Pharmacokinetics of methotrexate–albumin conjugates in tumor-bearing rats

@article{Stehle1997PharmacokineticsOM,
  title={Pharmacokinetics of methotrexate–albumin conjugates in tumor-bearing rats},
  author={Gerd Stehle and Andreas Wunder and Hannsjörg Sinn and Hans Hermann Schrenk and Sandra Schiitt and Eva Frei and Gernot Hartung and W Maier-borst and Dieter L. Heene},
  journal={Anti-Cancer Drugs},
  year={1997},
  volume={8},
  pages={835-844}
}
Linking chemotherapeutic drugs to a macromolecular carrier system may enhance tumor targeting, reduce toxicity and overcome drug resistance mechanisms. As an elementary model to evaluate the pharmacological properties of macromolecular drug carrier systems we chose rat serum albumin (RSA) for carrier and methotrexate (MTX) as antineoplastic drug. The conjugation procedure yielded conjugates with an approximate 1:1 molar loading rate (MTX(1)-RSA). In the first part of the study a residualizing… Expand
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We reported recently that albumin is a suitable drug carrier for targeted delivery of methotrexate (MTX) to tumors. Due to pathophysiological conditions in neoplastic tissue, high amounts of albumin… Expand
Albumin as a drug carrier: design of prodrugs, drug conjugates and nanoparticles.
  • F. Kratz
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  • Journal of controlled release : official journal of the Controlled Release Society
  • 2008
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This review summarizes the Phase I – III studies that have been performed with drug conjugates that have recently entered clinical trials and includes a methotrexate–albumin conjugate and an albumin-binding doxorubicin prodrug. Expand
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Cell-penetrating peptide conjugation of MTX is a new way of increasing delivery, and thereby, the potency of already well-characterized therapeutic molecules into drug resistant tumour cells. Expand
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This review covers the diagnostic evidence for tumor accumulation of serum proteins and the design, development, and biological evaluation of drug conjugates with transferrin, albumin, and low-density lipoprotein. Expand
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Interestingly, it was noticed that the conjugates based on dextran and albumin were more cytotoxic than the free drug in the highest concentrations tested (1000 and 10000 ng/ml). Expand
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