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35 pages, 3902 KiB

Open AccessFeature PaperReview

Advancements in Nanoemulsion-Based Drug Delivery Across Different Administration Routes

by Maria D. Chatzidaki and Evgenia Mitsou

Pharmaceutics 2025, 17(3), 337; https://doi.org/10.3390/pharmaceutics17030337 - 5 Mar 2025

Cited by 6 | Viewed by 2447

Nanoemulsions (NEs) have emerged as effective drug delivery systems over the past few decades due to their multifaceted nature, offering advantages such as enhanced bioavailability, protection of encapsulated compounds, and low toxicity. In the present review, we focus on advancements in drug delivery [...] Read more.

Nanoemulsions (NEs) have emerged as effective drug delivery systems over the past few decades due to their multifaceted nature, offering advantages such as enhanced bioavailability, protection of encapsulated compounds, and low toxicity. In the present review, we focus on advancements in drug delivery over the last five years across (trans)dermal, oral, ocular, nasal, and intra-articular administration routes using NEs. Rational selection of components, surface functionalization, incorporation of permeation enhancers, and functionalization with targeting moieties are explored for each route discussed. Additionally, apart from NEs, we explore NE-based drug delivery systems (e.g., NE-based gels) while highlighting emerging approaches such as vaccination and theranostic applications. The growing interest in NEs for drug delivery purposes is reflected in clinical trials, which are also discussed. By summarizing the latest advances, exploring new strategies, and identifying critical challenges, this review focuses on developments for efficient NE-based therapeutic approaches. Full article

(This article belongs to the Special Issue Micro- and Nanoemulsions in Therapeutics: Advancements in Targeted Drug Delivery and Theranostic Applications)

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12 pages, 315 KiB

Open AccessArticle

Topical Administration of Cannabidiol: Influence of Vehicle-Related Aspects on Skin Permeation Process

by Antonella Casiraghi, Umberto M. Musazzi, Giorgio Centin, Silvia Franzè and Paola Minghetti

Pharmaceuticals 2020, 13(11), 337; https://doi.org/10.3390/ph13110337 - 23 Oct 2020

Cited by 57 | Viewed by 10438

Abstract

Cannabidiol (CBD) is a non-psychoactive cannabinoid isolated from Cannabis sativa which, given its claimed beneficial properties and therapeutic potential, has lately aroused considerable attention from the scientific community. Starting from the little literature evidence, the main purpose of this study was to investigate [...] Read more.

Cannabidiol (CBD) is a non-psychoactive cannabinoid isolated from Cannabis sativa which, given its claimed beneficial properties and therapeutic potential, has lately aroused considerable attention from the scientific community. Starting from the little literature evidence, the main purpose of this study was to investigate the topical administration of CBD, with particular focus on the influence of vehicle-related aspects on the skin permeation process. This could provide useful information for the design of suitable drug delivery systems which could be used in developing topical medicines and cosmetics. In vitro human skin permeation studies were conducted using modified Franz diffusion cells to compare the performance of four solutions and two semisolid formulations. The Hildebrand solubility parameter was used to better understand the thermodynamic aspects implied in the partitioning process of the cannabinoid compound into the skin. It was interestingly found that a hydrophilic gel, mostly consisting of propylene glycol (79%, w/w), can be an optimal choice for the topical administration of CBD. Moreover, the feasibility of the preparation of CBD-loaded (trans)dermal patches, made with new printing technology, was also demonstrated. Full article

(This article belongs to the Special Issue Cannabidiol: Advances in Therapeutic Applications and Future Perspectives)

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18 pages, 5056 KiB

Open AccessArticle

Universal Applicator for Digitally-Controlled Pressing Force and Impact Velocity Insertion of Microneedles into Skin

by Mara Leone, Bart H. Van Oorschot, M. Reza Nejadnik, Andrea Bocchino, Matteo Rosato, Gideon Kersten, Conor O’Mahony, Joke Bouwstra and Koen Van der Maaden

Pharmaceutics 2018, 10(4), 211; https://doi.org/10.3390/pharmaceutics10040211 - 1 Nov 2018

Cited by 44 | Viewed by 6332

Abstract

Microneedle technologies have been developed for dermal drug and vaccine delivery, including hollow-, solid-, coated-, and dissolving microneedles. Microneedles have been made in many different geometries and of many different materials, all of which may influence their skin-penetrating ability. To ensure reproducible and [...] Read more.

