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Kaiyue Yu, Yixuan Wang, Tao Wan, Yuanhao Zhai, Sisi Cao, Wenyi Ruan, Chuanbin Wu, Yuehong Xu
Background: Topical application of tacrolimus (FK506) was effective in the treatment of atopic dermatitis (AD); however, adverse effects frequently occurred with the increase of FK506 dose during long-term treatment. Objective: The objective of this project was to develop a hybrid skin targeting system encapsulating FK506 based on nicotinamide (NIC) and chitosan nanoparticles (CS-NPs), ie, FK506-NIC-CS-NPs, which took advantages of both of NIC and CS-NPs to obtain the synergetic effects of percutaneous delivery and treatment efficacy enhancement along with dose reduction...
2018: International Journal of Nanomedicine
Jolanta Artym, Maja Kocięba, Ewa Zaczyńska, Michał Zimecki, Małgorzata Jeleń, Beata Morak-Młodawska, Krystian Pluta, Katarzyna Kaleta-Kuratewicz, Jan P Madej, Piotr Kuropka, Jan Kuryszko
In this work we investigated the efficacy of two topically applied azaphenothiazine derivatives, 9-chloro-6-acetylaminobutylquinobenzo[3,2-b][1,4]thiazine (compound 4) and 6-chloroethylureidoethyldiquino[3,2-b;2';3'-e][1,4]thiazine (compound 5), in the amelioration of inflammatory symptoms of contact sensitivity (CS) to oxazolone in mice, in relation to the commercial ointment Protopic® (tacrolimus), the reference drug. The compounds were administered 24 h following elicitation of CS and, 24 h later, the parameters of inflammation, such as ear edema, blood composition, leukocyte level, numbers of cells in the draining lymph nodes, histological picture of the inflamed tissue, and the morphometric analysis, were analyzed...
February 2018: Histology and Histopathology
Vedrana Savić, Marija Todosijević, Tanja Ilić, Milica Lukić, Evgenia Mitsou, Vassiliki Papadimitriou, Spyridon Avramiotis, Bojan Marković, Nebojša Cekić, Snežana Savić
In order to improve skin penetration of tacrolimus we aimed to develop potentially non-irritant, lecithin-based microemulsions containing ethanol, isopropanol and/or propylene glycol as cosurfactants, varying caprylic/capric triglycerides and propylene glycol monocaprylate as oil phase. The influence of excipients on the size of microemulsion region in pseudo-ternary phase diagrams and their ability to form different types of microemulsions was evaluated. The comprehensive physicochemical characterization of microemulsions and the evaluation of their structure was performed, while the localization of tacrolimus in microemulsions was further investigated using electron paramagnetic resonance spectroscopy...
August 30, 2017: International Journal of Pharmaceutics
Tao Wan, Jingtong Pan, Yueming Long, Kaiyue Yu, Yixuan Wang, Wenhui Pan, Wenyi Ruan, Mengyao Qin, Chuanbin Wu, Yuehong Xu
In this study, we demonstrate for the first time the dual roles of Tocopheryl Polyethylene Glycol 1000 Succinate (TPGS) based microemulsion (ME) for tacrolimus (TAC) to enhance TAC percutaneous delivery and anti-psoriatic efficacy. The ME formulation was developed and optimized based on pseudo-ternary phase diagrams combined with in vitro permeation. The result of Fourier transform infrared spectroscopy (FTIR) demonstrated that TAC was completely solubilized in the TPGS-ME. In vitro permeation studies showed that TPGS-ME enhanced TAC permeation through and into the skin, and the enhanced deposition of TAC in the normal or psoriatic skin was further confirmed in vivo...
