more restricted. Therefore, the focus of dermal [...] Read more.

There is an increasing demand for transdermal transport measurements to optimize topical drug formulations and to achieve proper penetration profile of cosmetic ingredients. Reflecting ethical concerns the use of both human and animal tissues is becoming more restricted. Therefore, the focus of dermal research is shifting towards in vitro assays. In the current proof-of-concept study a three-layer skin equivalent using human HaCaT keratinocytes, an electrospun polycaprolactone mesh and a collagen-I gel was compared to human excised skin samples. We measured the permeability of the samples for 2% caffeine cream using a miniaturized dynamic diffusion cell (“skin-on-a-chip” microfluidic device). Caffeine delivery exhibits similar transport kinetics through the artificial skin and the human tissue: after a rapid rise, a long-lasting high concentration steady state develops. This is markedly distinct from the kinetics measured when using cell-free constructs, where a shorter release was observable. These results imply that both the established skin equivalent and the microfluidic diffusion chamber can serve as a suitable base for further development of more complex tissue substitutes. Full article

(This article belongs to the Special Issue Drug Delivery and Penetration through Skin and Its Formulations)

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15 pages, 1727 KiB

Open AccessArticle

Enhanced Transdermal Delivery of Bisoprolol Hemifumarate via Combined Effect of Iontophoresis and Chemical Enhancers: Ex Vivo Permeation/In Vivo Pharmacokinetic Studies

by Mahmoud H. Teaima, Mohamed Azmi Ahmed Mohamed, Randa Tag Abd El Rehem, Saadia A. Tayel, Mohamed A. El-Nabarawi and Shahinaze A. Fouad

Pharmaceutics 2021, 13(5), 682; https://doi.org/10.3390/pharmaceutics13050682 - 10 May 2021

Cited by 8 | Viewed by 2708

Abstract

Bisoprolol hemifumarate (BH) is an antihypertensive drug that is used as first-line treatment for chronic hypertension and angina pectoris. Our study was performed to enhance the transdermal delivery of BH, a hydrophilic drug active with high molecular weight, through differently prepared hydrogels. The [...] Read more.

Bisoprolol hemifumarate (BH) is an antihypertensive drug that is used as first-line treatment for chronic hypertension and angina pectoris. Our study was performed to enhance the transdermal delivery of BH, a hydrophilic drug active with high molecular weight, through differently prepared hydrogels. The synergistic effect of permeation enhancers and iontophoresis was investigated via both ex vivo and in vivo permeation studies. Ex vivo iontophoretic permeation studies were performed by using male albino Wistar rat skin. Cellosolve^® hydrogel (F7) showed a 1.5-fold increase in Q₁₈₀, Jss, and FER compared to F5 (lacking permeation enhancer). BH pharmacokinetic data were studied in human volunteers, following transdermal delivery of F7, using Phoresor^® Unit II iontophoresis device, compared to conventional oral tablets. F7 showed 1.9- and 2-fold higher values of C_max and AUC_0–40, respectively compared to Concor^® tablets, as well as a smaller T_max (2.00 ± 2.00 h). The relative bioavailability of F7 was found to be 201.44%, relative to Concor^® tablets, demonstrating the significantly enhanced transdermal permeation of BH from the selected hydrogel by iontophoresis, in human volunteers. Finally, results showed the successful utility of permeation enhancers combined with iontophoresis in significantly enhanced transdermal permeation of BH, despite its large molecular weight and hydrophilic nature. Therefore, this strategy could be employed as a successful alternative route of administration to conventional oral tablets. Full article

(This article belongs to the Special Issue Drug Delivery and Penetration through Skin and Its Formulations)

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15 pages, 3844 KiB

Open AccessArticle

Design and Evaluation of Dissolving Microneedles for Enhanced Dermal Delivery of Propranolol Hydrochloride

by Jingjing He, Zichen Zhang, Xianzi Zheng, Lu Li, Jianping Qi, Wei Wu and Yi Lu

Pharmaceutics 2021, 13(4), 579; https://doi.org/10.3390/pharmaceutics13040579 - 19 Apr 2021

Cited by 28 | Viewed by 4238

Abstract

Oral propranolol hydrochloride has been the first-line treatment for infantile hemangioma (IH), whereas systemic exposure to propranolol has the potential of causing serious adverse reactions. Dermal delivery of propranolol is preferable due to high local drug concentration and fewer adverse effects. However, propranolol [...] Read more.

