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Enhanced anticancer efficacy of alpha-tocopheryl succinate by conjugation with polyethylene glycol

Cited 129 time in Web of Science Cited 135 time in Scopus
Authors
Youk, Hee-Jeong; Lee, Eunmyong; Choi, Moon-Kyung; Lee, Young-Ju; Chung, Jun Ho; Kim, So-Hee; Lee, Chang-Hun; Lim, Soo-Jeong
Issue Date
2005-08-06
Publisher
Elsevier
Citation
J Control Release. 2005 Sep 20;107(1):43-52.
Keywords
AnimalsAntineoplastic Agents/*chemistry/*pharmacologyApoptosis/drug effectsCell Line, TumorCell Survival/drug effectsDose-Response Relationship, DrugDrug CarriersDrug Evaluation, PreclinicalFemaleFlow CytometryHumansImmunoblottingInjections, SubcutaneousKineticsMiceMice, NudeMolecular StructureNeoplasm TransplantationPolyethylene Glycols/*chemistry/metabolism/pharmacologyReactive Oxygen Species/metabolismTransplantation, HeterologousVitamin E/*analogs & derivatives/chemistry/metabolism/pharmacologyXenograft Model Antitumor Assays
Abstract
Alpha-tocopheryl polyethylene glycol succinate (TPGS) has been used to enhance the bioavailability of poorly absorbed drugs and as a vehicle for drug delivery systems. In response to recent reports that alpha-tocopheryl succinate (TOS) acts as an anticancer agent, we investigated whether its polyethylene glycol (PEG) conjugate, TPGS, also possesses anticancer activity. TPGS inhibited the growth of human lung carcinoma cells implanted in nude mice, and in an in vitro cell culture, even more potently than TOS. The time-dependent uptake of TPGS into cells did not differ from that of TOS, indicating that the enhanced antitumor efficacy of TPGS was not due to its increased uptake into cells. Compared with TOS, TPGS was more effective at inducing apoptosis and the generation of reactive oxygen species, suggesting that the superior anticancer efficacy of TPGS is associated with its increased ability to induce apoptosis. Our data suggest that further studies assessing the potential usefulness of TPGS in cancer therapeutics are warranted, since its use as a vehicle in the formulation of anticancer drugs may provide an effective way to improve their therapeutic efficacy.
ISSN
0168-3659 (Print)
Language
English
URI
http://www.ncbi.nlm.nih.gov/entrez/query.fcgi?cmd=Retrieve&db=PubMed&dopt=Citation&list_uids=16081183

http://hdl.handle.net/10371/29036
DOI
https://doi.org/10.1016/j.jconrel.2005.05.014
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College of Medicine/School of Medicine (의과대학/대학원)Dept. of Biochemistry & Molecular Biology (생화학교실)Journal Papers (저널논문_생화학교실)
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