Special Issue "Recent Technology of Transdermal and Topical Drug Delivery"

A special issue of Pharmaceutics (ISSN 1999-4923).

Deadline for manuscript submissions: closed (30 June 2017)

Special Issue Editors

Guest Editor
Prof. Dr. Kenji Sugibayashi

Faculty of Pharmaceutical Sciences, Josai University, Saitama 350-0295, Japan
Website | E-Mail
Interests: transdermal drug delivery; skin permeation
Guest Editor
Prof. Dr. Yoshihiro Tokudome

Faculty of Pharmaceutical Sciences, Josai University, Saitama 350-0295, Japan
Website | E-Mail
Interests: skin physiology; dermatological sciences; transdermal drug delivery

Special Issue Information

Dear Colleagues,

Transdermal and topical drug delivery offers many potential advantages over conventional delivery methods of drugs. Skin has been used as an application site for therapeutic drugs to avoid the hepatic first pass effect and side-effects in the GI tract. Thus, topical formulations are beneficial, especially for elderly patients and infants who sometimes have difficulty swallowing medicines. In recent years, novel alternative methods for animal experiments and potent analytical techniques have been developed in the percutaneous absorption and skin permeation studies.

We would like to invite contributions from researchers in these fields, including pharmaceutical researchers/engineers and academicians as well.

Prof. Dr. Kenji Sugibayashi
Prof. Dr. Yoshihiro Tokudome
Guest Editors

Manuscript Submission Information

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Keywords

  • Transdermal drug delivery
  • Topical formulation
  • Compound analysis in skin
  • Species difference
  • Alternative animals

Published Papers (5 papers)

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Research

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Open AccessArticle Efficient Transdermal Delivery of Alendronate, a Nitrogen-Containing Bisphosphonate, Using Tip-Loaded Self-Dissolving Microneedle Arrays for the Treatment of Osteoporosis
Pharmaceutics 2017, 9(3), 29; doi:10.3390/pharmaceutics9030029
Received: 13 July 2017 / Revised: 11 August 2017 / Accepted: 14 August 2017 / Published: 17 August 2017
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Abstract
To improve the transdermal bioavailability and safety of alendronate (ALN), a nitrogen-containing bisphosphonate, we developed self-dissolving microneedle arrays (MNs), in which ALN is loaded only at the tip portion of micron-scale needles by a dip-coating method (ALN(TIP)–MN). We observed micron-scale pores in rat
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To improve the transdermal bioavailability and safety of alendronate (ALN), a nitrogen-containing bisphosphonate, we developed self-dissolving microneedle arrays (MNs), in which ALN is loaded only at the tip portion of micron-scale needles by a dip-coating method (ALN(TIP)–MN). We observed micron-scale pores in rat skin just after application of ALN(TIP)–MN, indicating that transdermal pathways for ALN were created by MN. ALN was rapidly released from the tip of MNs as observed in an in vitro release study. The tip portions of MNs completely dissolved in the rat skin within 5 min after application in vivo. After application of ALN(TIP)–MN in mice, the plasma concentration of ALN rapidly increased, and the bioavailability of ALN was approximately 96%. In addition, the decrease in growth plate was effectively suppressed by this efficient delivery of ALN in a rat model of osteoporosis. Furthermore, no skin irritation was observed after application of ALN(TIP)–MN and subcutaneous injection of ALN, while mild skin irritation was induced by whole-ALN-loaded MN (ALN–MN)—in which ALN is contained in the whole of the micron-scale needles fabricated from hyaluronic acid—and intradermal injection of ALN. These findings indicate that ALN(TIP)–MN is a promising transdermal formulation for the treatment of osteoporosis without skin irritation. Full article
(This article belongs to the Special Issue Recent Technology of Transdermal and Topical Drug Delivery)
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Open AccessFeature PaperArticle Development of Novel Faster-Dissolving Microneedle Patches for Transcutaneous Vaccine Delivery
Pharmaceutics 2017, 9(3), 27; doi:10.3390/pharmaceutics9030027
Received: 30 June 2017 / Revised: 24 July 2017 / Accepted: 27 July 2017 / Published: 3 August 2017
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Abstract
Microneedle (MN) patches are promising for transcutaneous vaccination because they enable vaccine antigens to physically penetrate the stratum corneum via low-invasive skin puncturing, and to be effectively delivered to antigen-presenting cells in the skin. In second-generation MN patches, the dissolving MNs release the
[...] Read more.
Microneedle (MN) patches are promising for transcutaneous vaccination because they enable vaccine antigens to physically penetrate the stratum corneum via low-invasive skin puncturing, and to be effectively delivered to antigen-presenting cells in the skin. In second-generation MN patches, the dissolving MNs release the loaded vaccine antigen into the skin. To shorten skin application time for clinical practice, this study aims to develop novel faster-dissolving MNs. We designed two types of MNs made from a single thickening agent, carboxymethylcellulose (CMC) or hyaluronan (HN). Both CMC-MN and HN-MN completely dissolved in rat skin after a 5-min application. In pre-clinical studies, both MNs could demonstrably increase antigen-specific IgG levels after vaccination and prolong antigen deposition compared with conventional injections, and deliver antigens into resected human dermal tissue. In clinical research, we demonstrated that both MNs could reliably and safely puncture human skin without any significant skin irritation from transepidermal water loss measurements and ICDRG (International Contact Dermatitis Research Group) evaluation results. Full article
(This article belongs to the Special Issue Recent Technology of Transdermal and Topical Drug Delivery)
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Open AccessFeature PaperArticle A Possible Percutaneous Penetration Pathway That Should Be Considered
Pharmaceutics 2017, 9(3), 26; doi:10.3390/pharmaceutics9030026
Received: 25 June 2017 / Revised: 19 July 2017 / Accepted: 21 July 2017 / Published: 27 July 2017
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Abstract
The intercellular lipids in the stratum corneum form structures composed of ordered phases with orthorhombic and hexagonal hydrocarbon-chain packing structures and, in addition, a structure composed of a disordered fluid phase. Although the fluid phase plays an important role in percutaneous penetration, little
[...] Read more.
The intercellular lipids in the stratum corneum form structures composed of ordered phases with orthorhombic and hexagonal hydrocarbon-chain packing structures and, in addition, a structure composed of a disordered fluid phase. Although the fluid phase plays an important role in percutaneous penetration, little attention has been paid to it in the literature thus far. Recently, a method to estimate the proportion of the fluid phase within the lipids of the stratum corneum was proposed and it was shown to reach about 80%. However, since that study assumed uniform extraction of the intercellular lipids from the stratum corneum, the analysis might give rise to an overestimation of the proportion of the lipids in the fluid phase. We developed a way to investigate the proportion of the lipids in the fluid phase by treating with ethanol, into which the lipids in the fluid phase might be dominantly dissolved. From the experiment we pointed out the possibility that the proportion of the lipids in the fluid phase reached more than 50% of the whole intercellular lipids. Therefore, the fluid-phase region in the intercellular lipid matrix should be taken into account when considering the percutaneous penetration mechanism. Full article
(This article belongs to the Special Issue Recent Technology of Transdermal and Topical Drug Delivery)
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Review

