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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 December 2020) | Viewed by 46309

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Special Issue Editors

Dr. Sandra I. D. Simões

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Guest Editor

Research Institute for Medicine (iMed.ULisboa), Faculty of Pharmacy, University of Lisbon, 1649-003 Lisboa, Portugal
Interests: skin delivery; transdermal delivery; drug delivery systems; liposomes; nanoparticles; animal models of skin disease
Special Issues, Collections and Topics in MDPI journals

Dr. Joana Marques Marto

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Guest Editor

Research Institute for Medicines (iMed.ULisboa), Universidade de Lisboa, 1649-003 Lisbon, Portugal
Interests: transdermal/topical systems; skin delivery; cosmetic formulations; 3D printing; quality-by-design
Special Issues, Collections and Topics in MDPI journals

Special Issue Information

Dear Colleagues,

The area of skin formulations gathers knowledge from several scientific disciplines, yet the interactions between the skin and the formulations remain a challenge for pharmacists, biologists, chemists and physicians. Formulations are aimed at the topical or transdermal delivery of pharmacologically active compounds. Some products meet the definitions of both cosmetics and drugs, and formulations play an important role in this definition.

Advanced formulations, especially those incorporating nanocarriers, have received significant attention as many active agents in skin formulations show unfavorable physicochemical properties, such as excessive lipophilicity or hydrophilicity, chemical instability or poor skin penetration, that actively limit their effectiveness after topical application.

In silico and in vitro models are useful tools to support the selection of optimal formulations to improve cutaneous drug deposition or to enhance through-the-skin transport and systemic delivery.

More recently, 3D scanning and 3D printing appeared as innovative technologies for manufacturing personalized patches or masks as topical drug delivery systems.

This Special Issue is directed at formulation variables affecting the development of topical and transdermal drug products, aspects related to drug-excipients, drug–skin and excipient–skin interactions, and technological innovative strategies to overcome the skin barrier properties for effective drug delivery.

It is our pleasure to invite you to submit a manuscript to this Special Issue. Full papers, communications, and reviews are welcome.

Dr. Sandra I.D. Simões
Dr. Joana Marques Marto
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. Pharmaceutics is an international peer-reviewed open access monthly journal published by MDPI.

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Keywords

Skin formulation
Topical delivery
Transdermal delivery
Advanced carriers
Skin barrier
Drug release
In vitro characterization
Formulation–drug–skin interactions
Quality-by-design

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Published Papers (10 papers)

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20 pages, 4080 KiB

Open AccessArticle

Investigations of Olive Oil Industry By-Products Extracts with Potential Skin Benefits in Topical Formulations

by Andreia Nunes, Lídia Gonçalves, Joana Marto, Ana Margarida Martins, Alexandra N. Silva, Pedro Pinto, Marta Martins, Carmo Fraga and Helena Margarida Ribeiro

Pharmaceutics 2021, 13(4), 465; https://doi.org/10.3390/pharmaceutics13040465 - 30 Mar 2021

Cited by 22 | Viewed by 7549

Abstract

The by-products of olive oil industry are a major ecological issue due to their phenolic content, highly toxic organic load, and low pH. However, they can be recovered and reused, since their components have antioxidant, anti-inflammatory, and photoprotector properties. In this work, oil-in-water creams containing three different olive oil industry by-products extracts were produced without the use of organic solvents. First, the extracts were thoroughly characterized in vitro for cytotoxicity, inhibition of skin enzymes, and antioxidant and photoprotection capacities. Safety studies were then performed, including ocular and skin irritation tests, ecotoxicity evaluation, and in vivo Human Repeat Insult Patch Test. The results obtained in this initial characterization supported the incorporation of the extracts in the cream formulations. After preparation, the creams were characterized for their organoleptic, physicochemical, droplet size and rheological properties, and microbial contamination. The results showed that all formulations were semi-solid creams, with stable pH, compatible with the skin, without microbial contamination, and with the expected droplet size range. The rheological analysis showed shear-thinning behavior with yield stress, with the viscosity decreasing with increasing shear rate. The oscillatory results suggest that the creams have a strong network structure, being easily rubbed into the skin. Finally, compatibility, acceptability and antioxidant efficacy were evaluated in vivo, in human volunteers. No adverse reactions were observed after application of the formulations on skin and the cream with the highest concentrations of phenolic compounds showed the highest antioxidant efficiency. In conclusion, the results suggest that olive oil industry by-products extracts have valuable properties that favor their re-use in the cosmetic industry. The example presented here showed their successful incorporation into creams and their impact in these formulations’ appearance, pH, and rheological performance, as well as their in vivo compatibility with skin and antioxidant efficiency. Full article

