Please use this identifier to cite or link to this item: http://scholarbank.nus.edu.sg/handle/10635/28303
Title: Doxorubicin conjugated to D-alpha-Tocopheryl Polyethylene Glycol 1000 Succinate (TPGS): In vitro cytotoxicity, in vivo Pharmacokinetics and Biodistribution
Authors: CAO NA
Keywords: Cancer nanotechnology; Chemotherapeutic engineering; Prodrug; Drug modification; Nanomedicine
Issue Date: 7-May-2008
Source: CAO NA (2008-05-07). Doxorubicin conjugated to D-alpha-Tocopheryl Polyethylene Glycol 1000 Succinate (TPGS): In vitro cytotoxicity, in vivo Pharmacokinetics and Biodistribution. ScholarBank@NUS Repository.
Abstract: To develop a novel polymer - anticancer drug conjugate, d-[alpha]-tocopheryl polyethylene glycol 1000 succinate (TPGS) was employed as a carrier of doxorubicin by chemical conjugation. The molecular structure, drug loading efficiency, release kinetics and stability of the conjugate were characterized. The cellular uptake, intracellular distribution, and cytotoxicity were accessed using MCF-7 breast cancer cells and C6 glioma cells as in vitro model. The conjugate showed higher cellular uptake efficiency and broader distribution. Judged by IC50, the conjugate was found more effective with both MCF-7 cells and C6 cells than the parent drug after 24, 48, 72 h culture, respectively. In vivo pharmacokinetics showed significantly larger area-under-the-curve (AUC) and longer half-life in comparison with doxorubicin at 5 mg/kg equivalent dose. The drug level in heart, gastric and intestine was significantly reduced. TPGS-doxorubicin conjugate showed great potential to be a prodrug of higher therapeutic effects and fewer side effects.
URI: http://scholarbank.nus.edu.sg/handle/10635/28303
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