Transferrin conjugates of doxorubicin: Synthesis, characterization, cellular uptake, and in vitro efficacy

Journal of Pharmaceutical Sciences

Volumn 87, Issue 3, 1998, Pages 338-346

  Kratz, Felix ^a   Beyer, Ulrich ^a   Roth, Thomas ^a   Tarasova, Nadya ^b   Collery, Philippe ^c   Lechenault, Francoise ^c   Cazabat, Annie ^c   Schumacher, Peter ^a   Unger, Clemens ^a   Falken, Ulrich ^a  

^a TUMOR BIOLOGY CENTER   (Germany)

^b NATIONAL CANCER INSTITUTE   (United States)

^c Inst Intl Rech Ions Metalliques   (France)

Author keywords

[No Author keywords available]

Indexed keywords

DOXORUBICIN; TRANSFERRIN;

ANTINEOPLASTIC ACTIVITY; ARTICLE; CANCER CELL CULTURE; CONFOCAL LASER MICROSCOPY; CYTOTOXICITY TEST; DRUG ACCUMULATION; DRUG CONJUGATION; DRUG DETERMINATION; DRUG DISTRIBUTION; DRUG EFFICACY; DRUG STABILITY; FLUORESCENCE MICROSCOPY; HUMAN; HUMAN CELL;

EID: 0012745920     PISSN: 00223549     EISSN: None     Source Type: Journal    
DOI: 10.1021/js970246a     Document Type: Article

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44. A smaller number of thiol groups can be introduced by reducing the amount of added iminothiolane, e.g. for introducing two HS groups, 85 μL of the iminothiolane solution is added.
45. It should be noted that commercially available transferrin also shows this peak with a peak area of approximately 3%. Isolation of this byproduct in the conjugates using a Superdex 200 (Pharmacia) confirmed that the peak observed on the BioSil-SEC 250 column can be assigned to a dimeric product.
46. 17).
47. Free doxorubicin is observed by the appearance of a peak at around 2.5 min on the Poros HQ 20 column, but the signal is quite broad and there is a lack of precision when integrating this peak. This is the reason why we preferred to use the decrease in the peak area of the conjugate as a measure of release of doxorubicin.
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