Microneedle technologies have been developed for dermal drug and vaccine delivery, including hollow-, solid-, coated-, and dissolving microneedles. Microneedles have been made in many different geometries and of many different materials, all of which may influence their skin-penetrating ability. To ensure reproducible and effective drug and vaccine delivery via microneedles, the optimal insertion parameters should be known. Therefore, a digitally-controlled microneedle applicator was developed to insert microneedles into the skin via impact insertion (velocity) or via pressing force insertion. Six microneedle arrays with different geometries and/or materials were applied onto ex vivo human skin with varying velocities or pressing forces. Penetration efficiency and delivered antigen dose into the skin after application of microneedles were determined. In general, microneedles pierced the skin more efficiently when applied by impact application as compared to application via pressing force. However, the angle of application of the applicator on the skin can affect the velocity of the impact, influencing the penetration efficiency of microneedles. Regarding the antigen delivery into the skin, the delivered dose was increasing by increasing the velocity or pressure, and thus, increasing the penetration efficiency. These data demonstrate that an applicator is an important tool to determine optimal application conditions with ex vivo human skin. Full article

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5 pages, 1392 KiB

Open AccessProceeding Paper

Fabrication of Sharp Tip-Separable Microneedle Device for Trans-Dermal Drug Delivery Systems

by Yuki Nabekura, Hitoshi Fukuyu, Yoshihiro Hasegawa and Mitsuhiro Shikida

Proceedings 2017, 1(4), 304; https://doi.org/10.3390/proceedings1040304 - 17 Aug 2017

Cited by 2 | Viewed by 2624

Abstract

An alignment mechanism for producing a sharp tip-separable microneedle device for trans-dermal drug delivery systems has been developed. The needle and base parts were placed on a mechanical precision motion stage to align their central axes. The overlapping region between them in the [...] Read more.

An alignment mechanism for producing a sharp tip-separable microneedle device for trans-dermal drug delivery systems has been developed. The needle and base parts were placed on a mechanical precision motion stage to align their central axes. The overlapping region between them in the height direction was controlled by inserting a thickness gauge between them. A 400-μm-high sharp tip-separable microneedle device was successfully produced by using the developed alignment mechanism with an accuracy of less than 19 μm. We also demonstrated that it can be used to produce an arrayed tip-separable microneedle device. Full article

(This article belongs to the Proceedings of Proceedings of Eurosensors 2017, Paris, France, 3–6 September 2017)

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14 pages, 4025 KiB

Open AccessArticle

Photothermal Radiometry for Skin Research

by Perry Xiao

Cosmetics 2016, 3(1), 10; https://doi.org/10.3390/cosmetics3010010 - 29 Feb 2016

Cited by 16 | Viewed by 6878

Abstract

Photothermal radiometry is an infrared remote sensing technique that has been used for skin and skin appendages research, in the areas of skin hydration, hydration gradient, skin hydration depth profiling, skin thickness measurements, skin pigmentation measurements, effect of topically applied substances, transdermal drug [...] Read more.

Photothermal radiometry is an infrared remote sensing technique that has been used for skin and skin appendages research, in the areas of skin hydration, hydration gradient, skin hydration depth profiling, skin thickness measurements, skin pigmentation measurements, effect of topically applied substances, transdermal drug delivery, moisture content of bio-materials, membrane permeation, and nail and hair measurements. Compared with other technologies, photothermal radiometry has the advantages of non-contact, non-destructive, quick to make a measurement (a few seconds), and being spectroscopic in nature. It is also colour blind, and can work on any arbitrary sample surfaces. It has a unique depth profiling capability on a sample surface (typically the top 20 µm), which makes it particularly suitable for skin measurements. In this paper, we present a review of the photothermal radiometry work carried out in our research group. We will first introduce the theoretical background, then illustrate its applications with experimental results. Full article

(This article belongs to the Section Cosmetic Dermatology)

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20 pages, 3762 KiB

Open AccessArticle

Insertion Process of Ceramic Nanoporous Microneedles by Means of a Novel Mechanical Applicator Design

by Xavier H. M. Hartmann, Peter Van der Linde, Erik F. G. A. Homburg, Lambert C. A. Van Breemen, Arthur M. De Jong and Regina Luttge

Pharmaceutics 2015, 7(4), 503-522; https://doi.org/10.3390/pharmaceutics7040503 - 18 Nov 2015

Cited by 23 | Viewed by 7465

Abstract

Arrays of microneedles (MNAs) are integrated in an out-of-plane fashion with a base plate and can serve as patches for the release of drugs and vaccines. We used soft-lithography and micromolding to manufacture ceramic nanoporous (np)MNAs. Failure modes of ceramic npMNAs are as [...] Read more.

