Ex vivo Cutaneous Bioavailability of Topical Mometasone Furoate in an O/W Preparation

被引:2
作者
Wohlrab, Johannes [1 ,2 ]
Neubert, Reinhard H. H. [2 ,3 ]
Sommer, Elfi [2 ]
Michael, Julia [2 ]
机构
[1] Martin Luther Univ Halle Wittenberg, Dept Dermatol & Venereol, Ernst Grube Str 40, DE-06097 Halle, Saale, Germany
[2] Martin Luther Univ Halle Wittenberg, Inst Appl Dermatopharm, Halle, Saale, Germany
[3] Martin Luther Univ Halle Wittenberg, Inst Pharm, Halle, Saale, Germany
关键词
Mometasone furoate; Drug delivery; Cutaneous bioavailability; Penetration; Scratch assay; SCRATCH-WOUND ASSAY; IN-VITRO; TACROLIMUS; 0.1-PERCENT; FLUTICASONE PROPIONATE; HUMAN KERATINOCYTES; HUMAN SKIN; GLUCOCORTICOIDS; CREAM; FIBROBLASTS; EFFICACY;
D O I
10.1159/000452743
中图分类号
R75 [皮肤病学与性病学];
学科分类号
100206 ;
摘要
Mometasone furoate (MMF) is a modern glucocorticoid of the 4th generation, which has been proven not only for inhalation but also for cutaneous treatment. Due to its lipophilic character, it is mainly used in ointments and creams with an outer lipophilic phase (W/O type). However, this study investigated the cutaneous cytotoxicology of MMF and tried to characterize its pharmacokinetic effects on the skin using an O/W preparation. An HPLC method has been developed and validated for the detection of MMF in cutaneous tissue, and concentration-time curves of MMF were created after cutaneous application on unaffected as well as lesional skin. Cytotoxicological characterization was carried out using scratch assays on keratinocytes and cutaneous fibroblasts. Results showed that the condition of the skin had no significant impact on the cutaneous bioavailability of MMF, but the intrinsic effect of the O/W vehicle could be utilized in periods of acute inflammation. Cytotoxicological data gave no new indications regarding the safety of MMF. (C) 2016 S. Karger AG, Basel
引用
收藏
页码:273 / 279
页数:7
相关论文
共 52 条
[1]   Efficacy of mometasone furoate microemulsion in the treatment of erosive-ulcerative oral lichen planus:: pilot study [J].
Aguirre, JM ;
Bagán, JV ;
Rodriguez, C ;
Jimenez, Y ;
Martínez-Conde, R ;
Díaz de Rojas, F ;
Ponte, A .
JOURNAL OF ORAL PATHOLOGY & MEDICINE, 2004, 33 (07) :381-385
[2]   Topical glucocorticoids and the skin-mechanisms of action: an update [J].
Ahluwalia, A .
MEDIATORS OF INFLAMMATION, 1998, 7 (03) :183-193
[3]   Topical tacrolimus 0.1% ointment (Protopic®) reverses nickel contact dermatitis elicited by allergen challenge to a similar degree to mometasone furoate 0.1% with greater suppression of late erythema [J].
Alomar, A ;
Puig, L ;
Gallardo, CM ;
Valenzuela, N .
CONTACT DERMATITIS, 2003, 49 (04) :185-188
[4]  
[Anonymous], 2001, GUID IND BIOAN METH
[5]  
Cattaneo A, 2003, J REPROD MED, V48, P444
[6]  
Chunharas Amornsri, 2002, Journal of the Medical Association of Thailand, V85, P482
[7]  
Cory G, 2011, METHODS MOL BIOL, V769, P25, DOI 10.1007/978-1-61779-207-6_2
[8]   A review of the pharmacology and pharmacokinetics of inhaled fluticasone propionate and mometasone furoate [J].
Crim, C ;
Pierre, LN ;
Daley-Yates, PT .
CLINICAL THERAPEUTICS, 2001, 23 (09) :1339-1354
[9]   Topical glucocorticoid therapy directly induces up-regulation of functional CXCR4 on primed T lymphocytes in the aqueous humor of patients with uveitis [J].
Curnow, SJ ;
Wloka, K ;
Faint, JM ;
Amft, N ;
Cheung, CMG ;
Savant, V ;
Lord, J ;
Akbar, AN ;
Buckley, CD ;
Murray, PI ;
Salmon, M .
JOURNAL OF IMMUNOLOGY, 2004, 172 (11) :7154-7161
[10]   Human keratinocyte isolation and cell culture: A survey of current practices in the UK [J].
Daniels, JT ;
Kearney, JN ;
Ingham, E .
BURNS, 1996, 22 (01) :35-39