Journal
JOURNAL OF PHARMACY AND PHARMACOLOGY
Volume 71, Issue 8, Pages 1243-1254Publisher
OXFORD UNIV PRESS
DOI: 10.1111/jphp.13126
Keywords
breast cancer; D-alpha-tocopheryl polyethylene glycol 1000 succinate; docetaxel; liposome; multidrug resistance
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Objectives Multidrug resistance (MDR) remains a primary challenge in breast cancer treatment. In the present study, D-alpha-tocopheryl polyethylene glycol 1000 succinate (TPGS)-coated docetaxel-loaded liposomes were developed as a novel drug delivery system to reverse MDR and enhance breast cancer therapy compared with the traditional liposomes, DSPE-mPEG-coated liposomes (stealth liposomes) and commercial Taxotere (R). Key findings Liposomes were prepared by thin - film dispersion method. Evaluations were performed using human breast cancer MCF-7 and resistant MCF-7/ADR cells. The reversal multidrug-resistant effect was assessed by P-gp inhibition assay, cytotoxicity, cellular uptake and apoptosis assay. Results The TPGS-chol-liposomes were of an appropriate particle size (140.0 +/- 6.0 nm), zeta potential (-0.196 +/- 0.08 mv), high encapsulation efficiency (99.0 +/- 0.9) and favourable in vitro sustained release. The TPGS-coated liposomes significantly improved cytotoxicity and increased the intracellular accumulation of docetaxel in both types of breast cancer cells. The TPGS-coated liposomes were confirmed to induce apoptosis via a synergistic effect between docetaxel and TPGS. It was demonstrated that TPGS enhanced the intracellular accumulation of drug by inhibiting overexpressed P-glycoprotein. Conclusions The TPGS-conjugated liposomes showed significant advantages in vitro compared with the PEG-conjugated liposomes. The TPGS-conjugated liposomes could reverse the MDR and enhance breast cancer therapy.
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