August 7, 2017: International Journal of Pharmaceutics
Tao Wan, Wenhui Pan, Yueming Long, Kaiyue Yu, Sibo Liu, Wenyi Ruan, Jingtong Pan, Mengyao Qin, Chuanbin Wu, Yuehong Xu
The hybrid system based on nanoparticles (NPs) self-assembled by the conjugations of hyaluronic acid with cholesterol (HA-Chol NPs) combined with nicotinamide (NIC) for tacrolimus (FK506), ie, FK506 NPs-NIC, has been confirmed to exhibit a significant synergistic effect on FK506 permeation through and into intact skin; thus, it may be a promising approach for FK506 to effectively treat skin diseases. The aim of this study was to evaluate its potential for the treatment of psoriasis. In vitro permeation through the psoriatic skin was carried out, and the results revealed that the combination of NPs with NIC exhibited a significant synergistic effect on FK506 deposition within the psoriatic skin (3...
2017: International Journal of Nanomedicine
Xing-Hai Jin, Juhyeon Lim, Dong Hae Shin, Jeehye Maeng, Kyunglim Lee
Our previous study showed that dimerized translationally controlled tumor protein (dTCTP) plays a role in the pathogenesis of allergic diseases, such as asthma and allergic rhinitis. A 7-mer peptide, called dTCTP-binding peptide 2 (dTBP2), binds to dTCTP and inhibits its cytokine-like effects. We therefore examined the protective effects of dTBP2 in house dust mite-induced atopic dermatitis (AD)-like skin lesions in Nishiki-nezumi Cinnamon/Nagoya (NC/Nga) mice. We found that topical administration of dTBP2 significantly reduced the AD-like skin lesions formation and mast cell infiltration in NC/Nga mice, similarly to the response seen in the Protopic (tacrolimus)-treated group...
January 26, 2017: International Journal of Molecular Sciences
Doris Gabriel, Thibault Mugnier, Herve Courthion, Ksanthi Kranidioti, Niki Karagianni, Maria C Denis, Maria Lapteva, Yogeshvar Kalia, Michael Möller, Robert Gurny
We have developed a composite hydrogel for improved topical delivery of the poorly soluble drug Tacrolimus (TAC) to psoriasis lesions. TAC is efficiently solubilized in methoxy poly- (ethylene glycol) hexyl substituted poly-(lactic acid) (mPEGhexPLA) based nanocarriers. For convenient and patient-friendly topical administration, TAC loaded polymeric nanocarriers were incorporated in a Carbopol® based hydrogel, to yield a composite hydrogel formulation (TAC composite hydrogel). TAC composite hydrogel was designed to have superior pharmaceutical formulation properties, delivery efficiency and local bioavailability, compared to currently available paraffin-based TAC ointments...
November 28, 2016: Journal of Controlled Release: Official Journal of the Controlled Release Society
Gloria López-Valverde, Elena Garcia-Martin, José Manuel Larrosa-Povés, Vicente Polo-Llorens, Luis E Pablo-Júlvez
PURPOSE: The purpose of this study is to describe a case of ocular rosacea with a very complex evolution. Rosacea is a chronic dermatological disease that may affect the ocular structures up to 6-72% of all cases. This form is often misdiagnosed, which may lead to long inflammatory processes with important visual consequences for affected patients. Therefore, an early diagnosis and an adequate treatment are important. METHODS: We report the case of a 43-year-old patient who had several relapses of what seemed an episode of acute bacterial conjunctivitis...
January 2016: Case Reports in Ophthalmology
Alfonso Pastor-Clerigues, Adela Serrano, Javier Milara, Ezequiel Marti-Bonmati, Francisco J Lopez-Perez, Sara Garcia-Montanes, Joan Sanfeliu, Ana C Saval-Victoria, Julio Cortijo
PURPOSE: Tacrolimus ocular preparations are commonly employed in autoimmune or inflammatory ocular disorders. However, currently there are not yet approved ocular formulations. Tacrolimus ocular side effects have been reported in clinical use, so the evaluation of different pharmaceutical preparations is mandatory. In this study, the local corneal tolerance and safety profile of three common tacrolimus 0.03% pharmaceutical preparations were evaluated. MATERIAL AND METHODS: Corneal irritation and permeability of tacrolimus preparations were evaluated with the bovine corneal opacity and permeability (BCOP) test...
