Back to Journals » International Journal of Nanomedicine » Volume 6

Biodistribution and pharmacokinetics of 188Re-liposomes and their comparative therapeutic efficacy with 5-fluorouracil in C26 colonic peritoneal carcinomatosis mice

Authors Tsai CC, Chang CH, Chen LC, Chang YJ, Lan KL, Wu YH, Hsu CW, Liu IH, Ho CL, Lee WC, Ni HC, Chang TJ, Ting G, Lee TW

Published 26 October 2011 Volume 2011:6 Pages 2607—2619

DOI https://doi.org/10.2147/IJN.S23834

Review by Single-blind

Peer reviewer comments 3

Chia-Che Tsai1, Chih-Hsien Chang1, Liang-Cheng Chen1, Ya-Jen Chang1, Keng-Li Lan2, Yu-Hsien Wu1, Chin-Wei Hsu1, I-Hsiang Liu1, Chung-Li Ho1, Wan-Chi Lee1, Hsiao-Chiang Ni1, Tsui-Jung Chang1, Gann Ting3, Te-Wei Lee1
1Institute of Nuclear Energy Research, Taoyuan, 2Cancer Center, Taipei Veterans General Hospital, Taipei, 3National Health Research Institutes, Taipei, Taiwan, ROC

Background: Nanoliposomes are designed as carriers capable of packaging drugs through passive targeting tumor sites by enhanced permeability and retention (EPR) effects. In the present study the biodistribution, pharmacokinetics, micro single-photon emission computed tomography (micro-SPECT/CT) image, dosimetry, and therapeutic efficacy of 188Re-labeled nanoliposomes (188Re-liposomes) in a C26 colonic peritoneal carcinomatosis mouse model were evaluated.
Methods: Colon carcinoma peritoneal metastatic BALB/c mice were intravenously administered 188Re-liposomes. Biodistribution and micro-SPECT/CT imaging were performed to determine the drug profile and targeting efficiency of 188Re-liposomes. Pharmacokinetics study was described by a noncompartmental model. The OLINDA|EXM® computer program was used for the dosimetry evaluation. For therapeutic efficacy, the survival, tumor, and ascites inhibition of mice after treatment with 188Re-liposomes and 5-fluorouracil (5-FU), respectively, were evaluated and compared.
Results: In biodistribution, the highest uptake of 188Re-liposomes in tumor tissues (7.91% ± 2.02% of the injected dose per gram of tissue [%ID/g]) and a high tumor to muscle ratio (25.8 ± 6.1) were observed at 24 hours after intravenous administration. The pharmacokinetics of 188Re-liposomes showed high circulation time and high bioavailability (mean residence time [MRT] = 19.2 hours, area under the curve [AUC] = 820.4%ID/g*h). Micro-SPECT/CT imaging of 188Re-liposomes showed a high uptake and targeting in ascites, liver, spleen, and tumor. The results were correlated with images from autoradiography and biodistribution data. Dosimetry study revealed that the 188Re-liposomes did not cause high absorbed doses in normal tissue but did in small tumors. Radiotherapeutics with 188Re-liposomes provided better survival time (increased by 34.6% of life span; P < 0.05), tumor and ascites inhibition (decreased by 63.4% and 83.3% at 7 days after treatment; P < 0.05) in mice compared with chemotherapeutics of 5-fluorouracil (5-FU).
Conclusion: The use of 188Re-liposomes for passively targeted tumor therapy had greater therapeutic effect than the currently clinically applied chemotherapeutics drug 5-FU in a colonic peritoneal carcinomatosis mouse model. This result suggests that 188Re-liposomes have potential benefit and are safe in treating peritoneal carcinomatasis of colon cancer.

Keywords: biodistribution, dosimetry, 5-fluorouracil, micro-SPECT/CT, 188Re-liposomes

Creative Commons License This work is published and licensed by Dove Medical Press Limited. The full terms of this license are available at https://www.dovepress.com/terms.php and incorporate the Creative Commons Attribution - Non Commercial (unported, v3.0) License. By accessing the work you hereby accept the Terms. Non-commercial uses of the work are permitted without any further permission from Dove Medical Press Limited, provided the work is properly attributed. For permission for commercial use of this work, please see paragraphs 4.2 and 5 of our Terms.

Download Article [PDF]  View Full Text [HTML][Machine readable]

 

Readers of this article also read:

Biodegradable magnesium nanoparticle-enhanced laser hyperthermia therapy

Wang Q, Xie L, He Z, Di D, Liu J

International Journal of Nanomedicine 2012, 7:4715-4725

Published Date: 28 August 2012

Simple room-temperature preparation of high-yield large-area graphene oxide

Huang NM, Lim HN, Chia CH, Yarmo MA, Muhamad MR

International Journal of Nanomedicine 2011, 6:3443-3448

Published Date: 19 December 2011

Subtle cytotoxicity and genotoxicity differences in superparamagnetic iron oxide nanoparticles coated with various functional groups

Hong SC, Lee JH, Lee J, Kim HY, Park JY, Cho J, Lee J, Han DW

International Journal of Nanomedicine 2011, 6:3219-3231

Published Date: 7 December 2011

The efficacy of mitochondrial targeting antiresistant epirubicin liposomes in treating resistant leukemia in animals

Men Y, Wang XX, Li RJ, Zhang Y, Tian W, Yao HJ, Ju RJ, Ying X, Zhou J, Li N, Zhang L, Yu Y, Lu WL

International Journal of Nanomedicine 2011, 6:3125-3137

Published Date: 2 December 2011

Embedded nanomicro syringe on chip for molecular therapy

Jalil MA, Suwanpayak N, Kulsirirat K, Suttirak S, Ali J, Yupapin PP

International Journal of Nanomedicine 2011, 6:2925-2932

Published Date: 18 November 2011

Translocation of PEGylated quantum dots across rat alveolar epithelial cell monolayers

Fazlollahi F, Sipos A, Kim YH, Hamm-Alvarez SF, Borok Z, Kim K-J, Crandall ED

International Journal of Nanomedicine 2011, 6:2849-2857

Published Date: 10 November 2011

Chemical nature and structure of organic coating of quantum dots is crucial for their application in imaging diagnostics

Bakalova R, Zhelev Z, Kokuryo D, Spasov L, Aoki I, Saga T

International Journal of Nanomedicine 2011, 6:1719-1732

Published Date: 18 August 2011

Preparation and evaluation of lidocaine hydrochloride in cyclodextrin inclusion complexes for development of stable gel in association with chlorhexidine gluconate for urogenital use

Soares da Silva LFJ, Carmo FA, Borges VRA, Monteiro LM, Rodrigues CR, Cabral LM, Sousa VP

International Journal of Nanomedicine 2011, 6:1143-1154

Published Date: 3 June 2011