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Titolo:
TUMOR-LOCALIZATION AND THERAPEUTIC EFFICA CY OF NOVEL METHOTREXATE SERUM-ALBUMIN (MTX-HSA) CONJUGATE IN-VIVO
Autore:
STEINMANN A; FRIEDRICH E; RATH U;
Indirizzi:
DEUTSCH KREBSFORSCHUNGSZENTRUM,FORSCH SCHWERPUNKT RADIOL DIAGNOST & THERAPIE D-69120 HEIDELBERG GERMANY UNIV KOBLENZ LANDAU,LEHRSTUHL ZELLBIOL KOBLENZ GERMANY UNIV HEIDELBERG,MED KLINIKUM,INNERE MED ABT 4 HEIDELBERG GERMANY
Titolo Testata:
Tumordiagnostik & Therapie
fascicolo: 4, volume: 15, anno: 1994,
pagine: 155 - 158
SICI:
0722-219X(1994)15:4<155:TATECO>2.0.ZU;2-6
Fonte:
ISI
Lingua:
GER
Soggetto:
ENHANCED TUMOR UPTAKE; CARRIER; PROTEIN; INVIVO; DESIGN;
Keywords:
DRUG CARRIER; EXPERIMENTAL TUMOR THERAPY; METHOTHREXATE; ALBUMIN;
Tipo documento:
Article
Natura:
Periodico
Settore Disciplinare:
Science Citation Index Expanded
Citazioni:
18
Recensione:
Indirizzi per estratti:
Citazione:
A. Steinmann et al., "TUMOR-LOCALIZATION AND THERAPEUTIC EFFICA CY OF NOVEL METHOTREXATE SERUM-ALBUMIN (MTX-HSA) CONJUGATE IN-VIVO", Tumordiagnostik & Therapie, 15(4), 1994, pp. 155-158

Abstract

The massive uptake and catabolism of serum albumin in tumors is well described. The pharmacokinetics of native albumin with a prolonged plasma half-life and enhanced tumor uptake suggest a possible use as a carrier for tumor therapy. In previous approaches to employ this distribution pattern for diagnosis and therapy of neoplastic diseases, albumin molecules were loaded with maximum quantities of cytostatic agents. To preserve the properties of native albumin and to avoid enhanced phagocytotic clearance, we used methotrexate-human serum albumin (MTX-HSA) conjugates with the molar loading ratio of 1:1. Using BDIX rats bearing the O-342 ovarian carcinoma, indirectly radioiodinated MTX-HSA showed enhanced scintigraphic tumor accumulation, indicating a distinct tumor localization 48 hours following injection. An average share of 9,9 % of the injected activity was found in the scintigraphic tumor region, thus confirming the prominent tumor uptake. In a therapeutic studywe compared the tumor volume post treatment and the area-under-the-curve of tumor volumes over treatment of animals receiving MTX-HSA treatment (0.4 mg MTX/kg) with those receiving saline as placebo. This low dosed MTX-HSA therapy caused significant (p = 0.025) effects on tumor growth. It is concluded that MTX-albumin conjugates created with optimized labeling techniques and loading ratios cause significant therapeutic effects even with very low MTX doses. Based on their enhanced tumor uptake these compounds may contribute to improve the efficacy of MTX-therapy.

ASDD Area Sistemi Dipartimentali e Documentali, Università di Bologna, Catalogo delle riviste ed altri periodici
Documento generato il 25/01/21 alle ore 16:19:09