AAPS-FDA Workshop White Paper: Microdialysis Principles, Application and Regulatory Perspectives

Chaurasia, Chandra S.; Müller, Markus; Bashaw, Edward D.; Benfeldt, Eva; Bolinder, Jan; Bullock, Ross; Bungay, Peter M.; DeLange, Elizabeth C. M.; Derendorf, Hartmut; Elmquist, William F.; Hammarlund‐Udenaes, Margareta; Joukhadar, Christian; Kellogg, Dean L.; Lunte, Craig E.; Nordstrom, Carl; Rollema, Hans; Sawchuk, Ronald J.; Cheung, Belinda W.Y.; Shah, Vinod P.; Ståhle, Lars; Ungerstedt, Urban; Welty, Devin; Yeo, Helen

doi:10.1007/s11095-006-9206-z

Cited by 246 publications

(157 citation statements)

References 57 publications

Supporting

Mentioning

152

Contrasting

Unclassified

Order By: Relevance

“…The absence of a target molecule in the dialysate can be due to actual absence of the agent in the tissue but can also be explained by methodological issues such as inadequate analytical sensitivity or binding of the target molecule to the membrane. Many experimental conditions, including probe membrane composition and surface area, perfusate flow rate, temperature, nature of the dialyzed tissue and physicochemical properties of the target molecules need to be considered in the experimental design [18].…”

Section: Introductionmentioning

confidence: 99%

Identification of Lipid Mediators in Peripheral Human Tissues Using an Integrative In Vivo Microdialysis Approach

2016

J Anal Bioanal Tech

View full text Add to dashboard Cite

Endocannabinoids and related N-acylethanolamines (NAEs) are lipid mediators involved in a number of physiological and pathological mechanisms in peripheral tissues. Microdialysis (MD) technique allows continues sampling of endogenous substances in the interstitial fluids of the tissues. The main limitation of MD sampling of lipophilic compounds is low recovery due to adsorption to the MD system and particularly to the catheter membranes. In this in vivo study microdialysate samples were collected from human trapezius muscle and forearm skin. The levels of arachidonoylethanolamide (AEA), 2-arachidonoylglycerol (2-AG), oleoylethanolamide (OEA), palmitoylethanolamide (PEA), and stearoylethanolamide (SEA) were analyzed in both microdialysate and in catheter membrane samples using liquid chromatography tandem mass spectrometry. OEA, PEA and SEA were identified in all microdialysate and catheter membrane samples from trapezius and skin. 2-AG was found in all catheter membrane samples from both tissues but not in the actual microdialysate. In conclusion sampling of OEA, PEA and SEA was achievable from trapezius and skin with the presented MD set-up. 2-AG is present in both trapezius muscle and skin tissue but adsorbs to the membranes in a higher extent than the NAEs. Furthermore, consideration of data conserved in the membrane during an MD experiment could be a relevant and more broadly applicable extension of MD sampling methodology which could fill an "information gap" and enhance an adequate interpretation of microdialysate data outcomes

show abstract

Section: Introductionmentioning

confidence: 99%

Identification of Lipid Mediators in Peripheral Human Tissues Using an Integrative In Vivo Microdialysis Approach

2016

J Anal Bioanal Tech

View full text Add to dashboard Cite

show abstract

“…In addition, microdialysis has its own limitations (45). While retrodialysis is a useful and simple calibration method commonly used to estimate recoveries, a drawback of this method is that possible changes in recovery over time are not measured (45)(46)(47)(48). Recovery is influenced by various solute and tissue-related factors.…”

Section: Discussionmentioning

confidence: 99%

Microdialysis-directed Intra-tumor Pharmacokinetic Modeling of Methotrexate in Mice and Humans

