The effect of age on serum concentrations of albumin and alpha 1‐acid glycoprotein.

Veering, Bernadette; Burm, A. G. L.; Souverijn, J.H.M.; Serree, J. M. P.; Spierdijk, J.

doi:10.1111/j.1365-2125.1990.tb03620.x

Cited by 102 publications

(55 citation statements)

References 31 publications

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“…However, due to the very low solubility of testosterone in purely aqueous systems, the addition of a solubilising additive was required. In compliance with the OECD guideline 428 and considering the fact that a concentration of 50 g/L is generally accepted to be the mean albumin concentration in human serum (21), 5% m/V BSA was used. As an alternative, addition of HPBCD as a solubilizer was evaluated as well.…”

Section: Resultsmentioning

confidence: 99%

A New Discriminative Criterion for the Development of Franz Diffusion Tests for Transdermal Pharmaceuticals

Baert¹,

Boonen²,

Burvenich³

et al. 2010

J Pharm Pharm Sci

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-PURPOSE.In vitro skin/membrane permeation profiling of topical pharmaceuticals is an important overall quality attribute in the evaluation of product consistency and it is also used for IVIVR (in vitro -in vivo relationship) purposes in product development and change control. Franz diffusion cell (FDC) experiments are emerging as a generally accepted methodology in this field, where the choice of operational conditions requires a data-supported justification towards the discriminating power of the test. A response function is therefore proposed to objectively quantify the discriminating power. METHODS. We evaluated the usefulness of the proposed response function by studying one of the operational conditions, i.e. the influence of receptor medium composition, on the FDC in vitro penetration behaviour of the model compound testosterone formulated in four different topical preparations, using both artificial membranes and dermatomed human skin. A second application is a FDC test system for spilanthol. RESULTS. From the obtained cumulative amount of the active (testosterone or spilanthol) in the receptor fluid versus time curves, the permeability coefficient Kp of testosterone from each formulation was calculated. The evaluation of the discriminating power of the different media was performed using our new objective response function based upon an equal spread criterion of normalised Kp values. CONCLUSION. The proposed new criterion was found to be useful for the rational design of an in vitro diffusion test for transdermal pharmaceuticals. We demonstrated significant differences in discriminating power between the different media used: (a) for testosterone-containing formulations, it was shown that HPBCD-containing media are more discriminative compared to ethanol-or BSA-containing media; (b) for spilanthol-containing formulations, PBS containing formulations also gave better discriminating results than ethanol-based receptor media. __________________________________________________________________________________________

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Section: Resultsmentioning

confidence: 99%

A New Discriminative Criterion for the Development of Franz Diffusion Tests for Transdermal Pharmaceuticals

Baert¹,

Boonen²,

Burvenich³

et al. 2010

J Pharm Pharm Sci

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“…Collectively, these observations suggest that under conditions where FFA levels are elevated, Zn 2+ displaced from serum albumin could bind HRG or fibrinogen to enhance their respective interactions with heparins and induce a pro-coagulatory effect [86], as summarized in Figure 3. In older adults, this may be further compounded as plasma albumin levels are known to decrease with age [87]. An age-related decrease in plasma albumin also correlates with an observable increase in the ratio of FFAs per albumin molecule [88].…”

Section: Ffa-mediated Alterations In Plasma Zinc Speciation: Implicatmentioning

confidence: 99%

Fatty Acid-Mediated Inhibition of Metal Binding to the Multi-Metal Site on Serum Albumin: Implications for Cardiovascular Disease