(This article belongs to the Special Issue Skin and Formulation)

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24 pages, 6052 KiB

Open AccessArticle

Increased Therapeutic Efficacy of SLN Containing Etofenamate and Ibuprofen in Topical Treatment of Inflammation

by Giuliana Mancini, Lídia M. D. Gonçalves, Joana Marto, Filomena A. Carvalho, Sandra Simões, Helena Margarida Ribeiro and António J. Almeida

Pharmaceutics 2021, 13(3), 328; https://doi.org/10.3390/pharmaceutics13030328 - 3 Mar 2021

Cited by 13 | Viewed by 3579

Abstract

Innovative formulations, including solid lipid nanoparticles (SLNs), have been sought to improve skin permeation of non-steroidal anti-inflammatory drugs (NSAIDs). The present study explores the use of SLNs, prepared using a fusion-emulsification method, to increase skin permeation and in vivo activity of two relevant NSAIDs: A liquid molecule (etofenamate) and a solid one (ibuprofen), formulated in a 2% hydroxypropyl methylcellulose gel through the gelation of SLN suspensions. Compritol^® 888 ATO and Tween^® 80 were used as a solid lipid and a surfactant, respectively. All production steps were up scalable, resulting in SLNs with high encapsulation efficiency (>90%), a mean particle size of <250 nm, a polydispersity index <0.2, and that were stable for 12 months. In vitro permeation, using human skin in Franz diffusion cells, showed increased permeation and similar cell viability in Df and HaCaT cell lines for SLN formulations when compared to commercial formulations of etofenamate (Reumon^® Gel 5%) and ibuprofen (Ozonol^® 5%). In vivo activity in the rat paw edema inflammation model showed that SLN hydrogels containing lower doses of etofenamate (8.3 times lower) and ibuprofen (16.6 times lower) produced similar effects compared to the commercial formulations, while decreasing edema and inflammatory cell infiltration, and causing no histological changes in the epidermis. These studies demonstrate that encapsulation in SLNs associated to a suitable hydrogel is a promising technological approach to NSAIDs dermal application. Full article

(This article belongs to the Special Issue Skin and Formulation)

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26 pages, 10639 KiB

Open AccessArticle

Design and Characterization of Elastic Artificial Skin Containing Adenosine-Loaded Solid Lipid Nanoparticles for Treating Wrinkles

by Sooho Yeo, Sukkyun Jung, Heui Kyoung Cho, Young Ho Kim, Gi Hwan Kim, Dohyun Kim, Byoung Hyen Ko and Jaehwi Lee

Pharmaceutics 2021, 13(1), 33; https://doi.org/10.3390/pharmaceutics13010033 - 28 Dec 2020

Cited by 13 | Viewed by 3861

Abstract

Adenosine (AD), which is used for treating wrinkles, exhibits poor skin permeation. The aim of the present study was to develop a cross-linked silicone-based cellulose elastomer as an elastic artificial skin for the treatment of skin wrinkles, a biocompatible lipid-based nano-carrier for enhancing the skin permeation of AD, and a formulation consisting of the lipid-based carrier incorporated in the elastic artificial skin. AD-loaded solid lipid nanoparticles (SLNs) were prepared using a double-emulsion method. Particle characteristics and mechanical properties of SLNs and elastic artificial skin, respectively, were assessed. Skin permeation was evaluated using SkinEthic RHE tissue, a reconstructed human epidermis model. The mean particle size and zeta potential for SLNs ranged from 123.57 to 248.90 nm and −13.23 to −41.23 mV, respectively. The components of neither SLNs nor the elastic artificial skin were cytotoxic, according to cell- and tissue-viability assays and EU classification. SLNs and the elastic artificial skin exhibited sustained drug release for 48 h. The amount of AD released from SLNs and elastic artificial skin was approximately 10 times and 5 times higher, respectively, than that from AD solution. Therefore, elastic artificial skin incorporated with AD-loaded SLNs may serve as a promising topical delivery system for cosmeceutical treatment of skin wrinkles. Full article

