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Clin Cancer Res ; 12(10): 3193-9, 2006 May 15.
Article in English | MEDLINE | ID: mdl-16707620

ABSTRACT

PURPOSE: Quercetin is a potent chemotherapeutic drug. Clinical trials exploring different schedules of administration of quercetin have been hampered by its extreme water insolubility. To overcome this limitation, this study is aimed to develop liposomal quercetin and investigate its distribution in vivo and antitumor efficacy in vivo and in vitro. EXPERIMENTAL DESIGN: Quercetin was encapsulated in polyethylene glycol 4000 liposomes. Biodistribution of liposomal quercetin i.v. at 50 mg/kg in tumor-bearing mice was detected by high-performance liquid chromatography. Induction of apoptosis by liposomal quercetin in vitro was tested. The antitumor activity of liposomal quercetin was evaluated in the immunocompetent C57BL/6N mice bearing LL/2 Lewis lung cancer and in BALB/c mice bearing CT26 colon adenocarcinoma and H22 hepatoma. Tumor volume and survival time were observed. The mechanisms underlying the antitumor effect of quercetin in vivo was investigated by detecting the microvessel density, apoptosis, and heat shock protein 70 expression in tumor tissues. RESULTS: Liposomal quercetin could be dissolved in i.v. injection and effectively accumulate in tumor tissues. The half-time of liposomal quercetin was 2 hours in plasma. The liposomal quercetin induced apoptosis in vitro and significantly inhibited tumor growth in vivo in a dose-dependent manner. The optimal dose of liposomal quercetin resulted in a 40-day survival rate of 40%. Quantitative real-time PCR showed that liposomal quercetin down-regulated the expression of heat shock protein 70 in tumor tissues. Immunohistochemistry analysis showed that liposomal quercetin inhibited tumor angiogenesis as assessed by CD31 and induced tumor cell apoptosis. CONCLUSIONS: Our data indicated that pegylated liposomal quercetin can significantly improve the solubility and bioavailability of quercetin and can be a potential application in the treatment of tumor.


Subject(s)
Adenocarcinoma/drug therapy , Carcinoma, Hepatocellular/drug therapy , Carcinoma, Lewis Lung/drug therapy , Colonic Neoplasms/drug therapy , Liver Neoplasms/drug therapy , Quercetin/administration & dosage , Quercetin/pharmacology , Animals , Apoptosis/drug effects , Biological Availability , Chromatography, High Pressure Liquid , Disease Models, Animal , Down-Regulation , Drug Carriers , HSP70 Heat-Shock Proteins/biosynthesis , Injections, Intravenous , Liposomes , Mice , Mice, Inbred BALB C , Mice, Inbred C57BL , Polyethylene Glycols , Quercetin/pharmacokinetics , Solubility , Tissue Distribution , Tumor Cells, Cultured
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