SPR Biosensor Studies of the Direct Interaction between 27 Drugs and a Liposome Surface:  Correlation with Fraction Absorbed in Humans

Danelian, Ernest; Karlén, Anders; Karlsson, Robert; Winiwarter, Susanne; Hansson, Annelie; Löfås, Stefan; Lennernäs, Hans; Hämäläinen, M.

doi:10.1021/jm991156g

Cited by 125 publications

(59 citation statements)

References 12 publications

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“…It has been demonstrated that SPR is a useful tool for the direct analysis of the binding of drugs to phospholipid vesicles immobilised on a commercially available L1 sensor chip. [6][7][8] Using SPR, we have extended previous studies of the effects of membrane fluidity [6] and demonstrated the ability of CADs to accumulate in various phospholipid bilayers.…”

Section: Introductionmentioning

confidence: 52%

Characterisation of the Binding of Cationic Amphiphilic Drugs to Phospholipid Bilayers Using Surface Plasmon Resonance

et al. 2007

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The interactions of three cationic amphiphilic drugs (CPZ, AMI, PROP) with phospholipid vesicles comprising DOPC, DMPC, or DSPC were investigated using surface plasmon resonance (SPR). Responses for CAD concentrations in the range 15.625 to 1500 microM were measured. The greatest uptake by each phospholipid bilayer occurred with CPZ. Inclusion of CAD concentrations between 750 and 1500 microM provided evidence for a second nonsaturable binding process, which may arise from intercalation of the drugs within the lipid bilayer. CAD binding was additionally shown to be dependent on membrane fluidity. Responses were initially fitted over a concentration range of 15.625 to 500 microM using a model which incorporated terms for a saturable binding site. This yielded very poor values of K(D) and nonsensible values of saturation responses. Subsequently, responses were fit to the expression for a model which incorporated terms for both a saturable binding site and second nonsaturable site. Measurable binding affinities (K(D) values ranged from 170 to 814 microM) were obtained for DOPC and DMPC bilayers which are similar to values reported previously. This work demonstrates that SPR studies with synthetic phospholipid bilayers provide a potentially useful approach for characterising drug-membrane binding interactions and for providing insight into the processes that contribute to drug-membrane binding.

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Section: Introductionmentioning

confidence: 52%

Characterisation of the Binding of Cationic Amphiphilic Drugs to Phospholipid Bilayers Using Surface Plasmon Resonance

et al. 2007

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“…Various label-free biosensors that do not use the traditional fluorescence and radioactivity labeling methods have been developed to provide quick and simple methods for biomolecular detection by converting the molecular-recognition events into easily detectable optical, [1,2] calorimetric, [3] or acoustic [4] signals. Porous silicon (PSi) has been demonstrated to be a sensitive sensing platform because of its large internal surface area.…”

Section: Introductionmentioning

confidence: 99%

Macroporous Silicon Microcavities for Macromolecule Detection

Ouyang

Christophersen

Viard

et al. 2005

Adv Funct Materials

226

201

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Macroporous silicon microcavities for detection of large biological molecules have been fabricated from highly doped n‐type silicon. Well‐defined controllable pore sizes up to 120 nm have been obtained by systematically optimizing the etching parameters. The dependence of the sensor sensitivity on pore size is discussed. Excellent infiltration inside these macroporous silicon microcavities is demonstrated using 60 nm diameter latex spheres and rabbit IgG (150 kDa; 1Da = 1 g mol–1). The sensing performance of the device is tested using a biotin/streptavidin couple, and protein concentration down to 1–2 μM (equivalent to 0.3 ng mm–2) could be detected. Simulations show that the sensitivity of the technique is currently approximately 1–2 % of a protein monolayer.

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“…These assays are based on small molecule binding to liposome surfaces for prediction of absorption properties (Baird et al, 2002;Danelian et al, 2000) and on compound binding to immobilized plasma proteins (Day and Myszka, 2003;Rich et al, 2001;Frostell-Karlsson et al, 2000) for estimation of the level of free drug in the blood stream. These assays can be used either in screening mode where one concentration of each compound is analyzed or for more detailed characterization where concentration series of compounds are used.…”

Section: Spr-emerging Applications 155mentioning

confidence: 99%

SPR for molecular interaction analysis: a review of emerging application areas

Karlsson¹

2004

J of Molecular Recognition

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405

248

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PubMed searches identified four emerging application areas for surface plasmon resonance systems. Food analysis, proteomics, immunogenicity and drug discovery. These application areas are reviewed. In connection with the review of drug discovery applications a case study is presented. This study demonstrates the value of combining results from drug-target and ADME predictive assays for compound selection.

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SPR Biosensor Studies of the Direct Interaction between 27 Drugs and a Liposome Surface: Correlation with Fraction Absorbed in Humans

Cited by 125 publications

References 12 publications

Characterisation of the Binding of Cationic Amphiphilic Drugs to Phospholipid Bilayers Using Surface Plasmon Resonance

Characterisation of the Binding of Cationic Amphiphilic Drugs to Phospholipid Bilayers Using Surface Plasmon Resonance

Macroporous Silicon Microcavities for Macromolecule Detection

SPR for molecular interaction analysis: a review of emerging application areas

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