(This article belongs to the Special Issue Skin and Formulation)

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14 pages, 2065 KiB

Open AccessArticle

The Influence of Increasing Concentrations of AMPD on the Efficacy of Its Penetration into a Model Skin Sebum Layer

by Agnieszka Kostrzębska and Witold Musiał

Pharmaceutics 2020, 12(12), 1228; https://doi.org/10.3390/pharmaceutics12121228 - 18 Dec 2020

Cited by 5 | Viewed by 2329

Abstract

Alcoholamines are widely used as auxiliary substances in various topical preparations. Their impact on the components of skin sebum allows them to be used in preparations that cleanse the skin of sebum in hair follicles. We measured the effects of various concentrations of aqueous solutions of AMPD (2-amino-2-methyl-1,3-propanediol) on model skin sebum. The volume of reacted sebum was calculated using two methods: optical assessment of the interaction of alcoholamines with the components of model skin sebum and determination of the reacted volume of model skin sebum based on the measurements of changes in the pH of the AMPD solutions. Both methods showed that the most favorable AMPD concentration for model sebum penetration was approximately 1–2%. Lower values of alcoholamine caused premature exhaustion from the solution. Excessively high concentrations resulted in the formation of a dense layer of products hindering effective skin cleansing. Full article

(This article belongs to the Special Issue Skin and Formulation)

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17 pages, 3147 KiB

Open AccessArticle

Topical Delivery of Carvedilol Loaded Nano-Transfersomes for Skin Cancer Chemoprevention

by Mengbing Chen, Md Abdullah Shamim, Ayaz Shahid, Steven Yeung, Bradley T. Andresen, Jeffrey Wang, Vijaykumar Nekkanti, Frank L. Meyskens, Jr., Kristen M. Kelly and Ying Huang

Pharmaceutics 2020, 12(12), 1151; https://doi.org/10.3390/pharmaceutics12121151 - 27 Nov 2020

Cited by 42 | Viewed by 4020

Abstract

The β-blocker carvedilol has been shown to prevent skin carcinogenesis in vitro and in vivo. Since systemic absorption of the β-blocker may cause cardiovascular disturbance, we developed a carvedilol loaded transfersome for skin-targeted delivery. Transfersomes were prepared using phospholipids and surfactants at various ratios and characterized. One formulation (F18) selected for further analysis was composed of carvedilol, soy phosphatidylcholine, and Tween-80 at a ratio of 1:3:0.5, which had a particle size of 115.6 ± 8.7 nm, a zeta potential of 11.34 ± 0.67 mV, and an encapsulation efficiency of 93.7 ± 5.1%. F18 inhibited EGF-induced neoplastic transformation of mouse epidermal JB6 P+ cells at non-toxic concentrations, while only high concentrations induced cytotoxicity in JB6 P+ and human keratinocytes HaCaT. Compared to the free drug, F18 released through the dialysis membrane and permeated through the porcine ear skin at a slower rate, but similarly depositing the drug in the epidermis and dermis of the skin. Consistently, surface application of F18 on reconstructed full-thickness human skin showed slower drug permeation, while it suppressed ultraviolet-induced DNA damage, inflammatory gene expression, and apoptosis. These data indicate that transfersome is a promising topical delivery system of carvedilol for preventing ultraviolet-induced skin damage and carcinogenesis. Full article

(This article belongs to the Special Issue Skin and Formulation)

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17 pages, 4855 KiB

Open AccessArticle

Tofacitinib Loaded Squalenyl Nanoparticles for Targeted Follicular Delivery in Inflammatory Skin Diseases

by Rebekka Christmann, Duy-Khiet Ho, Jenny Wilzopolski, Sangeun Lee, Marcus Koch, Brigitta Loretz, Thomas Vogt, Wolfgang Bäumer, Ulrich F. Schaefer and Claus-Michael Lehr

