Diclofenac concentrations in defined tissue layers after topical administration

Müller, Markus; Mascher, Hermann; Kikuta, Christian; Schäfer, Sabine; Brunner, Martin; Dorner, Guido T.; Eichler, Hans Georg

doi:10.1016/s0009-9236(97)90032-1

Cited by 91 publications

(64 citation statements)

References 16 publications

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“…Following this, several studies have demonstrated a lack of correlation between the depth of the probe and the drug concentration [35,41,42,44,45] .…”

Section: Measuring Probe Depth By Ultrasound Scanningmentioning

confidence: 99%

Microdialysis Sampling for Investigations of Bioavailability and Bioequivalence of Topically Administered Drugs: Current State and Future Perspectives

Holmgaard

Nielsen

Benfeldt

2010

Skin Pharmacol Physiol

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Microdialysis (MD) in the skin is a unique technique for in vivo sampling of topically as well as systemically administered drugs at the site of action, e.g. sampling the unbound tissue concentrations in the dermis and subcutaneous tissue. MD as a research method has undergone significant development, improvement and validation during the last decade and has proved to be a versatile, safe and valuable tool for pharmacokinetic and pharmacodynamic studies. This review gives an overview of the current state and future perspectives of dermal MD sampling. Methodological issues such as choice of instrumentation, calibration and experimental procedures are discussed along with the analytical considerations necessary for successful sampling. Clinical MD studies in the skin are reviewed with emphasis on pharmacokinetic studies of topically applied drugs with or without impairment of skin barrier function by skin disease or barrier perturbation. A comparison between MD and other tissue sampling techniques reveals the advantages and limitations of the method. Subsequently, an in-depth discussion of the application of MD for the evaluation of bioavailability and bioequivalence of topical formulations is concluded by the current regulatory point of view. The future perspective includes further expansion and validation of the use of MD in the experimental and clinical setting as well as in the optimization of the method for regulatory purposes, i.e. the commercialization of bioequivalent, generic drug products.

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“…Following this, several studies have demonstrated a lack of correlation between the depth of the probe and the drug concentration [35,41,42,44,45] .…”

Section: Measuring Probe Depth By Ultrasound Scanningmentioning

confidence: 99%

Microdialysis Sampling for Investigations of Bioavailability and Bioequivalence of Topically Administered Drugs: Current State and Future Perspectives

Holmgaard

Nielsen

Benfeldt

2010

Skin Pharmacol Physiol

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“…Four sterilized probes were inserted 3 h (shown for HETE analyses) and 24 h (shown for isoprostane analyses) after UVB irradiation intracutaneously, at least 5 cm apart into the UV-irradiated skin of the lateral arm without any local anaesthetic. According to investigations of other groups including Müller et al [13], the presumed probe depth ranged between 0.8 and 1.2 mm.…”

Section: Microdialysismentioning

confidence: 95%

Detection of Monohydroxyeicosatetraenoic Acids and F<sub>2</sub>-Isoprostanes in Microdialysis Samples of Human UV-Irradiated Skin byGas Chromatography-Mass Spectrometry

Grundmann

Wiswedel²,

Hirsch³

et al. 2003

Skin Pharmacol Physiol

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UV irradiation of the human skin leads to induction of oxidative stress and inflammation mediated by reactive oxygen radicals, lipid peroxidation, liberation of arachidonic acid from membrane phospholipids and formation of prostaglandins and leucotrienes. We investigated ‘lipid mediators’, such as F₂-isoprostanes (8-iso-PGF_2α, 9α,11α-PGF_2α) and monohydroxyeicosatetraenoic acids (HETEs)in the dermal interstitial fluid obtained by a cutaneous microdialysis technique. Defined areas on the volar forearm of 10 healthy volunteers were exposed to UVB irradiation (20–60 mJ/cm²). Microdialysis membranes were cutaneously inserted beneath the irradiated area. The probes were perfused with isotonic saline solution, and microdialysate samples were collected at 20-min intervals up to 4–5 h. Oxidized arachidonic acid derivatives (2-, 3-, 5-, 8–12- and 15-HETEs, 8-iso-PGF_2α and 9α,11α-PGF_2α) could be detected and quantified in microdialysates of normal skin in the picomole (HETEs) and femtomole (isoprostanes) range and after UVB irradiation using sensitive gas chromatography-mass spectrometry/negative ion chemical ionization. UVB irradiation enhanced the levels of 8-iso-PGF_2α after 24 h significantly, whereas the HETE levels were slightly increased within shorter time intervals (3 h after UVB irradiation). Further investigations have to show whether these new findings are relevant to validate therapeutic strategies for topical and systemic UV prevention agents or for monitoring of specific therapeutic strategies in inflammatory skin disorders.

