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

Holmgaard, Rikke; Nielsen, Jesper Bo; Benfeldt, Eva

doi:10.1159/000314698

Cited by 80 publications

(59 citation statements)

References 223 publications

(119 reference statements)

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“…Another area of development is the use of microdialysis for cutaneous bioavailability of drugs that has not come too far in spite of promising results (93)(94)(95)(96). In comparison to blister techniques, it can be said to be very sophisticated, although still being limited by adsorption phenomena.…”

Section: Development Of Microdialysis and Alternativesmentioning

confidence: 99%

Microdialysis as an Important Technique in Systems Pharmacology—a Historical and Methodological Review

Hammarlund‐Udenaes

2017

AAPS J

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Abstract.Microdialysis has contributed with very important knowledge to the understanding of target-specific concentrations and their relationship to pharmacodynamic effects from a systems pharmacology perspective, aiding in the global understanding of drug effects. This review focuses on the historical development of microdialysis as a method to quantify the pharmacologically very important unbound tissue concentrations and of recent findings relating to modeling microdialysis data to extrapolate from rodents to humans, understanding distribution of drugs in different tissues and disease conditions. Quantitative microdialysis developed very rapidly during the early 1990s. Method development was in focus in the early years including development of quantitative microdialysis, to be able to estimate true extracellular concentrations. Microdialysis has significantly contributed to the understanding of active transport at the blood-brain barrier and in other organs. Examples are presented where microdialysis together with modeling has increased the knowledge on tissue distribution between species, in overweight patients and in tumors, and in metabolite contribution to drug effects. More integrated metabolomic studies are still sparse within the microdialysis field, although a great potential for tissue and disease-specific measurements is evident.

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Section: Development Of Microdialysis and Alternativesmentioning

confidence: 99%

Microdialysis as an Important Technique in Systems Pharmacology—a Historical and Methodological Review

Hammarlund‐Udenaes

2017

AAPS J

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“…21 The preliminary results have demonstrated the ability of microdialysis probes to continuously monitor the concentrations of drugs in the dermis in vivo. 22 Microdialysis has also been successfully used to obtain reliable pharmacokinetic data for routine estimation of cutaneous permeation. 23 In the present study, we employed in vivo microdialysis to compare a novel transdermal drug delivery using ethosomes with one using a conventional tincture.…”

Section: Introductionmentioning

confidence: 99%

Evaluation of psoralen ethosomes for topical delivery in rats by using in vivo microdialysis

Zhang

Shen

Zhao

2014

IJN

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This study aimed to improve skin permeation and deposition of psoralen by using ethosomes and to investigate real-time drug release in the deep skin in rats. We used a uniform design method to evaluate the effects of different ethosome formulations on entrapment efficiency and drug skin deposition. Using in vitro and in vivo methods, we investigated skin penetration and release from psoralen-loaded ethosomes in comparison with an ethanol tincture. In in vitro studies, the use of ethosomes was associated with a 6.56-fold greater skin deposition of psoralen than that achieved with the use of the tincture. In vivo skin microdialysis showed that the peak concentration and area under the curve of psoralen from ethosomes were approximately 3.37 and 2.34 times higher, respectively, than those of psoralen from the tincture. Moreover, it revealed that the percutaneous permeability of ethosomes was greater when applied to the abdomen than when applied to the chest or scapulas. Enhanced permeation and skin deposition of psoralen delivered by ethosomes may help reduce toxicity and improve the efficacy of long-term psoralen treatment.

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“…Several experimental methods have been elaborated for this purpose, for instance, skin blister fluid and microdialysis, particularly in the skin which is described in papers of Holmgaard (2010), Klimowicz (2007) and Olczyk (2008). Apart from these two methods, using labeled compounds is one of the techniques frequently applied to estimate drug penetration into the skin and other body tissue or organs (Bielecka-Grzela et al 2002).…”

Section: Introductionmentioning

confidence: 99%

The penetration of topically applied ointment containing hyaluronic acid in rabbit tissues

Birkenfeld¹,

Parafiniuk²,

Bielecka-Grzela³

et al. 2011

Polish Journal of Veterinary Sciences

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The properties of hyaluronic acid used for treatment of acute and chronic joint disease are known for many years and this compound is widely used both in humans and animals.To obtain a therapeutic effect of a certain drug, the appropriate concentration in the target organ or tissue is important. The application of labeled compounds is one of the frequently applied techniques to estimate drug penetration into the skin and other body tissues or organs. The aim of the study was to evaluate the penetration of hyaluronic acid labeled with I-131 through the skin and its distribution within the knee joint and other internal organs in rabbits after a topical application of an ointment containing hyaluronic acid.The experiment was performed on 22 albino rabbits divided into control and examined groups. Fifteen rabbits were exposed to the multicomponent ointment containing hyaluronic acid labeled with I-131. Time of exposure was 48 hours.Hyaluronate penetrated to a high degree into the examined tissues. No significant differences in terms of leg tissue activity were observed between a leg tissue exposed to labeled ointment and that unexposed, suggesting that after topical administration, the active component of the ointment is delivered to the joint via the blood stream.Hyaluronate applied topically penetrates through the skin into the rabbit tissues and organs and into the joint fluid of both legs (exposed and not exposed). This route of administration seems to be useful for this drug delivery and allows to avoid unnecessary side effects.

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

Cited by 80 publications

References 223 publications

Microdialysis as an Important Technique in Systems Pharmacology—a Historical and Methodological Review

Microdialysis as an Important Technique in Systems Pharmacology—a Historical and Methodological Review

Evaluation of psoralen ethosomes for topical delivery in rats by using in vivo microdialysis

The penetration of topically applied ointment containing hyaluronic acid in rabbit tissues

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