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Pharmaceutics
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Drugs in Dermatology: Topical Agent, Cosmetics, Dermatological Drug Delivery, Natural...
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Drugs in Dermatology: Topical Agent, Cosmetics, Dermatological Drug Delivery, Natural Product in Dermatology

A special issue of Pharmaceutics (ISSN 1999-4923). This special issue belongs to the section "Physical Pharmacy and Formulation".

Deadline for manuscript submissions: closed (10 March 2023) | Viewed by 33995

Special Issue Editor

Prof. Dr. Seyeon Park

E-Mail Website
Guest Editor
Department of Applied Chemistry, Dongduk Women’s University, Seoul 136-714, Republic of Korea
Interests: anesthesia; cancer; mitochondrial dynamics; pharmacoproteomics

Special Issue Information

Dear Colleagues,

Skin disease is influenced by both intrinsic (genetics) and extrinsic factors (environmental exposure). Pharmacologic agents are commonly prescribed for the treatment of many dermatological diseases. Many medicine remedies have been used based on scientific evidence and the results of randomized controlled trials. Nonetheless, there is a lack of standardization of bioactive ingredients in alterative and traditional medicine. Certain drug entities are used for different indications than those indicated by their FDA approval. Additionally, many dermatological drugs are also used in topical application to the site. Natural products such as polyphenols have been proven to be beneficial for reducing the risk of developing skin disease. Although various flavonoids exert useful biological activities, some have limited bioavailability due to low solubility and penetration. As a result, supramolecular complexation of carbohydrates or delivery systems with flavonoids has been suggested to increase solubility and thus improve bioavailability.

In this Special Issue, original research articles and reviews are welcome. Research areas may include (but are not limited to) the following:

  • Pharmaceutical formulation of dermatological drugs;
  • Delivery and controlled-release systems for topical agents or cosmetics;
  • Natural products in dermatology;
  • Drug targeting for dermal tissue;
  • Functional ingredients of cosmetics: pharmacogenetics and pharmacogenomics;
  • Target discovery for skin aging or hair regrowth.

We look forward to receiving your contributions.

Prof. Dr. Seyeon Park
Guest Editor

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.

Please visit the Instructions for Authors page before submitting a manuscript. The Article Processing Charge (APC) for publication in this open access journal is 2900 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

  • skin disease
  • dermatological drugs
  • topical agent
  • cosmetics
  • natural products
  • drug targeting
  • functional ingredients
  • skin aging
  • hair regrowth

Published Papers (9 papers)

