Albumin as a drug carrier: Design of prodrugs, drug conjugates and nanoparticles

Kratz, Felix

doi:10.1016/j.jconrel.2008.05.010

Cited by 1,929 publications

(1,420 citation statements)

References 83 publications

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“…Moreover, HSA and HSA-bound drugs are known to accumulate in solid tumors as a consequence of the enhanced permeability and retention effect, which can be an operative way of selective tumor targeting [59]. HSA has nonspecific binding pockets and the principal regions of these sites are located in subdomains IIA and IIIA called as site I and II, respectively [60,61].…”

Section: Interaction Of Rhcp* Complexes Of En Bpy and Dhp With Humanmentioning

confidence: 99%

Comparative solution equilibrium studies on pentamethylcyclopentadienyl rhodium complexes of 2,2ʹ-bipyridine and ethylenediamine and their interaction with human serum albumin

Enyedy

Mészáros

Dömötör

et al. 2015

Journal of Inorganic Biochemistry

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Complex formation equilibrium processes of the (N,N) donor containing 2,2'-bipyridine (bpy) and ethylenediamine (en) with (η 5 -pentamethylcyclopentadienyl)rhodium(III) were investigated in aqueous solution via pH-potentiometry, 1 H NMR spectroscopy, and UV-Vis spectrophotometry in the absence and presence of chloride ions. 2+ , and formation of ternary HSA-RhCp*-ligand adducts was proved. In the case of the deferiprone complex, the RhCp* fragment is cleaved off when HSA is loaded with low equivalents of the compound.

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Section: Interaction Of Rhcp* Complexes Of En Bpy and Dhp With Humanmentioning

confidence: 99%

Comparative solution equilibrium studies on pentamethylcyclopentadienyl rhodium complexes of 2,2ʹ-bipyridine and ethylenediamine and their interaction with human serum albumin

Enyedy

Mészáros

Dömötör

et al. 2015

Journal of Inorganic Biochemistry

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“…An unsaturated SCFA, crotonic acid (crotonyl-coenzyme A is an intermediate in the fermentation of butyric acid) and a long chain fatty acid, myristic acid, were also used as acylating agents. Myristic acid can bind to human serum albumin resulting in significant accumulation of the bioconjugate in the surrounding of the tumor [20].…”

Section: Short-chain Fatty Acid Acylated Daunorubicin-gnrh-iii Derivamentioning

confidence: 99%

Enhanced cellular uptake and in vitro antitumor activity of short-chain fatty acid acylated daunorubicin–GnRH-III bioconjugates

Hegedüs

Manea

Orbán

et al. 2012

European Journal of Medicinal Chemistry

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Here we report on the synthesis and biochemical characterization (enzymatic stability, cellular uptake, in vitro antitumor activity, membrane interaction and GnRH-receptor binding affinity) of novel short-chain fatty acid (SCFA) acylated daunorubicin-GnRH-III bioconjugates, which may serve as drug delivery systems for targeted cancer chemotherapy. Ser in position 4 of GnRH-III was replaced by Lys, followed by the acylation of its ε-amino group with various fatty acids. SCFAs are potentially chemoprotective agents by suppressing the growth of cancer cells and therefore may enhance the antitumor activity of the bioconjugates. We found that all synthesized bioconjugates had high cytostatic effect in vitro, were stable in cell culture medium for 6 h and degraded in the presence of rat liver lysosomal homogenate leading to the formation of an oxime bond-linked daunorubicin-Lys as the smallest active metabolite. In the presence of α-chymotrypsin, all compounds were digested, the degradation rate strongly depending on the type of fatty acid. The bioconjugate containing Lys(nBu) in position 4 was taken up most efficiently by the cancer cells and exerted higher in vitro cytostatic effect than the previously developed GnRH-III( 4 Lys(Ac), 8 Lys(Dau=Aoa)) or the parent GnRH-III(Dau=Aoa) bioconjugate. Our results could be explained by the increased binding affinity of the newly developed compound containing Lys(nBu) to the GnRH receptors.

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“…Haemoglobin (Hb) and HSA are preferred for monitoring molecules because they are accessible in large amounts, are chemically stable and are not prone to repair mechanisms such as DNA-adducts. Because of the long life span of Hb (approximately 120 days) and the long half-life of HSA (approximately 19 days (Kratz, 2008)), these adducts accumulate in the human body, making their concentrations very sensitive parameters for human biomonitoring (Angerer et al , 2007). Similar results were found among smoker subjects who inhaled formaldehyde through smoke.…”

Section: Introductionmentioning

confidence: 64%

“…Conversely, HSA exhibits a shorter average life-time (Kratz, 2008) and represents the main target of AA, on which an immune reaction takes place; in our view such type of reaction is better defined through a biological and dynamic assay, especially when low levels of ethanol could be expected as in the general healthy population.…”

Section: Discussionmentioning

confidence: 95%

Immune response to acetaldehyde-human serum albumin adduct among healthy subjects related to alcohol intake

Romanazzi

Schilirò

Carraro

et al. 2013

Environmental Toxicology and Pharmacology

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Albumin as a drug carrier: Design of prodrugs, drug conjugates and nanoparticles

Cited by 1,929 publications

References 83 publications

Comparative solution equilibrium studies on pentamethylcyclopentadienyl rhodium complexes of 2,2ʹ-bipyridine and ethylenediamine and their interaction with human serum albumin

Comparative solution equilibrium studies on pentamethylcyclopentadienyl rhodium complexes of 2,2ʹ-bipyridine and ethylenediamine and their interaction with human serum albumin

Enhanced cellular uptake and in vitro antitumor activity of short-chain fatty acid acylated daunorubicin–GnRH-III bioconjugates

Immune response to acetaldehyde-human serum albumin adduct among healthy subjects related to alcohol intake

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