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Hydrodynamic Radii of Ranibizumab, Aflibercept and Bevacizumab Measured by Time-Resolved Phosphorescence Anisotropy.


ABSTRACT:

Purpose

To measure the hydrodynamic radii of intravitreal anti-VEGF drugs ranibizumab, aflibercept and bevacizumab with ?s time-resolved phosphorescence anisotropy.

Methods

Ruthenium-based dye Ru(bpy)2(mcbpy?-?O?-?Su?-?ester)(PF6)2, whose lifetime of several hundred nanoseconds is comparable to the rotational correlation time of these drugs in buffer, was used as a label. The hydrodynamic radii were calculated from the rotational correlation times of the Ru(bpy)2(mcbpy?-?O?-?Su?-?ester)(PF6)2-labelled drugs obtained with time-resolved phosphorescence anisotropy measurements in buffer/glycerol solutions of varying viscosity.

Results

The measured radii of 2.76±0.04 nm for ranibizumab, 3.70±0.03 nm for aflibercept and 4.58±0.01 nm for bevacizumab agree with calculations based on molecular weight and other experimental measurements.

Conclusions

Time-resolved phosphorescence anisotropy is a relatively simple and straightforward method that allows experimental measurement of the hydrodynamic radius of individual proteins, and is superior to theoretical calculations which cannot give the required accuracy for a particular protein.

SUBMITTER: Hirvonen LM 

PROVIDER: S-EPMC4942501 | biostudies-literature | 2016 Aug

REPOSITORIES: biostudies-literature

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Publications

Hydrodynamic Radii of Ranibizumab, Aflibercept and Bevacizumab Measured by Time-Resolved Phosphorescence Anisotropy.

Hirvonen Liisa M LM   Fruhwirth Gilbert O GO   Srikantha Nishanthan N   Barber Matthew J MJ   Neffendorf James E JE   Suhling Klaus K   Jackson Timothy L TL  

Pharmaceutical research 20160525 8


<h4>Purpose</h4>To measure the hydrodynamic radii of intravitreal anti-VEGF drugs ranibizumab, aflibercept and bevacizumab with μs time-resolved phosphorescence anisotropy.<h4>Methods</h4>Ruthenium-based dye Ru(bpy)2(mcbpy - O - Su - ester)(PF6)2, whose lifetime of several hundred nanoseconds is comparable to the rotational correlation time of these drugs in buffer, was used as a label. The hydrodynamic radii were calculated from the rotational correlation times of the Ru(bpy)2(mcbpy - O - Su -   ...[more]

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