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Open AccessReview Topical Nano and Microemulsions for Skin Delivery
Pharmaceutics 2017, 9(4), 37; doi:10.3390/pharmaceutics9040037
Received: 11 August 2017 / Revised: 11 September 2017 / Accepted: 13 September 2017 / Published: 21 September 2017
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Abstract
Nanosystems such as microemulsions (ME) and nanoemulsions (NE) offer considerable opportunities for targeted drug delivery to and via the skin. ME and NE are stable colloidal systems composed of oil and water, stabilised by a mixture of surfactants and cosurfactants, that have received
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Nanosystems such as microemulsions (ME) and nanoemulsions (NE) offer considerable opportunities for targeted drug delivery to and via the skin. ME and NE are stable colloidal systems composed of oil and water, stabilised by a mixture of surfactants and cosurfactants, that have received particular interest as topical skin delivery systems. There is considerable scope to manipulate the formulation components and characteristics to achieve optimal bioavailability and minimal skin irritancy. This includes the incorporation of established chemical penetration enhancers to fluidize the stratum corneum lipid bilayers, thus reducing the primary skin barrier and increasing permeation. This review discusses nanosystems with utility in skin delivery and focuses on the composition and characterization of ME and NE for topical and transdermal delivery. The mechanism of skin delivery across the stratum corneum and via hair follicles is reviewed with particular focus on the influence of formulation. Full article
(This article belongs to the Special Issue Recent Technology of Transdermal and Topical Drug Delivery)
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Open AccessReview Transdermal Permeation of Drugs in Various Animal Species
Pharmaceutics 2017, 9(3), 33; doi:10.3390/pharmaceutics9030033
Received: 31 July 2017 / Revised: 21 August 2017 / Accepted: 28 August 2017 / Published: 6 September 2017
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Abstract
Excised human skin is utilized for in vitro permeation experiments to evaluate the safety and effect of topically-applied drugs by measuring its skin permeation and concentration. However, ethical considerations are the major problem for using human skin to evaluate percutaneous absorption. Moreover, large
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Excised human skin is utilized for in vitro permeation experiments to evaluate the safety and effect of topically-applied drugs by measuring its skin permeation and concentration. However, ethical considerations are the major problem for using human skin to evaluate percutaneous absorption. Moreover, large variations have been found among human skin specimens as a result of differences in age, race, and anatomical donor site. Animal skins are used to predict the in vivo human penetration/permeation of topically-applied chemicals. In the present review, skin characteristics, such as thickness of skin, lipid content, hair follicle density, and enzyme activity in each model are compared to human skin. In addition, intra- and inter-individual variation in animal models, permeation parameter correlation between animal models and human skin, and utilization of cultured human skin models are also descried. Pig, guinea pig, and hairless rat are generally selected for this purpose. Each animal model has advantages and weaknesses for utilization in in vitro skin permeation experiments. Understanding of skin permeation characteristics such as permeability coefficient (P), diffusivity (D), and partition coefficient (K) for each skin model would be necessary to obtain better correlations for animal models to human skin permeation. Full article
(This article belongs to the Special Issue Recent Technology of Transdermal and Topical Drug Delivery)
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