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“…Gel, liquid or cream form of medicines are applied to skin and these forms serves as a medium for the effectiveness of ultrasound. However, transfer of the ultrasound energy from a material to another is depending on the physical properties of these substances (1,21,27).…”

Section: Introductionmentioning

confidence: 99%

Comparison of the effects of phonophoresis and ultrasound therapy on recovery of experimental tenorrhaphy in rabbits

DÜZGÜN¹

2015

Ankara Üniversitesi Veteriner Fakültesi Dergisi

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Tendon ruptures occur generally at distal portions of extremities and require relatively long recovery period. Traumatic ruptures of Achilles tendon need 6-8 weeks of immobility period including pre and postoperative days. In order to avoid other orthopedical problems by this application and to speed up the recovery period, postoperative local administrations are done. Therapeutic Ultrasound (TUS) is one of these applications. Phonophoresis is the local absorbing procedure of some drugs by means of TUS which is applied to the affected area. Forty male New Zealand rabbits were used in the study which were one year old and mean 3 kg bodyweight. The rabbits were divided into 4 groups and experimental Achilles tendon rupture was created in both legs of all rabbits and repaired immediately by tenorrhaphy. The right legs of rabbits of groups 1 and 3 were treated postoperatively with TUS for 10 days. The right legs of rabbits in groups 2 and 4 were treated postoperatively with phonophoresis for 10 days. Left legs of all rabbits served as the control group. All rabbits were euthanized at the end of the 30th day. Samples which were taken from groups 1 and 2 were examined histopathologically and those in groups 3 and 4 were examined biomechanically. In biomechanical investigations, the rupture points of the tendons in N (Newton) were compared. At the end of the study, it was concluded that TUS is a superior for tendon healing when compared to phonophoresis. Deneysel olarak tenorafi yapılan tavşanlarda ultrason terapi ile fonoforezisin iyileşme üzerine etkilerinin karşılaştırılması Özet: Tendo kopukları çoğunlukla ekstremitelerin distal kısımlarında meydana gelmekte ve uzun süreli bir iyileşme periyodu gerektirmektedir. Travmatik aşil tendo kopuklarında operasyon öncesi ve sonrasını da kapsayan 6-8 haftalık bir bandaj uygulaması ile hareketsizlik sağlanmaktadır. Bu uygulamanın neden olacağı diğer ortopedik problemleri önlemek ve iyileşme periyodunu hızlandırabilmek amacıyla, operasyon sonrası lokal uygulamalar yapılmaktadır. Ultrason terapi (TUS) bunlardan biridir. Fonoforezis ise emilim özelliği olan ilaçların TUS eşliğinde lokal olarak bölgeye emdirilmesidir. Deneysel çalışmamızda 40 adet erkek, 1 yaşında, ortalama 3 kg ağırlığında, Yeni Zelanda tavşanı kullanıldı. Tavşanlar 4 gruba ayrıldı ve tüm tavşanların her iki arka bacağında deneysel Aşil tendo rupturu oluşturuldu ve hemen akabinde tenorafi ile onarıldı. Birinci ve üçüncü gruptaki tavşanların sağ bacaklarına operasyondan sonraki 10 gün boyunca ultrason terapi uygulandı. İkinci ve dördüncü gruptaki tavşanların sağ bacaklarına ise operasyondan sonraki 10 gün boyunca fonoforez uygulandı. Tüm çalışma gruplarında, sol bacaklar kontrol grubunu oluşturdu. Tavşanlar 30. gün sonunda ötenazi edilerek grup 1 ve 2'deki örnekler histopatolojik olarak, grup 3 ve 4'teki örnekler ise biyomekanik olarak incelendi. Biyomekanik inceleme için tendoların kopma noktaları N (Newton) cinsinden karşılaştırıldı. Çalışmanın sonucunda; ultrason terapinin fonoforezle karşılaştırıldığında tend...

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Diclofenac concentrations in defined tissue layers after topical administration

Abstract: We conclude that transdermal penetration of diclofenac, at least after single doses, is not predictable and may strongly be influenced by individual skin properties.

Cited by 91 publications

References 16 publications

Microdialysis Sampling for Investigations of Bioavailability and Bioequivalence of Topically Administered Drugs: Current State and Future Perspectives

Microdialysis Sampling for Investigations of Bioavailability and Bioequivalence of Topically Administered Drugs: Current State and Future Perspectives

Detection of Monohydroxyeicosatetraenoic Acids and F<sub>2</sub>-Isoprostanes in Microdialysis Samples of Human UV-Irradiated Skin byGas Chromatography-Mass Spectrometry

Comparison of the effects of phonophoresis and ultrasound therapy on recovery of experimental tenorrhaphy in rabbits

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