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[Nanoliposomal quercetin inhibits formation of malignant ascites of hepatocellular carcinoma].
Ai Zheng. 2006 Aug; 25(8):941-5.AZ

Abstract

BACKGROUND & OBJECTIVE

Quercetin is a potential chemotherapeutic drug with many biological activities. However, the insolubility of quercetin seriously limits its clinical use. This study was to investigate the biodistribution of quercetin encapsulated by pegylated nanoliposomes and its therapeutic efficacy on the formation of carcinomatous ascites of hepatocellular carcinoma in mice.

METHODS

Nanoliposomal quercetin was prepared with conventional rotary evaporation method. BALB/c mice inoculated with hepatocellular carcinoma cells (H22) at the anterior right subaxilla for twelve days were given intravascular injection with nanoliposomal quercetin at 1.5 mg/body (based on quercetin) at different time points. Then the levels of quercetin in the plasma, tumor tissues and normal organs were tested by high pressure liquid chromatography (HPLC). Various dosages of nanoliposomal quercetin were peritoneally given to tumor-bearing mice to determine the optimal dose. The tumor-bearing mice were treated intraperitoneally with 100 mg/kg nanoliposomal quercetin once a day for 14 days. The formation of malignant ascites, increase of body weight, survival time and peritoneal capillary permeability were assessed. Apoptotic cells in ascites were detected by flow cytometry.

RESULTS

Nanoliposomal quercetin was a spherical particle with 25% drug content (W/W) and 130+/-20 nm in diameter. Nanoliposomal quercetin effectively aggregated in tumor tissues and its half-life period was 4 h. Nanoliposome quercetin inhibited the formation of malignant ascites of hepatocellular carcinoma model in a dose-dependent manner. Moreover, 100 mg/kg nanoliposomal quercetin significantly enhanced the apoptosis of cancer cells in ascites, inhibited the increase of body weight, reduced peritoneal capillary permeability and prolonged the survival time of tumor-bearing mice compared with PBS control.

CONCLUSION

Nanoliposomal quercetin can effectively accumulate in tumor tissues and inhibit the formation of malignant ascites, thus it might be used as a potential antitumor drug which deserves future study.

Authors+Show Affiliations

State Key Laboratory of Biotherapy West China Hospital, West China Medical School, Sichuan University, Chengdu, Sichuan, 610041, P. R. China.No affiliation info availableNo affiliation info availableNo affiliation info availableNo affiliation info availableNo affiliation info available

Pub Type(s)

Journal Article
Research Support, Non-U.S. Gov't

Language

chi

PubMed ID

16965672

Citation

Yuan, Zhi-Ping, et al. "[Nanoliposomal Quercetin Inhibits Formation of Malignant Ascites of Hepatocellular Carcinoma]." Ai Zheng = Aizheng = Chinese Journal of Cancer, vol. 25, no. 8, 2006, pp. 941-5.
Yuan ZP, Chen LJ, Wei YQ, et al. [Nanoliposomal quercetin inhibits formation of malignant ascites of hepatocellular carcinoma]. Ai Zheng. 2006;25(8):941-5.
Yuan, Z. P., Chen, L. J., Wei, Y. Q., Fan, L. Y., Tang, M. H., & Yang, G. L. (2006). [Nanoliposomal quercetin inhibits formation of malignant ascites of hepatocellular carcinoma]. Ai Zheng = Aizheng = Chinese Journal of Cancer, 25(8), 941-5.
Yuan ZP, et al. [Nanoliposomal Quercetin Inhibits Formation of Malignant Ascites of Hepatocellular Carcinoma]. Ai Zheng. 2006;25(8):941-5. PubMed PMID: 16965672.
* Article titles in AMA citation format should be in sentence-case
TY - JOUR T1 - [Nanoliposomal quercetin inhibits formation of malignant ascites of hepatocellular carcinoma]. AU - Yuan,Zhi-Ping, AU - Chen,Li-Juan, AU - Wei,Yu-Quan, AU - Fan,Lin-Yu, AU - Tang,Ming-Hai, AU - Yang,Guang-Li, PY - 2006/9/13/pubmed PY - 2009/5/29/medline PY - 2006/9/13/entrez SP - 941 EP - 5 JF - Ai zheng = Aizheng = Chinese journal of cancer JO - Ai Zheng VL - 25 IS - 8 N2 - BACKGROUND & OBJECTIVE: Quercetin is a potential chemotherapeutic drug with many biological activities. However, the insolubility of quercetin seriously limits its clinical use. This study was to investigate the biodistribution of quercetin encapsulated by pegylated nanoliposomes and its therapeutic efficacy on the formation of carcinomatous ascites of hepatocellular carcinoma in mice. METHODS: Nanoliposomal quercetin was prepared with conventional rotary evaporation method. BALB/c mice inoculated with hepatocellular carcinoma cells (H22) at the anterior right subaxilla for twelve days were given intravascular injection with nanoliposomal quercetin at 1.5 mg/body (based on quercetin) at different time points. Then the levels of quercetin in the plasma, tumor tissues and normal organs were tested by high pressure liquid chromatography (HPLC). Various dosages of nanoliposomal quercetin were peritoneally given to tumor-bearing mice to determine the optimal dose. The tumor-bearing mice were treated intraperitoneally with 100 mg/kg nanoliposomal quercetin once a day for 14 days. The formation of malignant ascites, increase of body weight, survival time and peritoneal capillary permeability were assessed. Apoptotic cells in ascites were detected by flow cytometry. RESULTS: Nanoliposomal quercetin was a spherical particle with 25% drug content (W/W) and 130+/-20 nm in diameter. Nanoliposomal quercetin effectively aggregated in tumor tissues and its half-life period was 4 h. Nanoliposome quercetin inhibited the formation of malignant ascites of hepatocellular carcinoma model in a dose-dependent manner. Moreover, 100 mg/kg nanoliposomal quercetin significantly enhanced the apoptosis of cancer cells in ascites, inhibited the increase of body weight, reduced peritoneal capillary permeability and prolonged the survival time of tumor-bearing mice compared with PBS control. CONCLUSION: Nanoliposomal quercetin can effectively accumulate in tumor tissues and inhibit the formation of malignant ascites, thus it might be used as a potential antitumor drug which deserves future study. UR - https://www.unboundmedicine.com/medline/citation/16965672/[Nanoliposomal_quercetin_inhibits_formation_of_malignant_ascites_of_hepatocellular_carcinoma]_ L2 - http://www.cancercommun.com/fulltextnew.asp?y=2006&m=8&ym=941 DB - PRIME DP - Unbound Medicine ER -