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Research

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24 pages, 11077 KiB  
Article
Nanoemulsions Based on Sunflower and Rosehip Oils: The Impact of Natural and Synthetic Stabilizers on Skin Penetration and an Ex Vivo Wound Healing Model
by Cynthia Nara Pereira Oliveira, Marcel Nani Leite, Natália Aparecida de Paula, Yugo Araújo Martins, Sonia Aparecida Figueiredo, Marco Andrey Cipriani Frade and Renata Fonseca Vianna Lopez
Pharmaceutics 2023, 15(3), 999; https://0-doi-org.brum.beds.ac.uk/10.3390/pharmaceutics15030999 - 20 Mar 2023
Cited by 5 | Viewed by 1922
Abstract
Vegetable oils offer excellent biological properties, but their high lipophilicity limits their bioavailability. This work aimed to develop nanoemulsions based on sunflower and rosehip oils and to evaluate their wound-healing activity. The influence of phospholipids of plant origin on nanoemulsions’ characteristics was investigated. [...] Read more.
Vegetable oils offer excellent biological properties, but their high lipophilicity limits their bioavailability. This work aimed to develop nanoemulsions based on sunflower and rosehip oils and to evaluate their wound-healing activity. The influence of phospholipids of plant origin on nanoemulsions’ characteristics was investigated. A nanoemulsion prepared with a mixture of phospholipids and synthetic emulsifiers (Nano-1) was compared with another prepared only with phospholipids (Nano-2). The healing activity was evaluated in wounds induced in human organotypic skin explant culture (hOSEC) based on histological and immunohistochemical analysis. The hOSEC wound model was validated, showing that high nanoparticle concentration in the wound bed interferes with cell mobility and the ability to respond to the treatment. Nanoemulsions were 130 to 370 nm, with a concentration of 1013 particles/mL, and a low potential to induce inflammatory processes. Nano-2 was three times larger than Nano-1 but less cytotoxic and could target the oils to the epidermis. Nano-1 permeated intact skin to the dermis and showed a more prominent healing effect than Nano-2 in the hOSEC wound model. Changes in the lipid nanoemulsion stabilizers impacted the cutaneous and cellular penetration of the oils, cytotoxicity, and healing kinetics, resulting in versatile delivery systems. Full article
(This article belongs to the Special Issue Drugs in Dermatology: Topical Agent, Cosmetics, Dermatological Drug Delivery, Natural Product in Dermatology)
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22 pages, 6593 KiB  
Article
Topical Delivery of Atraric Acid Derived from Stereocaulon japonicum with Enhanced Skin Permeation and Hair Regrowth Activity for Androgenic Alopecia
by Sultan Pulat, Laxman Subedi, Prashant Pandey, Suresh R. Bhosle, Jae-Seoun Hur, Jung-Hyun Shim, Seung-Sik Cho, Ki-Taek Kim, Hyung-Ho Ha, Hangun Kim and Jin Woo Park
Pharmaceutics 2023, 15(2), 340; https://0-doi-org.brum.beds.ac.uk/10.3390/pharmaceutics15020340 - 19 Jan 2023
Cited by 3 | Viewed by 2115
Abstract
Atraric acid (AA) is a phenolic compound isolated from Stereocaulon japonicum that has demonstrated anti-androgen properties and was used to design an alternative formulation for the treatment of alopecia. This new topical formulation was designed using a solvent mixture system composed of ethanol [...] Read more.
Atraric acid (AA) is a phenolic compound isolated from Stereocaulon japonicum that has demonstrated anti-androgen properties and was used to design an alternative formulation for the treatment of alopecia. This new topical formulation was designed using a solvent mixture system composed of ethanol as a volatile vehicle, oleic acid as a permeation enhancer, and water for skin hydration. The ideal topical AA formulation (AA–TF#15) exhibited an 8.77-fold higher human skin flux and a 570% increase in dermal drug deposition, compared to 1% (w/w) AA in ethanol. In addition, compared to other formulations, AA–TF#15 (1% [w/w] AA) activated keratinocytes and human dermal papilla cell proliferation at a concentration of 50 µM AA, which is equivalent to 50 µM minoxidil. Moreover, AA–TF#15 treatment produced a significant increase in hair regrowth by 58.0% and 41.9% compared to the 1% (w/w) minoxidil and oral finasteride (1 mg/kg)-treated mice. In addition, AA–TF#15 showed a higher expression level of aldehyde dehydrogenase 1, β-catenin, cyclin D1, and pyruvate kinase M2 proteins in the skin of AA–TF#15-treated mice compared to that of those treated with minoxidil and oral finasteride. These findings suggest AA–TF#15 is an effective formulation for the treatment of scalp androgenic alopecia. Full article
(This article belongs to the Special Issue Drugs in Dermatology: Topical Agent, Cosmetics, Dermatological Drug Delivery, Natural Product in Dermatology)
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23 pages, 5893 KiB  
Article
A Novel Perilla frutescens (L.) Britton Cell-Derived Phytocomplex Regulates Keratinocytes Inflammatory Cascade and Barrier Function and Preserves Vaginal Mucosal Integrity In Vivo
by Giovanna Pressi, Giovanna Rigillo, Paolo Governa, Vittoria Borgonetti, Giulia Baini, Raffaella Rizzi, Chiara Guarnerio, Oriana Bertaiola, Marco Frigo, Matilde Merlin, Stefania Paltrinieri, Roberto Zambonin, Stefano Pandolfo and Marco Biagi
Pharmaceutics 2023, 15(1), 240; https://0-doi-org.brum.beds.ac.uk/10.3390/pharmaceutics15010240 - 10 Jan 2023
Cited by 5 | Viewed by 1830
Abstract
In the last years, the medicinal plant Perilla frutescens (L.) Britton has gained scientific interest because leaf extracts, due to the presence of rosmarinic acid and other polyphenols, have shown anti-allergic and skin protective potential in pre-clinical studies. Nevertheless, the lack of standardized [...] Read more.