Blindauer

Khazaipoul²,

Yu³

et al. 2016

CTMC

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(2016) Fatty acid-mediated inhibition of metal binding to the multi-metal site on serum albumin : implications for cardiovascular disease. Current Trends in Medicinal Chemistry, 16. Permanent WRAP URL:http://wrap.warwick.ac.uk/78963 Copyright and reuse:The Warwick Research Archive Portal (WRAP) makes this work by researchers of the University of Warwick available open access under the following conditions. Copyright © and all moral rights to the version of the paper presented here belong to the individual author(s) and/or other copyright owners. To the extent reasonable and practicable the material made available in WRAP has been checked for eligibility before being made available.Copies of full items can be used for personal research or study, educational, or not-for-profit purposes without prior permission or charge. Provided that the authors, title and full bibliographic details are credited, a hyperlink and/or URL is given for the original metadata page and the content is not changed in any way.Publisher's statement: © Bentham Science Publishers. http://dx.doi.org/10.2174/1568026616666160216155927 A note on versions:The version presented here may differ from the published version or, version of record, if you wish to cite this item you are advised to consult the publisher's version. Please see the 'permanent WRAP URL' above for details on accessing the published version and note that access may require a subscription. Abstract: Human serum albumin (HSA) is the major protein in blood plasma and is responsible for circulatory transport of a range of small molecules including fatty acids, metal ions and drugs. We previously identified the major plasma Zn 2+ transport site on HSA and revealed that fatty-acid binding (at a distinct site called the FA2 site) and Zn 2+ binding are interdependent via an allosteric mechanism. Since binding affinities of long-chain fatty acids exceed those of plasma Zn 2+ , this means that under certain circumstances the binding of fatty acid molecules to HSA is likely to diminish HSA Zn 2+ -binding, and hence affects the control of circulatory and cellular Zn 2+ dynamics. This relationship between circulatory fatty acid and Zn 2+ dynamics is likely to have important physiological and pathological implications, especially since it has been recognised that Zn 2+ acts as a signalling agent in many cell types. Fatty acid levels in the blood are dynamic, but most importantly, chronic elevation of plasma fatty acid levels is associated with some metabolic disorders and disease states -including myocardial infarction and other cardiovascular diseases. In this article, we briefly review the metalbinding properties of albumin and highlight the importance of their interplay with fatty acid binding. We also consider the impact of this dynamic link upon levels and speciation of plasma Zn 2+ , its effect upon cellular Zn 2+ homeostasis and its relevance to cardiovascular and circulatory processes in health and disease.

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“…However, in practice, their use was not feasible as they were not biocompatible with the receptor medium for establishing an in vitro-in vivo relationship. 14 As a concentration of 50 g L −1 is quite often accepted as the mean albumin concentrations in human serum, 19 5% of BSA was added in all biorelevant media. As an alternative, 0.5% of HPBCD was also added.…”

Section: Receptor Medium For In Vitro Drug Release Studymentioning

confidence: 99%

“…These membranes are considerably useful for the development and assessment of drug release kinetics from semisolid formulations as they permit the determination of the maximum liberation rate of the active substances from an emulsion matrix. 19 Furthermore, the synthetic membrane model is not influenced by the pH of the formulation, partition coefficient between the drug or the skin, or inherent factors of the source of skin samples, including sex, age, and site of skin excised. 23 The use of an artificial membrane is also justified as it minimizes the number of experimental variables for gaining an in-depth understanding of hormone release.…”

Section: In Vitro Drug Releasementioning

confidence: 99%

TRANSDERMAL FORMULATIONS CONTAINING HUMAN SEXUAL STEROIDS: DEVELOPMENT AND VALIDATION OF METHODS ANDIN VITRODRUG RELEASE

et al. 2014

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In vitro release of bioidentical hormones in four different liposomal transdermal emulsions (containing testosterone, progesterone, estradiol, or estradiol and estriol) was assessed. For this purpose, novel high-performance liquid chromatography methods were developed and validated in an eco-friendly manner and used to determine the in vitro release of such products. The methods were suitable for our intended goal, and the emulsions employed were found to be effective as transporting candidates for the efficient release of hormones in the transdermal delivery of human sexual steroids.

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The effect of age on serum concentrations of albumin and alpha 1‐acid glycoprotein.

Cited by 102 publications

References 31 publications

A New Discriminative Criterion for the Development of Franz Diffusion Tests for Transdermal Pharmaceuticals

A New Discriminative Criterion for the Development of Franz Diffusion Tests for Transdermal Pharmaceuticals

Fatty Acid-Mediated Inhibition of Metal Binding to the Multi-Metal Site on Serum Albumin: Implications for Cardiovascular Disease

TRANSDERMAL FORMULATIONS CONTAINING HUMAN SEXUAL STEROIDS: DEVELOPMENT AND VALIDATION OF METHODS ANDIN VITRODRUG RELEASE

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