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A PEG-Fmoc conjugate as a nanocarrier for paclitaxel
dc.contributor.author | Zhang, Peng | |
dc.contributor.author | Huang, Yixian | |
dc.contributor.author | Liu, Hao | |
dc.contributor.author | Marquez, Rebecca T. | |
dc.contributor.author | Lu, Jianqin | |
dc.contributor.author | Zhao, Wenchen | |
dc.contributor.author | Zhang, Xiaolan | |
dc.contributor.author | Gao, Xiang | |
dc.contributor.author | Li, Jiang | |
dc.contributor.author | Venkataramanan, Raman | |
dc.contributor.author | Xu, Liang | |
dc.contributor.author | Li, Song | |
dc.date.accessioned | 2017-05-10T17:49:49Z | |
dc.date.available | 2017-05-10T17:49:49Z | |
dc.date.issued | 2014-08 | |
dc.identifier.citation | Zhang, P., Huang, Y., Liu, H., Marquez, R., Lu, J., Zhao, W., … Li, S. (2014). A PEG-Fmoc conjugate as a nanocarrier for paclitaxel. Biomaterials, 35(25), 7146–7156. http://doi.org/10.1016/j.biomaterials.2014.04.108 | en_US |
dc.identifier.uri | http://hdl.handle.net/1808/24073 | |
dc.description.abstract | We report here that a simple, well-defined, and easy-to-scale up nanocarrier, PEG5000-lysyl-(α-Fmoc-ε-t-Boc-lysine)2 conjugate (PEG-Fmoc), provides high loading capacity, excellent formulation stability and low systemic toxicity for paclitaxel (PTX), a first-line chemotherapeutic agent for various types of cancers. 9-Fluorenylmethoxycarbonyl (Fmoc) was incorporated into the nanocarrier as a functional building block to interact with drug molecules. PEG-Fmoc was synthesized via a three-step synthetic route, and it readily interacted with PTX to form mixed nanomicelles of small particle size (25–30 nm). The PTX loading capacity was about 36%, which stands well among the reported micellar systems. PTX entrapment in this micellar system is achieved largely via an Fmoc/PTX π-π stacking interaction, which was demonstrated by fluorescence quenching studies and 13C-NMR. PTX formulated in PEG-Fmoc micelles demonstrated sustained release kinetics, and in vivo distribution study via near infrared fluorescence imaging demonstrated an effective delivery of Cy5.5-labled PTX to tumor sites. The maximal tolerated dose for PTX/PEG-Fmoc (MTD > 120 mg PTX/kg) is higher than those for most reported PTX formulations, and in vivo therapeutic study exhibited a significantly improved antitumor activity than Taxol, a clinically used formulation of PTX. Our system may hold promise as a simple, safe, and effective delivery system for PTX with a potential for rapid translation into clinical study. | en_US |
dc.publisher | Elsevier | en_US |
dc.rights | This article is available under a Creative Commons Attribution-NonCommercial-NoDerivs 3.0 Unported (CC BY-NC-ND 3.0) License. | en_US |
dc.rights.uri | https://creativecommons.org/licenses/by-nc-nd/3.0/ | en_US |
dc.subject | Micelle | en_US |
dc.subject | 9-Fluorenylmethoxycarbonyl | en_US |
dc.subject | Drug-carrier interaction | en_US |
dc.subject | Drug delivery | en_US |
dc.subject | Paclitaxel | en_US |
dc.subject | Cancer therapy | en_US |
dc.title | A PEG-Fmoc conjugate as a nanocarrier for paclitaxel | en_US |
dc.type | Article | en_US |
kusw.kuauthor | Liu, Hao | |
kusw.kuauthor | Marquez, Rebecca | |
kusw.kuauthor | Xu, Liang | |
kusw.kudepartment | Molecular Biosciences and Radiation Oncology | en_US |
dc.identifier.doi | 10.1016/j.biomaterials.2014.04.108 | en_US |
kusw.oaversion | Scholarly/refereed, author accepted manuscript | en_US |
kusw.oapolicy | This item meets KU Open Access policy criteria. | en_US |
dc.identifier.pmid | PMC4102141 | en_US |
dc.rights.accessrights | openAccess |