July 2016: Current Eye Research
Norashikin Shamsudin, Suraiya H Hussein, Hermawan Nugroho, Mohd Hani Ahmad Fadzil
UNLABELLED: An objective tool to quantify treatment response in vitiligo is currently lacking. This study aimed to objectively evaluate the treatment response in vitiligo by using a computerised digital imaging analysis system (C-DIAS) and to compare it with the physician's global assessment (PGA). Tacrolimus ointment 0.1% (Protopic; Astellas Pharma Tech,Toyama, Japan) was applied twice daily on selected lesions which were photographed every 6 weeks for 24 weeks. The primary efficacy end-point was the mean percentage of repigmentation (MPR), as assessed by the digital method (MPR-C-DIAS) or by the PGA...
November 2015: Australasian Journal of Dermatology
Maria Lapteva, Karine Mondon, Michael Möller, Robert Gurny, Yogeshvar N Kalia
Tacrolimus (TAC) suffers from poor cutaneous bioavailability when administered topically using conventional vehicles with the consequence that although it is indicated for the treatment of atopic dermatitis, it has poor efficacy against psoriasis. The aim of this work was to formulate TAC loaded polymeric micelles using the biodegradable and biocompatible methoxy-poly(ethylene glycol)-dihexyl substituted polylactide (MPEG-dihexPLA) diblock copolymer and to investigate their potential for targeted delivery of TAC into the epidermis and upper dermis...
September 2, 2014: Molecular Pharmaceutics
Y E Kim, S-C Eun
OBJECTIVE: FK-506 (tacrolimus) is a well known immunosuppressive agent used to prevent allograft rejection. The need for chronic allograft immunosuppression and the consequent harmful systemic effects preclude the use of tissue allograft as a routine surgical reconstructive option. This study assessed the effects of FK-506 ointment (Protopic) therapy versus subcutaneous injection of FK-506 (Prograf) on rat skin graft model. METHODS: Donor Wistar rat dorsal skin was grafted to recipient Sprague-Dawley rats...
May 2014: Transplantation Proceedings
Hyekyung Ha, Hoyoung Lee, Chang Seob Seo, Hye-Sun Lim, Jun Kyoung Lee, Mee-Young Lee, Hyeunkyoo Shin
BACKGROUND: Artemisia capillaries Thunb. (AC) has been used to treat inflammatory and hepatic disorders such as hepatic injury, hepatic fibrosis and hepatitis. However, the efficacy of AC against atopic dermatitis (AD), an inflammatory disease, has not been examined. In the present study, AC was evaluated for anti-inflammatory and anti-AD effects using both in vitro and in vivo systems. METHODS: The contents of six compounds (chlorogenic acid, caffeic acid, isochlorogenic acid A, hyperoside, isoquercitrin and scoparone) in AC were simultaneously assayed using HPLC system...
March 14, 2014: BMC Complementary and Alternative Medicine
Masayuki Yamanaka, Shoji Yokota, Yasunori Iwao, Shuji Noguchi, Shigeru Itai
We developed an oil/water-type tacrolimus (FK506) cream formulation as an alternative to Protopic ointment for atopic dermatitis treatment. We determined the effects of solvents used in topical preparations on FK506 solubility and stability, and evaluated FK506 transdermal absorption into rat skin from solutions, emulsions, and creams. Screening indicated that diethyl sebacate (DES), isopropyl myristate (IPM), propylene glycol (PG), and oleyl alcohol (OA) were adequate FK506 solvents. When FK506 solutions prepared using these solvents were transdermally administered, AUC0-24 values for DES and IPM were higher than or similar to that for 0...
April 10, 2014: International Journal of Pharmaceutics
Abdulrahman Mohammed Al-Amri
PURPOSE: To evaluate the long-term clinical outcomes of 0.1% tacrolimus dermatologic ointment (Protopic) in cases of refractory atopic keratoconjunctivitis (AKC). DESIGN: Prospective, nonrandomized, noncontrolled case series. METHODS: Twenty-two eyes from 11 patients with severe AKC who were treated with 0.1% tacrolimus ointment were followed prospectively. The mean age of the patients was 32.27 ± 12.7 years (range, 19-61 years). Each patient completed a follow-up period of at least 48 months, during which the signs and symptoms of AKC were assessed...
