Tacrolimus ointment improves psoriasis in a microplaque assay

Abstract

Tacrolimus (FK506) is an effective and well tolerated immunosuppressant used to prevent allograft rejection. We describe the evaluation of two tacrolimus ointment formulations for treatment of chronic plaque-type psoriasis. This was a microplaque assay with randomized, double-blind design. Sixteen patients (15 men, one woman, all white and 28-69 years old) with chronic plaque-type psoriasis participated. Six different ointments were applied to discrete microplaques, 17 mm in diameter, on a descaled psoriasis lesion: these were tacrolimus ointment with diisopropyl adipate as penetration enhancer, tacrolimus ointment without diisopropyl adipate, 0.1% betamethasone 17alpha-valerate ointment, 0.005% calcipotriol ointment and, as controls, the ointment bases for tacrolimus and betamethasone. Ointments were reapplied and the area was sealed every 2-3 days during the 14-day treatment period. After 7 and 14 days, erythema and infiltration were graded on a scale of 0-4, and superficial blood flow was measured with a laser Doppler flowmeter. Epidermal thickness was measured histologically at the end of treatment. Compared with the vehicle controls, sites treated with tacrolimus ointment (with or without penetration enhancer) showed a significant reduction in erythema and infiltration (P < 0. 001), a significant reduction in superficial blood flow (P < 0.01) and a significant decrease in epidermal thickness (P < or = 0.001). Results for betamethasone and calcipotriol, when compared with the vehicle controls, were similar. These results suggest that, under conditions of descaling and occlusion, tacrolimus ointment is effective in the treatment of psoriasis.

An Aliphatic Ester Diisopropyl Sebacate Exhibited an Adjuvant Effect on Fluorescein Isothiocyanate-Induced Contact Hypersensitivity Mouse Models

“…DIPA is used for cosmetics and drug formulations. 13,14) DIPA is an ester made of an aliphatic dicarboxylic acid of carbon number 6 (C6). DIPS is another aliphatic ester but has a dicarboxylic acid of C10.…”

Effects of nanoparticles with hydrotropic nicotinamide on tacrolimus: permeability through psoriatic skin and antipsoriatic and antiproliferative activities

“…Several reports demonstrated that topical application of FK506 ointment was only effective under occlusion or to some specific regions of the body where the skin was thinner and more permeable, such as the face and intertriginous areas. [23][24][25][26][27] The poor efficacy of FK506 for topical therapy was attributed to its high hydrophobicity and high molecular weight (822.05 Da), which prevent it from penetrating into and through the skin. In our previous study, 28 we have formulated a hybrid nanoparticle system for FK506 percutaneous delivery.…”

Efficacy of 0.1% tacrolimus ointment in chronic plaque psoriasis: A randomized double-blind placebo-controlled study

“…Bu çalışmanın hemen ardından Remitz ve ark. topikal uygulanan %0,3 takrolimus, %0,005 kalsipotriol, %0,1 betametazonun plasebo ile karşılaştırmalı etkisini değerlendirmek için önceden %2 salisilik asitle inceltilen psoriatik plaklara bu ilaçları 2 hafta boyunca her 2-3 günde bir oklüzyonla uygulamışlardır 10 . Tedavi sonunda plasebo ile karşılaştırıldığında takrolimus uygulanan alanda eritem ve infiltrasyonda azalma izlenirken, kalsipotriol ile takrolimus arasındaki belirgin fark saptanmamıştır.…”

“…Psoriasiste topikal takrolimusun etkinliğinin değerlendirildiği çalışmalarda özellikle fasiyal, invers ve genital psoriasiste başarılı sonuçlar bildirilmiştir [5][6][7][8][9] . Bunun yanında kronik plak tipi psoriasiste etkinliği plaseboya benzer, plasebodan üstün ve potent steroidlere eşdeğer şeklinde çelişkili sonuçlar bildirilmektedir [10][11][12] . Son yıllarda topikal takrolimus tırnak tutulumunda da etkili olarak bildirilmiştir 13 .…”