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Title: Trastuzumab-conjugated vitamin e TPGS liposomes for sustained and targeted delivery of docetaxel
Authors: Raju, A.
Muthu, M.S.
Feng, S.-S. 
Keywords: Cancer nanotechnology
Chemotherapeutic engineering
Drug targeting
Solvent injection method
Issue Date: Jun-2013
Citation: Raju, A., Muthu, M.S., Feng, S.-S. (2013-06). Trastuzumab-conjugated vitamin e TPGS liposomes for sustained and targeted delivery of docetaxel. Expert Opinion on Drug Delivery 10 (6) : 747-760. ScholarBank@NUS Repository.
Abstract: Objectives: In this study, the authors developed d-α-tocopheryl polyethylene glycol 1000 succinate (vitamin E TPGS or simply TPGS) liposomes and further conjugated them to trastuzumab for controlled and targeted delivery of docetaxel (DTX) as a model hydrophobic drug. Methods: DTX-or coumarin-6-loaded liposomes were prepared by solvent injection method and characterized for size and size distribution, surface charge, surface chemistry and drug encapsulation efficiency and drug release profile. SK-BR-3 cells were employed as an in vitro model for HER2-positive breast cancer and assessed for their cellular uptake and cytotoxicity of the two liposomal formulations. In vivo pharmacokinetics (PK) was investigated in Sprague-Dawley rats. Results: The IC50 value was found to be 20.23 ± 1.95, 3.74 ± 0.98, 0.08 ± 0.4 μg/ml for the marketed preparation of DTX, TPGS liposomes and trastuzumab-conjugated TPGS liposomes, respectively after 24 h incubation with SK-BR-3 cells. In vivo PK experiments showed that i.v. administration of trastuzumab-conjugated liposomes achieved 1.9 and 10 times longer half-life, respectively than PEG-coated liposomes and DTX. The area under the curve (AUC) was increased by 3.47-and 1.728-fold, respectively. Conclusion: The trastuzumab-conjugated vitamin E TPGS-coated liposomes showed greater potential for sustained and targeted chemotherapy in the treatment of HER2 overexpressing breast cancer. © 2013 Informa UK, Ltd.
Source Title: Expert Opinion on Drug Delivery
ISSN: 17425247
Appears in Collections:Staff Publications

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