In the last years, the medicinal plant Perilla frutescens (L.) Britton has gained scientific interest because leaf extracts, due to the presence of rosmarinic acid and other polyphenols, have shown anti-allergic and skin protective potential in pre-clinical studies. Nevertheless, the lack of standardized extracts has limited clinical applications to date. In this work, for the first time, a standardized phytocomplex of P. frutescens, enriched in rosmarinic acid and total polyphenols, was produced through innovative in vitro cell culture biotechnology and tested. The activity of perilla was evaluated in an in vitro inflammatory model of human keratinocytes (HaCaT) by monitoring tight junctions, filaggrin, and loricrin protein levels, the release of pro-inflammatory cytokines and JNK MAPK signaling. In a practical health care application, the perilla biotechnological phytocomplex was tested in a multilayer model of vaginal mucosa, and then, in a preliminary clinical observation to explore its capacity to preserve vaginal mucosal integrity in women in peri-menopause. In keratinocytes cells, perilla phytocomplex demonstrated to exert a marked activity in epidermis barrier maintenance and anti-inflammatory effects, preserving tight junction expression and downregulating cytokines release through targeting JNK activation. Furthermore, perilla showed positive effects in retaining vaginal mucosal integrity in the reconstructed vaginal mucosa model and in vivo tests. Overall, our data suggest that the biotechnological P. frutescens phytocomplex could represent an innovative ingredient for dermatological applications. Full article
(This article belongs to the Special Issue Drugs in Dermatology: Topical Agent, Cosmetics, Dermatological Drug Delivery, Natural Product in Dermatology)
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15 pages, 1519 KiB  
Article
Development of a Standardized Method for Measuring Bioadhesion and Mucoadhesion That Is Applicable to Various Pharmaceutical Dosage Forms
by Lola Amorós-Galicia, Anna Nardi-Ricart, Clara Verdugo-González, Carmen Martina Arroyo-García, Encarna García-Montoya, Pilar Pérez-Lozano, Josep Mª Suñé-Negre and Marc Suñé-Pou
Pharmaceutics 2022, 14(10), 1995; https://0-doi-org.brum.beds.ac.uk/10.3390/pharmaceutics14101995 - 21 Sep 2022
Cited by 9 | Viewed by 2307
Abstract
Although some methods for measuring bioadhesion/mucoadhesion have been proposed, a standardized method is not yet available. This is expected to hinder systematic comparisons of results across studies. This study aimed to design a single/systematic in vitro method for measuring bioadhesion/mucoadhesion that is applicable [...] Read more.
Although some methods for measuring bioadhesion/mucoadhesion have been proposed, a standardized method is not yet available. This is expected to hinder systematic comparisons of results across studies. This study aimed to design a single/systematic in vitro method for measuring bioadhesion/mucoadhesion that is applicable to various pharmaceutical dosage forms. To this end, we measured the peak force and work of adhesion of minitablets, pellets, and a bioadhesive emulsion using a texture analyzer. Porcine tissue was used to simulate human stomach/skin conditions. The results of these formulations were then compared to those for formulations without the bioadhesive product. We conducted a case study to assess the stability of a bioadhesive emulsion. The results for the two parameters assessed were contact time = 60 s and contact force = 0.5 N at a detachment speed of 0.1 mm/s. Significant differences were observed between the bioadhesive and control formulations, thus demonstrating the adhesive capacity of the bioadhesive formulations. In this way, a systematic method for assessing the bioadhesive capacity of pharmaceutical dosage forms was developed. The method proposed here may enable comparisons of results across studies, i.e., results obtained using the same and different pharmaceutical formulations (in terms of their bioadhesion/mucoadhesion capacity). This method may also facilitate the selection of potentially suitable formulations and adhesive products (in terms of bioadhesive properties). Full article
(This article belongs to the Special Issue Drugs in Dermatology: Topical Agent, Cosmetics, Dermatological Drug Delivery, Natural Product in Dermatology)
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15 pages, 3087 KiB  
Article
Antipsoriatic Potential of Quebecol and Its Derivatives
by Corinne Bouchard, Alexe Grenier, Sébastien Cardinal, Sarah Bélanger, Normand Voyer and Roxane Pouliot
Pharmaceutics 2022, 14(6), 1129; https://0-doi-org.brum.beds.ac.uk/10.3390/pharmaceutics14061129 - 26 May 2022
Cited by 1 | Viewed by 2386
Abstract
Psoriasis is a chronic inflammatory skin disease mainly characterized by the hyperproliferation and abnormal differentiation of the epidermal keratinocytes. An interesting phenolic compound, namely quebecol (2,3,3-tri-(3-methoxy-4-hydroxyphenyl)-1-propanol) (compound 1, CPD1), was isolated from maple syrup in 2011 and was recently synthesized. Quebecol and [...] Read more.
