Tumor targeting using liposomal antineoplastic drugs

Figures & data

Table 1 Pharmacokinetic properties in human of commercial preparations of doxorubicin (DOX). Free doxorubicin is compared to doxorubicin encapsulated in conventional liposomes (Myocet) and doxorubicin encapsulated in pegylated liposomes (Doxil, Caelyx). Liposome diameter: 85 to 150 nm. Data nor-malisation using an average body surface area of 1.7 m² and an average body weight of 70 kg. Examples of representative studies (Hamilton et al 2002; Gabizon et al 2003; Mross et al 2004).

	Free DOX	Myocet (non-pegylated liposomal DOX)	Doxil/Caelyx (pegylated liposomal DOX)
Dose (mg/kg)	1.2	1.8	1.5
AUC (mg.h/L)	3.5	19.4	4082
Clearance (ml/h)	25’300	9’520	23
Vss (L)	365	139	3.0
Half-life (h)	0.06/10.4a	<1/52.6a	84

a Two elimination phases.

HamiltonABiganzoliLColemanREORTC 10968: a phase I clinical and pharmacokinetic study of polyethylene glycol liposomal doxorubicin (Caelyx, Doxil) at a 6-week interval in patients with metastatic breast cancer. European Organization for Research and Treatment of CancerAnn Oncol200213910812123337

 PubMed Web of Science ®Google Scholar

GabizonAShmeedaHBarenholzYPharmacokinetics of pegylated liposomal Doxorubicin: review of animal and human studiesClin Pharmacokinet2003424193612739982

 PubMed Web of Science ®Google Scholar

MrossKNiemannBMassingUPharmacokinetics of liposomal doxorubicin (TLC-D99; Myocet) in patients with solid tumors: an open-label, single-dose studyCancer Chemother Pharmacol200454514512415322827

 PubMed Web of Science ®Google Scholar