In vitro release study, in vivo evaluation of biodistribution and antitumor activity of HPMA copolymer-5-fluorouracil conjugates / 药学学报
Acta Pharmaceutica Sinica
;
(12): 1152-1156, 2008.
Article
Dans Chinois
| WPRIM
| ID: wpr-232626
ABSTRACT
The in vitro release behavior, in vivo biodistribution and antitumor activity of N-(2-hydroxypropyl) methacrylamide (HPMA) copolymer-5-fluorouracil conjugates (P-FU) were studied. The in vitro release behavior was evaluated by determining the amount of 5-fluorouracil (5-FU) released from P-FU in mice plasma at 37 degrees C. The in vivo biodistribution and therapeutic evaluation were investigated with Kunming mice bearing hepatoma 22 (H22). The in vitro half-life (t1/2) of P-FU in mice plasma was 32.4 h. It appeared that the circulation life time of the conjugates were 166 times longer than that of 5-FU. The AUC and t1/2 of P-FU in tumor were 3.3 times and 2.3 times more than those of 5-FU, respectively. Therapeutic evaluation also demonstrated that the treatment with P-FU displayed stronger inhibition of the tumor growth when compared with that of 5-FU (P < 0.05). HPMA copolymer is a potential carrier for 5-FU for effective treatment of cancer.
Texte intégral:
Disponible
Indice:
WPRIM (Pacifique occidental)
Sujet Principal:
Anatomopathologie
/
Pharmacologie
/
Acrylamides
/
Vecteurs de médicaments
/
Pharmacocinétique
/
Distribution tissulaire
/
Répartition aléatoire
/
Aire sous la courbe
/
Lignée cellulaire tumorale
/
Charge tumorale
Type d'étude:
Étude pronostique
Limites du sujet:
Animaux
langue:
Chinois
Texte intégral:
Acta Pharmaceutica Sinica
Année:
2008
Type:
Article
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