Alsulimani¹,

Kim²,

Sani³

2016

J Pharm Pharm Sci

View full text Add to dashboard Cite

-Purpose. To develop a quantitative pharmacokinetic model to characterize the disposition of methotrexate (MTX) at tumor site in tumor-bearing mice and to predict MTX concentrations in the human tumor. Methods. The plasma profiles of MTX were obtained from normal mice, while microdialysis technique was employed to characterize the time course of MTX in tumor from breast tumor-bearing mice. Disposition profiles of plasma and tumor were analyzed by a hybrid physiologically-based pharmacokinetic (hPBPK) model that incorporates physiologically-relevant parameters such as tumor blood flow and volume, while plasma concentrations were used as a forcing input into the vascular-interstitial spaces of the tumor. The plasma profiles were initially described by a biexponential decay model to obtain a forcing function that enters into the vascularinterstitial spaces in the tumor. Using a defined forcing function, the tumor free concentrations were fitted to the hPBPK model. Based on the model developed, sensitivity analysis was conducted with a perturbation of PK parameters to predict different scenarios of intratumoral MTX transport. The relevant physiological PK parameters from the mouse model were then scaled-up and utilized to simulate human tumor concentrations. Results. The mouse hPBPK model adequately characterized the concentration-time profiles of MTX in both plasma and tumor and produced various transfer rate constants between plasma and tumor. Our model was also able to reasonably predict MTX concentrations in the human tumor when human physiological data were utilized. Conclusions. The hPBPK model was able to quantitatively characterize the atypical transport of MTX in the tumor, supporting the idea that microdialysis is a valuable tool to study tumor biodistribution of drugs and to predict tumor concentrations in humans based on the pre-clinical data. This information can ultimately aid in the development of anticancer drugs with improved PK profiles.

show abstract

“…In vitro drug release is sensitive to several physical and chemical parameters, such as drug solubility, particle size, and the arrangement and rheological property of semisolid dosage forms. In addition, in vitro release test is easier to be carried out than in vivo test, and also gives insights into drug permeation mechanism [21]. IVRT involves the application of a drug product on to a membrane (synthetic membrane, excised animal skin, or excised human skin) that separates the donor and receiver chambers.…”

Section: In-vitro Studiesmentioning

confidence: 99%

Untitled

2018

RJLBPCS

View full text Add to dashboard Cite

ABSTRACT:The assessment of the bioequivalence of topical products not intended for absorption into the systemic circulation has presented a formidable challenge over the years. In particular, dermatological dosage forms such as creams, ointments, lotions and gels, apart from those containing topical corticosteroids, cannot readily be assessed for bioequivalence using "conventional" methodology and the only recourse to-date has been to undertake tedious, time consuming and expensive clinical end-point trials for such products. Although the human skin blanching assay (HSBA), also known as the vasoconstriction assay (VCA) has been successfully used for dermatological products containing topical corticosteroids but no surrogate methodology for the bioequivalence assessment of other topical dermatological products such as those containing nonsteroidal anti-infl ammatory drugs, anti-fungals, antibiotics and antivirals has been successfully accepted by regulatory agencies. The regulatory agencies and pharmaceutical industries are forging ahead to the development of new surrogate BE assessment approaches for other topical dermatological products. These promising approaches include dermatopharmacokinetic study (DPK), dermal microdialysis (DMD), in vitro studies, pharmacokinetic study (PK), near-infrared spectrometry (NIR), and confocal Raman spectroscopy (CRS). In addition, the expansion of biowaivers for topical dermatological products has been explored by pharmaceutical scientists.

show abstract

AAPS-FDA Workshop White Paper: Microdialysis Principles, Application and Regulatory Perspectives

Cited by 246 publications

References 57 publications

Identification of Lipid Mediators in Peripheral Human Tissues Using an Integrative In Vivo Microdialysis Approach

Identification of Lipid Mediators in Peripheral Human Tissues Using an Integrative In Vivo Microdialysis Approach

Microdialysis-directed Intra-tumor Pharmacokinetic Modeling of Methotrexate in Mice and Humans

Untitled

Contact Info

Product

Resources

About