Document Detail

Design and characterization of PEG-derivatized vitamin E as a nanomicellar formulation for delivery of paclitaxel.
MedLine Citation:
PMID:  23768151     Owner:  NLM     Status:  MEDLINE    
Various PEG-Vitamin E conjugates including d-α-tocopheryl poly(ethylene glycol) succinate 1000 (TPGS) have been extensively studied as a nonionic surfactant in various drug delivery systems. However, limited information is available about the structure-activity relationship of PEG-Vitamin E conjugates as a micellar formulation for paclitaxel (PTX). In this study, four PEG-Vitamin E conjugates were developed that vary in the molecular weight of PEG (PEG2K vs PEG5K) and the molar ratio of PEG/Vitamin E (1/1 vs 1/2) in the conjugates. These conjugates were systematically characterized with respect to CMC, PTX loading efficiency, stability, and their efficiency in delivery of PTX to tumor cells in vitro and in vivo. Our data show that PEG5K-conjugates have lower CMC values and are more effective in PTX loading with respect to both loading capacity and stability. The conjugates with two Vitamin E molecules also worked better than the conjugates with one molecule of Vitamin E, particularly for PEG2K-system. Furthermore, all of the PEG-Vitamin E conjugates can induce significant suppression of P-gp function. More importantly, PTX-loaded PEG5K-VE2 resulted in significantly improved tumor growth inhibitory effect in comparison to PTX formulated in PEG2K-VE or PEG2K-VE2, as well as Cremophor EL (Taxol) in a syngeneic mouse model of breast cancer (4T1.2). Our study suggests that PEG5K-Vitmin E2 may hold promise as an improved micellar formulation for in vivo delivery of anticancer agents such as PTX.
Jianqin Lu; Yixian Huang; Wenchen Zhao; Yichao Chen; Jiang Li; Xiang Gao; Raman Venkataramanan; Song Li
Publication Detail:
Type:  Journal Article; Research Support, N.I.H., Extramural; Research Support, U.S. Gov't, Non-P.H.S.     Date:  2013-07-11
Journal Detail:
Title:  Molecular pharmaceutics     Volume:  10     ISSN:  1543-8392     ISO Abbreviation:  Mol. Pharm.     Publication Date:  2013 Aug 
Date Detail:
Created Date:  2013-08-05     Completed Date:  2014-03-05     Revised Date:  2014-08-06    
Medline Journal Info:
Nlm Unique ID:  101197791     Medline TA:  Mol Pharm     Country:  United States    
Other Details:
Languages:  eng     Pagination:  2880-90     Citation Subset:  IM    
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MeSH Terms
Cell Line, Tumor
Chemistry, Pharmaceutical / methods*
Mice, Inbred BALB C
Paclitaxel / administration & dosage*,  chemistry
Polyethylene Glycols / chemistry*
Vitamin E / chemistry*
Grant Support
R21 CA128415/CA/NCI NIH HHS; R21 CA155983/CA/NCI NIH HHS; R21CA128415/CA/NCI NIH HHS; R21CA155983/CA/NCI NIH HHS
Reg. No./Substance:
0/Micelles; 0/Polyethylene Glycols; 1406-18-4/Vitamin E; 33069-62-4/Paclitaxel

From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine

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