Preparation of Cystamine Core Dendrimer and Antibody–Dendrimer Conjugates for MRI Angiography

摘要: Herein we report the preparation along with in vivo and vitro MRI characterization of two generation four five cystamine core dendrimers loaded thirty fifty-eight derivatized Gd-DOTA (G4SS30, G5SS58) respectively. Likewise development half-dendrimers conjugated to F(ab')(2) fragment monoclonal antibody (mAb) panitumumab functionalized a maleimide conjugation functional group site (Ab-(G4S15)(4), Ab-(G5S29)(4)) are also described. The molar relaxivity Ab-(G4S15)(4) conjugate, measured at pH 7.4, 22 °C, 3T showed moderate increase as compared Magnevist (6.7 vs 4.0 mM(-1) s(-1)) while Ab-(G5S29)(4) conjugate was 2-fold higher (9.1 s(-1)). data that only high injection dose (0.050 mmol Gd(3+)/kg) produced detectable contrast enhanced for lower (0.035 sufficient conjugate. antibody-SMCC purified by Sephadex G-100 column, antibody-dendrimer-based agents were spin filtration using Centricon filter (50,000 MCO). protein assay coupled cysteine Ellman's indicated an dendrimer ratio 1:4. blood clearance half-lives jugular vein ~12-22 min.