Pharmaceutics 2020, 12(12), 1131; https://doi.org/10.3390/pharmaceutics12121131 - 24 Nov 2020

Cited by 18 | Viewed by 3788

Abstract

Tofacitinib (TFB), a Janus kinase inhibitor, has shown excellent success off-label in treating various dermatological diseases, especially alopecia areata (AA). However, TFB’s safe and targeted delivery into hair follicles (HFs) is highly desirable due to its systemic adverse effects. Nanoparticles (NPs) can enhance targeted follicular drug delivery and minimize interfollicular permeation and thereby reduce systemic drug exposure. In this study, we report a facile method to assemble the stable and uniform 240 nm TFB loaded squalenyl derivative (SqD) nanoparticles (TFB SqD NPs) in aqueous solution, which allowed an excellent loading capacity (LC) of 20%. The SqD NPs showed an enhanced TFB delivery into HFs compared to the aqueous formulations of plain drug in an ex vivo pig ear model. Furthermore, the therapeutic efficacy of the TFB SqD NPs was studied in a mouse model of allergic dermatitis by ear swelling reduction and compared to TFB dissolved in a non-aqueous mixture of acetone and DMSO (7:1 v/v). Whereas such formulation would not be acceptable for use in the clinic, the TFB SqD NPs dispersed in water illustrated a better reduction in inflammatory effects than plain TFB’s aqueous formulation, implying both encouraging good in vivo efficacy and safety. These findings support the potential of TFB SqD NPs for developing a long-term topical therapy of AA. Full article

(This article belongs to the Special Issue Skin and Formulation)

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20 pages, 6723 KiB

Open AccessArticle

Extraction, Characterization and Incorporation of Hypericum scruglii Extract in Ad Hoc Formulated Phospholipid Vesicles Designed for the Treatment of Skin Diseases Connected with Oxidative Stress

by Mohamad Allaw, Maria Manconi, Matteo Aroffu, Francesca Marongiu, Marco Porceddu, Gianluigi Bacchetta, Iris Usach, Rita Abi Rached, Hiba N. Rajha, Richard G. Maroun, Jose Luis Pedraz, Tania B. Lopez-Mendez, Anna Maria Fadda and Maria Letizia Manca

Pharmaceutics 2020, 12(11), 1010; https://doi.org/10.3390/pharmaceutics12111010 - 23 Oct 2020

Cited by 13 | Viewed by 3421

Abstract

An extract of Hypericum scruglii, an endangered endemic plant of Sardinia (Italy), was prepared and characterized. It was loaded in special phospholipid vesicles, glycerosomes, which were modified by adding maltodextrin (glucidex) and a polymer (gelatin or hyaluronan). The corresponding liposomes were also prepared and used as reference. The vesicles disclosed suitable physicochemical features for skin delivery. Indeed, their mean diameter ranged from 120 to 160 nm, they were homogeneously dispersed (polydispersity index ≤ 0.30), and their zeta potential was highly negative (~−45 mV). The vesicle dispersions maintained unchanged characteristics during 60 days of storage, were highly biocompatible, and were able to protect keratinocytes against damages due to oxidative stress induced by treating them with hydrogen peroxide. Vesicles were also capable of promoting cell proliferation and migration in vitro by means of a scratch wound assay. The results confirmed the fruitful delivery of the extract of H. scruglii in glycerosomes modified with glucidex and gelatin and their promising ability for skin protection and treatment. Full article

(This article belongs to the Special Issue Skin and Formulation)

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14 pages, 310 KiB

Open AccessReview

Topical and Systemic Formulation Options for Cutaneous T Cell Lymphomas

by Taku Fujimura, Ryo Amagai, Yumi Kambayashi and Setsuya Aiba

Pharmaceutics 2021, 13(2), 200; https://doi.org/10.3390/pharmaceutics13020200 - 2 Feb 2021