Oral propranolol hydrochloride has been the first-line treatment for infantile hemangioma (IH), whereas systemic exposure to propranolol has the potential of causing serious adverse reactions. Dermal delivery of propranolol is preferable due to high local drug concentration and fewer adverse effects. However, propranolol hydrochloride (BCS class I) is highly hydrophilic and has difficulty in penetrating the stratum corneum (SC) barrier. Dissolving microneedles (MNs) are an efficient tool for overcoming the barrier of the SC and enhancing dermal drug delivery. In this study, propranolol hydrochloride-loaded dissolving MNs were fabricated by using hyaluronic acid and polyvinyl pyrrolidone as matrix materials. Controllable drug loading in needle tips was achieved by a two-step casting procedure. The needles were good in mechanical strength for penetrating the SC while presented excellent dissolving capability for releasing propranolol hydrochloride. In comparison with the solution counterpart, irrespective of being applied to intact skin or solid MNs-pretreated skin, dissolving MNs significantly increased the permeability and skin retention of propranolol. In conclusion, dissolving MNs could be a potential approach for enhancing dermal delivery of propranolol to treat IH. Full article

(This article belongs to the Special Issue Drug Delivery and Penetration through Skin and Its Formulations)

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Review

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22 pages, 3333 KiB

Open AccessReview

Rotary Jet Spinning (RJS): A Key Process to Produce Biopolymeric Wound Dressings

by Juliana O. Bahú, Lucas R. Melo de Andrade, Sara Crivellin, Nadia G. Khouri, Sara O. Sousa, Luiza M. I. Fernandes, Samuel D. A. Souza, Luz S. Cárdenas Concha, Maria I. R. B. Schiavon, Cibelem I. Benites, Patrícia Severino, Eliana B. Souto and Viktor O. Cárdenas Concha

Pharmaceutics 2022, 14(11), 2500; https://doi.org/10.3390/pharmaceutics14112500 - 18 Nov 2022

Cited by 7 | Viewed by 2555

Abstract

Wounds result from different causes (e.g., trauma, surgeries, and diabetic ulcers), requiring even extended periods of intensive care for healing, according to the patient’s organism and treatment. Currently, wound dressings generated by polymeric fibers at micro and nanometric scales are promising for healing [...] Read more.

Wounds result from different causes (e.g., trauma, surgeries, and diabetic ulcers), requiring even extended periods of intensive care for healing, according to the patient’s organism and treatment. Currently, wound dressings generated by polymeric fibers at micro and nanometric scales are promising for healing the injured area. They offer great surface area and porosity, mimicking the fibrous extracellular matrix structure, facilitating cell adhesion, migration, and proliferation, and accelerating the wound healing process. Such properties resulted in countless applications of these materials in biomedical and tissue engineering, also as drug delivery systems for bioactive molecules to help tissue regeneration. The techniques used to engineer these fibers include spinning methods (electro-, rotary jet-), airbrushing, and 3D printing. These techniques have important advantages, such as easy-handle procedure and process parameters variability (type of polymer), but encounter some scalability problems. RJS is described as a simple and low-cost technique resulting in high efficiency and yield for fiber production, also capable of bioactive agents’ incorporation to improve the healing potential of RJS wound dressings. This review addresses the use of RJS to produce polymeric fibers, describing the concept, type of configuration, comparison to other spinning techniques, most commonly used polymers, and the relevant parameters that influence the manufacture of the fibers, for the ultimate use in the development of wound dressings. Full article

(This article belongs to the Special Issue Drug Delivery and Penetration through Skin and Its Formulations)

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32 pages, 2569 KiB

Open AccessReview

Transdermal Delivery of Chemotherapeutics: Strategies, Requirements, and Opportunities

by Rabin Neupane, Sai H. S. Boddu, Mariam Sami Abou-Dahech, Rinda Devi Bachu, David Terrero, R. Jayachandra Babu and Amit K. Tiwari

Pharmaceutics 2021, 13(7), 960; https://doi.org/10.3390/pharmaceutics13070960 - 26 Jun 2021

Cited by 26 | Viewed by 9021

Abstract

Chemotherapeutic drugs are primarily administered to cancer patients via oral or parenteral routes. The use of transdermal drug delivery could potentially be a better alternative to decrease the dose frequency and severity of adverse or toxic effects associated with oral or parenteral administration [...] Read more.

Chemotherapeutic drugs are primarily administered to cancer patients via oral or parenteral routes. The use of transdermal drug delivery could potentially be a better alternative to decrease the dose frequency and severity of adverse or toxic effects associated with oral or parenteral administration of chemotherapeutic drugs. The transdermal delivery of drugs has shown to be advantageous for the treatment of highly localized tumors in certain types of breast and skin cancers. In addition, the transdermal route can be used to deliver low-dose chemotherapeutics in a sustained manner. The transdermal route can also be utilized for vaccine design in cancer management, for example, vaccines against cervical cancer. However, the design of transdermal formulations may be challenging in terms of the conjugation chemistry of the molecules and the sustained and reproducible delivery of therapeutically efficacious doses. In this review, we discuss the nano-carrier systems, such as nanoparticles, liposomes, etc., used in recent literature to deliver chemotherapeutic agents. The advantages of transdermal route over oral and parenteral routes for popular chemotherapeutic drugs are summarized. Furthermore, we also discuss a possible in silico approach, Formulating for Efficacy™, to design transdermal formulations that would probably be economical, robust, and more efficacious. Full article

(This article belongs to the Special Issue Drug Delivery and Penetration through Skin and Its Formulations)

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