Psoriasis is a chronic inflammatory skin disease mainly characterized by the hyperproliferation and abnormal differentiation of the epidermal keratinocytes. An interesting phenolic compound, namely quebecol (2,3,3-tri-(3-methoxy-4-hydroxyphenyl)-1-propanol) (compound 1, CPD1), was isolated from maple syrup in 2011 and was recently synthesized. Quebecol and its derivatives ethyl 2,3,3-tris(3-hydroxy-4-methoxyphenyl)propenoate (compound 2, CPD2) and bis(4-hydroxy-3-methoxyphenyl)methane (compound 3, CPD3) have shown antiproliferative and anti-inflammatory potential, making them promising candidates for the treatment of psoriasis. This study aimed to evaluate the antipsoriatic potential of quebecol and its derivatives on psoriatic skin substitutes produced according to the self-assembly method. A sulforhodamine B (SRB) assay determining the concentration that inhibits 20% of cell growth (IC20) was performed for CPD1, CPD2 and CPD3, and their IC20 values were 400, 150 and 350 μM, respectively. At these concentrations, cell viability was 97%, 94% and 97%, respectively. The comparative control methotrexate (MTX) had a cell viability of 85% at a concentration of 734 μM. Histological analyses of psoriatic skin substitutes treated with CPD1, CPD2 and CPD3 exhibited significantly reduced epidermal thickness compared with untreated psoriatic substitutes, which agreed with a decrease in keratinocyte proliferation as shown by Ki67 immunofluorescence staining. The immunofluorescence staining of differentiation markers (keratin 14, involucrin and loricrin) showed improved epidermal differentiation. Taken together, these results highlight the promising potential of quebecol and its derivatives for the treatment of psoriasis. Full article
(This article belongs to the Special Issue Drugs in Dermatology: Topical Agent, Cosmetics, Dermatological Drug Delivery, Natural Product in Dermatology)
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14 pages, 4427 KiB  
Article
The Potential Anti-Photoaging Effect of Photodynamic Therapy Using Chlorin e6-Curcumin Conjugate in UVB-Irradiated Fibroblasts and Hairless Mice
by Ga-Hee Hur, A-Reum Ryu, Yong-Wan Kim and Mi-Young Lee
Pharmaceutics 2022, 14(5), 968; https://0-doi-org.brum.beds.ac.uk/10.3390/pharmaceutics14050968 - 30 Apr 2022
Cited by 9 | Viewed by 2257
Abstract
Photodynamic therapy (PDT) has been used to treat cancers and non-malignant skin diseases. In this study, a chlorin e6–curcumin conjugate (Ce6-PEG-Cur), a combination of chlorin e6 (Ce6) and curcumin via a PEG linker, was used as a photosensitizer. The in vitro and in [...] Read more.
Photodynamic therapy (PDT) has been used to treat cancers and non-malignant skin diseases. In this study, a chlorin e6–curcumin conjugate (Ce6-PEG-Cur), a combination of chlorin e6 (Ce6) and curcumin via a PEG linker, was used as a photosensitizer. The in vitro and in vivo effects of PDT using Ce6-PEG-Cur were analyzed in UVB-irradiated fibroblasts and hairless mice. The UVB-induced expression of MMPs was reduced in Hs68 fibroblast cells, and procollagen type Ⅰ expression was enhanced by Ce6-PEG-Cur-mediated PDT on a Western blotting gel. Moreover, UVB-induced collagen levels were restored upon application of Ce6-PEG-Cur-mediated PDT. Ce6-PEG-Cur-mediated PDT inhibited the expression of phosphorylated p38 in the MAPK signaling pathway, and it reduced the expression of phosphorylated NF-κB. In animal models, Ce6-PEG-Cur-mediated PDT inhibited the expression of MMPs, whereas procollagen type Ⅰ levels were enhanced in the dorsal skin of UVB-irradiated mice. Moreover, UVB-induced dorsal roughness was significantly reduced following Ce6-PEG-Cur-mediated PDT treatment. H&E staining and Masson’s trichrome staining showed that the thickness of the epidermal region was reduced, and the density of collagen fibers increased. Taken together, Ce6-PEG-Cur-mediated PDT might delay and improve skin photoaging by ultraviolet light, suggesting its potential for use as a more effective photo-aging treatment. Full article
(This article belongs to the Special Issue Drugs in Dermatology: Topical Agent, Cosmetics, Dermatological Drug Delivery, Natural Product in Dermatology)
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10 pages, 2225 KiB  
Article
Anti-Psoriasis Effect of Diclofenac and Celecoxib Using the Tail Model for Psoriasis
by Diana Ana-Maria Nițescu, Horia Păunescu, Alina Elena Ștefan, Laurențiu Coman, Corneliu Cristian Georgescu, Andrei Constantin Stoian, Daniela Gologan, Ion Fulga and Oana Andreia Coman
Pharmaceutics 2022, 14(4), 885; https://0-doi-org.brum.beds.ac.uk/10.3390/pharmaceutics14040885 - 18 Apr 2022
Cited by 2 | Viewed by 2425
Abstract
Non-steroidal anti-inflammatory drugs (NSAIDs) showed effects in some hyperproliferative dermatologic pathologies. The aim of the study is the assessment of anti-psoriasis effect of diclofenac and celecoxib using a mice tail model. The topical application of substances on the proximal mice tails was performed [...] Read more.
Non-steroidal anti-inflammatory drugs (NSAIDs) showed effects in some hyperproliferative dermatologic pathologies. The aim of the study is the assessment of anti-psoriasis effect of diclofenac and celecoxib using a mice tail model. The topical application of substances on the proximal mice tails was performed for two weeks. The effects on the epidermal granular layer and mean epidermal thickness (excluding the stratum corneum) were evaluated using hematoxylin–eosin staining. Orthokeratosis degree and percentual drug activity were calculated. A positive control group treated with tretinoin and two negative controls (white soft paraffin and untreated mice) were used. Orthokeratosis degree significantly increased in all the NSAIDs groups (celecoxib 1%, 2% and diclofenac 1%, 2%) and in the tretinoin 0.05% group, versus negative controls. Celecoxib 1% and 2%, tretinoin 0.05% and white soft paraffin significantly increased mean epidermal thickness, versus untreated mice. The values obtained in the case of celecoxib 2% ointment regarding the orthokeratosis degree and percentual drug activity are providing premises for further investigations regarding this effect and the mechanisms of action involved. Celecoxib 2% had the greatest percentual drug activity and is a promising substance for the anti-psoriasis topical treatment. Along with the COX-2 inhibition, celecoxib might have an anti-psoriasis effect by other independent mechanisms. Full article
(This article belongs to the Special Issue Drugs in Dermatology: Topical Agent, Cosmetics, Dermatological Drug Delivery, Natural Product in Dermatology)
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Review

