Back to Journals » International Journal of Nanomedicine » Volume 7

Preclinical evaluation of injectable sirolimus formulated with polymeric nanoparticle for cancer therapy

Authors Woo, Chung, Ju EJ, Jung, Kang, Lee, Seo, Lee, Lee JS, Park HJ, Song SY, Jeong S, Choi EK

Received 24 December 2011

Accepted for publication 3 March 2012

Published 27 April 2012 Volume 2012:7 Pages 2197—2208


Review by Single-blind

Peer reviewer comments 3

Ha Na Woo1*, Hye Kyung Chung2*, Eun Jin Ju1, Joohee Jung1,3, Hye-Won Kang4, Sa-Won Lee4, Min-Hyo Seo4, Jin Seong Lee5, Jung Shin Lee1,6, Heon Joo Park7, Si Yeol Song1,8, Seong-Yun Jeong1, Eun Kyung Choi1,2,8
Institute for Innovative Cancer Research, 2Center for Development and Commercialization of Anti-cancer Therapeutics, Asan Medical Center, Seoul, 3College of Pharmacy, Duksung Women's University, Seoul, 4Department of Parenteral Delivery Program, Samyang Pharmaceuticals R&D, Daejeon, 5Department of Radiology and Research Institute of Radiology, 6Department of Internal Medicine, Asan Medical Center, Seoul, 7Department of Microbiology, College of Medicine, Inha University, Inchon, 8Department of Radiation Oncology, Asan Medical Center, University of Ulsan College of Medicine, Seoul, Korea

*These authors contributed equally to this study

Abstract: Nanoparticles are useful delivery vehicles for promising drug candidates that face obstacles for clinical applicability. Sirolimus, an inhibitor of mammalian target of rapamycin has gained attention for targeted anticancer therapy, but its clinical application has been limited by its poor solubility. This study was designed to enhance the feasibility of sirolimus for human cancer treatment. Polymeric nanoparticle (PNP)–sirolimus was developed as an injectable formulation and has been characterized by transmission electron microscopy and dynamic light scattering. Pharmacokinetic analysis revealed that PNP–sirolimus has prolonged circulation in the blood. In addition, PNP–sirolimus preserved the in vitro killing effect of free sirolimus against cancer cells, and intravenous administration displayed its potent in vivo anticancer efficacy in xenograft tumor mice. In addition, PNP–sirolimus enhanced the radiotherapeutic efficacy of sirolimus both in vitro and in vivo. Clinical application of PNP–sirolimus is a promising strategy for human cancer treatment.

Keywords: sirolimus, polymeric nanoparticle, anticancer, radiotherapy

Creative Commons License This work is published and licensed by Dove Medical Press Limited. The full terms of this license are available at 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:

Potential recombinant vaccine against influenza A virus based on M2e displayed on nodaviral capsid nanoparticles

Yong CY, Yeap SK, Ho KL, Omar AR, Tan WS

International Journal of Nanomedicine 2015, 10:2751-2763

Published Date: 2 April 2015

Functionalization of immunostimulating complexes (ISCOMs) with lipid vinyl sulfones and their application in immunological techniques and therapy

Cruz-Bustos T, González-González G, Morales-Sanfrutos J, Megí­a-Fernández A, Santoyo-González F, Osuna A

International Journal of Nanomedicine 2012, 7:5941-5956

Published Date: 3 December 2012

Antibacterial hemostatic dressings with nanoporous bioglass containing silver

Hu G, Xiao L, Tong P, Bi D, Wang H, Ma H, Zhu G, Liu H

International Journal of Nanomedicine 2012, 7:2613-2620

Published Date: 28 May 2012

Zerovalent bismuth nanoparticles inhibit Streptococcus mutans growth and formation of biofilm

Hernandez-Delgadillo R, Velasco-Arias D, Diaz D, Arevalo-Niño K, Garza-Enriquez M, De la Garza-Ramos MA, Cabral-Romero C

International Journal of Nanomedicine 2012, 7:2109-2113

Published Date: 24 April 2012

Enhanced cellular uptake of aminosilane-coated superparamagnetic iron oxide nanoparticles in mammalian cell lines

Zhu XM, Wang YX, Leung KCF, Lee SF, Zhao F, Wang DW, Lai JMY, Wan C, Cheng CHK, Ahuja AT

International Journal of Nanomedicine 2012, 7:953-964

Published Date: 21 February 2012

Biscarbamate cross-linked polyethylenimine derivative with low molecular weight, low cytotoxicity, and high efficiency for gene delivery

Wang YQ, Su J, Wu F, Lu P, Yuan LF, Yuan WE, Sheng J, Jin T

International Journal of Nanomedicine 2012, 7:693-704

Published Date: 9 February 2012

Preliminary biocompatibility investigation of magnetic albumin nanosphere designed as a potential versatile drug delivery system

Estevanato L, Cintra D, Baldini N, Portilho F, Barbosa L, Martins O, Lacava B, Miranda-Vilela AL, Tedesco AC, Báo S, Morais PC, Lacava ZGM

International Journal of Nanomedicine 2011, 6:1709-1717

Published Date: 18 August 2011