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dc.contributor.authorZhang, Peng
dc.contributor.authorHuang, Yixian
dc.contributor.authorLiu, Hao
dc.contributor.authorMarquez, Rebecca T.
dc.contributor.authorLu, Jianqin
dc.contributor.authorZhao, Wenchen
dc.contributor.authorZhang, Xiaolan
dc.contributor.authorGao, Xiang
dc.contributor.authorLi, Jiang
dc.contributor.authorVenkataramanan, Raman
dc.contributor.authorXu, Liang
dc.contributor.authorLi, Song
dc.identifier.citationZhang, 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.
dc.description.abstractWe 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.rightsThis article is available under a Creative Commons Attribution-NonCommercial-NoDerivs 3.0 Unported (CC BY-NC-ND 3.0) License.en_US
dc.subjectDrug-carrier interactionen_US
dc.subjectDrug deliveryen_US
dc.subjectCancer therapyen_US
dc.titleA PEG-Fmoc conjugate as a nanocarrier for paclitaxelen_US
kusw.kuauthorLiu, Hao
kusw.kuauthorMarquez, Rebecca
kusw.kuauthorXu, Liang
kusw.kudepartmentMolecular Biosciences and Radiation Oncologyen_US
kusw.oanotesPer SherpaRomeo on 05/10/2017: Author's Pre-print: green tick author can archive pre-print (ie pre-refereeing) Author's Post-print: green tick author can archive post-print (ie final draft post-refereeing) Publisher's Version/PDF: cross author cannot archive publisher's version/PDF General Conditions: Authors pre-print on any website, including arXiv and RePEC Author's post-print on author's personal website immediately Author's post-print on open access repository after an embargo period of between 12 months and 48 months Permitted deposit due to Funding Body, Institutional and Governmental policy or mandate, may be required to comply with embargo periods of 12 months to 48 months Author's post-print may be used to update arXiv and RepEC Publisher's version/PDF cannot be used Must link to publisher version with DOI Author's post-print must be released with a Creative Commons Attribution Non-Commercial No Derivatives Licenseen_US
kusw.oaversionScholarly/refereed, author accepted manuscripten_US
kusw.oapolicyThis item meets KU Open Access policy criteria.en_US

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This article is available under a Creative Commons Attribution-NonCommercial-NoDerivs 3.0 Unported (CC BY-NC-ND 3.0) License.
Except where otherwise noted, this item's license is described as: This article is available under a Creative Commons Attribution-NonCommercial-NoDerivs 3.0 Unported (CC BY-NC-ND 3.0) License.