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24 pages, 2709 KiB  
Review
Modulation of Hair Growth Promoting Effect by Natural Products
by Seyeon Park and Joomin Lee
Pharmaceutics 2021, 13(12), 2163; https://0-doi-org.brum.beds.ac.uk/10.3390/pharmaceutics13122163 - 15 Dec 2021
Cited by 15 | Viewed by 9782
Abstract
A large number of people suffer from alopecia or hair loss worldwide. Drug-based therapies using minoxidil and finasteride for the treatment of alopecia are available, but they have shown various side effects in patients. Thus, the use of new therapeutic approaches using bioactive [...] Read more.
A large number of people suffer from alopecia or hair loss worldwide. Drug-based therapies using minoxidil and finasteride for the treatment of alopecia are available, but they have shown various side effects in patients. Thus, the use of new therapeutic approaches using bioactive products to reduce the risk of anti-hair-loss medications has been emphasized. Natural products have been used since ancient times and have been proven safe, with few side effects. Several studies have demonstrated the use of plants and their extracts to promote hair growth. Moreover, commercial products based on these natural ingredients have been developed for the treatment of alopecia. Several clinical, animal, and cell-based studies have been conducted to determine the anti-alopecia effects of plant-derived biochemicals. This review is a collective study of phytochemicals with anti-alopecia effects, focusing mainly on the mechanisms underlying their hair-growth-promoting effects. Full article
(This article belongs to the Special Issue Drugs in Dermatology: Topical Agent, Cosmetics, Dermatological Drug Delivery, Natural Product in Dermatology)
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Other