February 2014: American Journal of Ophthalmology
A Kyriakou, A Patsatsi, C Patsialas, D Sotiriadis
Plasma cell balanitis of Zoon (PCBZ) and plasma cell vulvitis (PCV) are characterized as idiopathic, benign, chronic irritant mucositis. The clinical symptoms and signs usually persist or reappear after treatment withdrawal. Therefore, many therapies have been tried and are available. Recently, several reports of PCBZ and PCV treated with calcineurin inhibitors, tacrolimus and pimecrolimus, have been reported in the literature. We present 9 cases of PCBZ treated with tacrolimus 0.1% ointment (Protopic, Toyama, Japan) that showed good therapeutic results within 4 weeks of treatment, and we review the literature of PCBZ and PCV and their response to these topical immunomodulators...
2014: Dermatology: International Journal for Clinical and Investigative Dermatology
João Paulo Marinho Resende, Maria das Graças Afonso Miranda Chaves, Fernando Monteiro Aarestrup, Beatriz Vieira Aarestrup, Sergio Olate, Henrique Duque Netto
Oral lichen planus (OLP) is considered a chronic autoimmune inflammatory disease and its presence may be related to increased emotional stress. The clinical relevance of OLP is the possibility of developing a squamous cell carcinoma, the etiology of which is still unknown. The aim of this study is to treat OLP lesions resistant to conventional treatment with corticosteroids, using topical tacrolimus 0.1% (Protopic(®)) twice a day for a period of eight weeks. Fifteen patients were selected who had filled out a history form and a visual analog scale for pain before and after treatment...
2013: International Journal of Clinical and Experimental Medicine
George D Kymionis, Nektarios E Klados, George A Kontadakis, Dimitrios G Mikropoulos
PURPOSE: To report 2 cases of superior limbic keratoconjunctivitis (SLK) treated with topical tacrolimus 0.03% ointment (Protopic; Fujisawa Healthcare). METHODS: A female patient aged 52 years and a male patient aged 21 years presented with SLK in both eyes. Both patients had previously received several treatments [such as topical steroids and lubrication, contact lenses, silicone punctal plugs, and vitamin A eye drops], with no improvement. Because of poor response to initial management, the authors started treatment with topical tacrolimus 0...
November 2013: Cornea
Stephan Dähnhardt-Pfeiffer, Dorothee Dähnhardt, Matthias Buchner, Kersten Walter, Ehrhardt Proksch, Regina Fölster-Holst
BACKGROUND: The skin barrier plays a crucial role in the pathophysiology of atopic dermatitis. The quality of the skin barrier can be assessed using a new semi-quantitative method to measure intercellular lipid lamellae. This procedure was used to evaluate the influence of the topical application of the calcineurin inhibitor tacrolimus 0.1% ointment (Protopic®) versus mometasone furoate cream (Ecural®) on the quality of the skin barrier. PATIENTS AND METHODS: 20 adult patients with active atopic dermatitis (SCORAD 10-63) were included in an open, non-interventional study...
May 2013: Journal der Deutschen Dermatologischen Gesellschaft, Journal of the German Society of Dermatology: JDDG
Guiling Li, Yating Fan, Chao Fan, Xinru Li, Xiaoning Wang, Mei Li, Yan Liu
The purpose of this work was to prepare and characterize a novel ethosomal carrier for tacrolimus, an immunosuppressant treating atopic dermatitis (AD), and to investigate inhibition action upon allergic reactions of mice aiming at improving pharmacological effect for tacrolimus in that commercial tacrolimus ointment (Protopic®) with poor penetration capability exhibited weak impact on AD compared with common glucocorticoid. Results indicated that the ethosomes showed lower vesicle size and higher encapsulation efficiency (EE) as compared with traditional liposomes with cholesterol...
September 2012: European Journal of Pharmaceutics and Biopharmaceutics
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