Journal
DRUG DELIVERY
Volume 23, Issue 4, Pages 1272-1281Publisher
TAYLOR & FRANCIS LTD
DOI: 10.3109/10717544.2016.1165312
Keywords
Docetaxel; liposome; pharmacokinetics; prodrug; redox-responsive
Categories
Funding
- National Nature Science Foundation of China [81273450]
- Nature Science Foundation of Liaoning Province [2014020079]
- General Project in Education Department of Liaoning Province [L2014396]
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There is a strong desire to develop docetaxel (DTX) formulation with good therapeutic effectiveness in view of serious adverse reactions of the commercial formulation of DTX (Taxotere (R)). In this study, a redox-responsive DTX-vitamin E prodrug was successfully formulated into liposomes with the drug loading of 4.14% +/- 0.10%. Compared with DTX liposomes, the DTX prodrug liposomes (DPLs) showed good stability for 30-d shelf life and during dilution with different media. In vitro antitumor activity of DPLs on human prostatic carcinoma PC-3 cells and human lung cancer A549 cells was evaluated using cytotoxicity and apoptosis assays. In spite of a decrease in in vitro antitumor activity, the in vivo pharmacokinetic study reveals that DPLs exhibit significantly longer DTX plasma half-life (t(1/2), 1.38-fold) and higher bioavailability (AUC(0-t), 14.49-fold) compared with DTX liposomes. The antitumor activity of DPLs to the A549 tumor xenograft model showed selective accumulation in tumor tissue, significant inhibition the growth of the tumors and a much lower toxicity as seen in body weight loss, compared with DTX-Solution. Taken together, the results showed that DPLs is a promising strategy for DTX antitumor delivery.
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