In Vivo Drug Delivery Performance of Lipiodol-Based Emulsion or Drug-Eluting Beads in Patients with Hepatocellular Carcinoma.

作者: Elsa Lilienberg , Ilse R. Dubbelboer , Amar Karalli , Rimma Axelsson , Torkel B. Brismar

DOI: 10.1021/ACS.MOLPHARMACEUT.6B00886

关键词: LipiodolHepatocellular carcinomaLiver cancerCmaxDrug deliveryUrologyDoxorubicinPharmacologyMedicineIn vivoPharmacokinetics

摘要: Doxorubicin (DOX) delivered in a lipiodol-based emulsion (LIPDOX) or drug-eluting beads (DEBDOX) is used as palliative treatment patients with intermediate-stage hepatocellular carcinoma (HCC). The primary objective of this study was to evaluate the vivo delivery performance DOX from LIPDOX DEBDOX HCC using local and systemic pharmacokinetics its main metabolite doxorubicinol (DOXol). Urinary excretion DOXol their short-term safety antitumor effects were also evaluated. In open, prospective, nonrandomized multicenter study, (n = 13) 12) injected into feeding arteries tumor. Local (vena cava/hepatic vein orifice) (peripheral vein) plasma concentrations determined samples obtained up 6 h 7 days after treatment. Tumor response assessed computed tomography magnetic resonance imaging. Cmax AUC0–24 h for 5.6-fold 2.4-fold higher in...

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