Arrays of microneedles (MNAs) are integrated in an out-of-plane fashion with a base plate and can serve as patches for the release of drugs and vaccines. We used soft-lithography and micromolding to manufacture ceramic nanoporous (np)MNAs. Failure modes of ceramic npMNAs are as yet poorly understood and the question remained: is our npMNA platform technology ready for microneedle (MN) assembly into patches? We investigated npMNAs by microindentation, yielding average crack fracture forces above the required insertion force for a single MN to penetrate human skin. We further developed a thumb pressure-actuated applicator-assisted npMNA insertion method, which enables anchoring of MNs in the skin by an adhesive in one handling step. Using a set of simple artificial skin models, we found a puncture efficiency of this insertion method a factor three times higher than by applying thumb pressure on the npMNA base plate directly. In addition, this new method facilitated zero MN-breakage due to a well-defined force distribution exerted onto the MNs and the closely surrounding area prior to bringing the adhesive into contact with the skin. Owing to the fact that such parameter space exists, we can conclude that npMNAs by soft lithography are a platform technology for MN assembly into a patch. Full article

(This article belongs to the Special Issue Microneedle Patches: Developing Strategies for Delivery)

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7 pages, 4025 KiB

Open AccessArticle

Transdermal Delivery of Adriamycin to Transplanted Ehrlich Ascites Tumor in Mice

by Masataka Shiozuka, Yoshiaki Nonomura and Ryoichi Matsuda

Pharmaceutics 2013, 5(3), 385-391; https://doi.org/10.3390/pharmaceutics5030385 - 11 Jul 2013

Cited by 2 | Viewed by 7051

Abstract

There is considerable interest in the skin as a site of anti-cancer drug application. Nevertheless, the skin poses a formidable barrier to drug penetration, thereby limiting topical and transdermal bioavailability. However, we previously showed that a thioglycolate-based depilatory agent increases the drug permeability [...] Read more.

There is considerable interest in the skin as a site of anti-cancer drug application. Nevertheless, the skin poses a formidable barrier to drug penetration, thereby limiting topical and transdermal bioavailability. However, we previously showed that a thioglycolate-based depilatory agent increases the drug permeability of mouse skin. In the present report, we investigated the skin permeability and efficacy of the anti-cancer drug adriamycin increased when administered transdermally to mice in combination with a thioglycolate-based depilatory agent. Adriamycin in combination with depilatory treatment reduced Ehrlich tumor growth in hairless mice about the weight and size of harvested tumors. In addition, our delivery method for adriamycin increased the therapeutic effectiveness of this agent by decreasing toxicity. Moreover, measurement of adriamycin autofluorescence revealed that topically applied adriamycin penetrate the dermis after depilatory agent treatment. These results indicate that the transdermal delivery of anti-cancer drugs is feasible by handy pretreatment of the skin with a thioglycolate-based depilatory agent. Full article

(This article belongs to the Special Issue Advanced Transdermal Drug Delivery)

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13 pages, 1061 KiB

Open AccessArticle

Effect of Penetration Enhancer Containing Vesicles on the Percutaneous Delivery of Quercetin through New Born Pig Skin

by Maura Chessa, Carla Caddeo, Donatella Valenti, Maria Manconi, Chiara Sinico and Anna Maria Fadda

Pharmaceutics 2011, 3(3), 497-509; https://doi.org/10.3390/pharmaceutics3030497 - 12 Aug 2011

Cited by 87 | Viewed by 10249

Abstract

Quercetin (3,3′,4′,5,7-pentahydroxyflavone) exerts multiple pharmacological effects: anti-oxidant activity, induction of apoptosis, modulation of cell cycle, anti-mutagenesis, and anti-inflammatory effect. In topical formulations quercetin inhibits oxidative skin damage and the inflammatory processes induced by solar UV radiation. In this work, quercetin (2 mg/mL) was [...] Read more.

Quercetin (3,3′,4′,5,7-pentahydroxyflavone) exerts multiple pharmacological effects: anti-oxidant activity, induction of apoptosis, modulation of cell cycle, anti-mutagenesis, and anti-inflammatory effect. In topical formulations quercetin inhibits oxidative skin damage and the inflammatory processes induced by solar UV radiation. In this work, quercetin (2 mg/mL) was loaded in vesicular Penetration Enhancer containing Vesicles (PEVs), prepared using a mixture of lipids (Phospholipon^® 50, P50) and one of four selected hydrophilic penetration enhancers: Transcutol^® P, propylene glycol, polyethylene glycol 400, and Labrasol^® at the same concentration (40% of water phase). Photon Correlation Spectroscopy results showed a mean diameter of drug loaded vesicles in the range 80–220 nm. All formulations showed a negative surface charge and incorporation efficiency in the range 48–75%. Transmission Electron Microscopy confirmed that size and morphology varied as a function of the used penetration enhancer. The influence of PEVs on ex vivo quercetin (trans)dermal delivery was evaluated using Franz-type diffusion cells, new born pig skin and Confocal Laser Scanning Microscopy. Results showed that drug delivery is affected by the penetration enhancer used in the PEVs' formulation. Full article

(This article belongs to the Special Issue Transdermal Drug Delivery)

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