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23 pages, 6162 KiB  
Systematic Review
Colchicine in Managing Skin Conditions: A Systematic Review
by Stefano Dastoli, Steven Paul Nisticò, Pietro Morrone, Cataldo Patruno, Antonio Leo, Rita Citraro, Luca Gallelli, Emilio Russo, Giovambattista De Sarro and Luigi Bennardo
Pharmaceutics 2022, 14(2), 294; https://0-doi-org.brum.beds.ac.uk/10.3390/pharmaceutics14020294 - 27 Jan 2022
Cited by 22 | Viewed by 7006
Abstract
(1) Background: Colchicine is a natural alkaloid with anti-inflammatory properties used to treat various disorders, including some skin diseases. This paper aims to incorporate all the available studies proposing colchicine as a treatment alternative in the management of cutaneous conditions. (2) Methods: In [...] Read more.
(1) Background: Colchicine is a natural alkaloid with anti-inflammatory properties used to treat various disorders, including some skin diseases. This paper aims to incorporate all the available studies proposing colchicine as a treatment alternative in the management of cutaneous conditions. (2) Methods: In this systematic review, the available articles present in various databases (PubMed, Scopus-Embase, and Web of Science), proposing colchicine as a treatment for cutaneous pathological conditions, have been selected. Exclusion criteria included a non-English language and non-human studies. (3) Results: Ninety-six studies were included. Most of them were case reports and case series studies describing colchicine as single therapy, or in combination with other drugs. Hidradenitis suppurativa, pyoderma gangrenosum, erythema nodosum, erythema induratum, storage diseases, perforating dermatosis, bullous diseases, psoriasis, vasculitis, acne, urticaria, stomatitis, actinic keratosis, and pustular dermatosis were the main diseases discussed in literature. Although the therapeutic outcomes were variable, most of the studies reported, on average, good clinical results (4) Conclusions: Colchicine could be, as a single therapy or in combination with other drugs, a possible treatment to manage several skin diseases. Full article
(This article belongs to the Special Issue Drugs in Dermatology: Topical Agent, Cosmetics, Dermatological Drug Delivery, Natural Product in Dermatology)
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