Cited by 9 | Viewed by 2295

Abstract

Although various anti-cutaneous T-cell lymphoma (CTCL) therapies are available for clinical use, appropriate chemotherapy lines for the treatment of CTCLs have yet to be established. Therefore, to date, various clinical trials for the treatment of advanced CTCLs are ongoing. In this review, we evaluate the therapeutic options that are available in clinical practice for treatment of early- and advanced-stage CTCLs (targeted therapies, histone deacetylase (HDAC) inhibitors, retinoids, interferons, cytotoxic drugs, etc.). We also examine clinical trials of novel regimens for the treatment of CTCLs. Full article

(This article belongs to the Special Issue Skin and Formulation)

17 pages, 1139 KiB

Open AccessReview

Delivery of Insulin via Skin Route for the Management of Diabetes Mellitus: Approaches for Breaching the Obstacles

by Abdul Ahad, Mohammad Raish, Yousef A. Bin Jardan, Abdullah M. Al-Mohizea and Fahad I. Al-Jenoobi

Pharmaceutics 2021, 13(1), 100; https://doi.org/10.3390/pharmaceutics13010100 - 14 Jan 2021

Cited by 38 | Viewed by 7705

Abstract

Insulin is used for the treatment of diabetes mellitus, which is characterized by hyperglycemia. Subcutaneous injections are the standard mode of delivery for insulin therapy; however, this procedure is very often invasive, which hinders patient compliance, particularly for individuals requiring insulin doses four times a day. Furthermore, cases have been reported of sudden hypoglycemia occurrences following multidose insulin injections. Such an invasive and intensive approach motivates the quest for alternative, more user-friendly insulin administration approaches. For example, transdermal delivery has numerous advantages, such as prolonged drug release, low variability in the drug plasma level, and improved patient compliance. In this paper, the authors summarize different approaches used in transdermal insulin delivery, including microneedles, chemical permeation enhancers, sonophoresis, patches, electroporation, iontophoresis, vesicular formulations, microemulsions, nanoparticles, and microdermabrasion. Transdermal systems for insulin delivery are still being widely researched. The conclusions presented in this paper are extracted from the literature, notably, that the transdermal route could effectively and reliably deliver insulin into the circulatory system. Consistent progress in this area will ensure that some of the aforementioned transdermal insulin delivery systems will be introduced in clinical practice and commercially available in the near future. Full article

(This article belongs to the Special Issue Skin and Formulation)

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32 pages, 4495 KiB

Open AccessReview

Nanotechnology-Based Medical Devices for the Treatment of Chronic Skin Lesions: From Research to the Clinic

by Marco Ruggeri, Eleonora Bianchi, Silvia Rossi, Barbara Vigani, Maria Cristina Bonferoni, Carla Caramella, Giuseppina Sandri and Franca Ferrari

Pharmaceutics 2020, 12(9), 815; https://doi.org/10.3390/pharmaceutics12090815 - 27 Aug 2020

Cited by 30 | Viewed by 5763

Abstract

Chronic wounds, such as pressure ulcers, diabetic ulcers, venous ulcers and arterial insufficiency ulcers, are lesions that fail to proceed through the normal healing process within a period of 12 weeks. The treatment of skin chronic wounds still represents a great challenge. Wound medical devices (MDs) range from conventional and advanced dressings, up to skin grafts, but none of these are generally recognized as a gold standard. Based on recent developments, this paper reviews nanotechnology-based medical devices intended as skin substitutes. In particular, nanofibrous scaffolds are promising platforms for wound healing, especially due to their similarity to the extracellular matrix (ECM) and their capability to promote cell adhesion and proliferation, and to restore skin integrity, when grafted into the wound site. Nanotechnology-based scaffolds are emphasized here. The discussion will be focused on the definition of critical quality attributes (chemical and physical characterization, stability, particle size, surface properties, release of nanoparticles from MDs, sterility and apyrogenicity), the preclinical evaluation (biocompatibility testing, alternative in vitro tests for irritation and sensitization, wound healing test and animal wound models), the clinical evaluation and the CE (European Conformity) marking of nanotechnology-based MDs. Full article

(This article belongs to the Special Issue Skin and Formulation)

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