Optimization of Weight Ratio for DSPE-PEG/TPGS Hybrid Micelles to Improve Drug Retention and Tumor Penetration.

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dc.contributor.author Jin, Ya en
dc.contributor.author Wu, Zimei en
dc.contributor.author Li, Caibin en
dc.contributor.author Zhou, Weisai en
dc.contributor.author Shaw, John en
dc.contributor.author Baguley, Bruce en
dc.contributor.author Liu, Jianping en
dc.contributor.author Zhang, Wenli en
dc.date.accessioned 2018-10-17T01:27:33Z en
dc.date.issued 2018-01-04 en
dc.identifier.issn 0724-8741 en
dc.identifier.uri http://hdl.handle.net/2292/42358 en
dc.description.abstract PURPOSE:To enhance therapeutic efficacy and prevent phlebitis caused by Asulacrine (ASL) precipitation post intravenous injection, ASL-loaded hybrid micelles with size below 40 nm were developed to improve drug retention and tumor penetration. METHODS:ASL-micelles were prepared using different weight ratios of 1,2-distearoyl-sn-glycero-3-phosphoethanolamine-polyethyleneglycol-2000 (DSPE-PEG2000) and D-α-tocopheryl polyethylene glycol 1000 succinate (TPGS) polymers. Stability of micelles was optimized in terms of critical micelle concentration (CMC) and drug release properties. The encapsulation efficiency (EE) and drug loading were determined using an established dialysis-mathematic fitting method. Multicellular spheroids (MCTS) penetration and cytotoxicity were investigated on MCF-7 cell line. Pharmacokinetics of ASL-micelles was evaluated in rats with ASL-solution as control. RESULTS:The ASL-micelles prepared with DSPE-PEG2000 and TPGS (1:1, w/w) exhibited small size (~18.5 nm), higher EE (~94.12%), better sustained in vitro drug release with lower CMC which may be ascribed to the interaction between drug and carriers. Compared to free ASL, ASL-micelles showed better MCTS penetration capacity and more potent cytotoxicity. Pharmacokinetic studies demonstrated that the half-life and AUC values of ASL-micelles were approximately 1.37-fold and 3.49-fold greater than that of free ASL. CONCLUSIONS:The optimized DSPE-PEG2000/TPGS micelles could serve as a promising vehicle to improve drug retention and penetration in tumor. en
dc.format.medium Electronic en
dc.language eng en
dc.relation.ispartofseries Pharmaceutical research en
dc.rights Items in ResearchSpace are protected by copyright, with all rights reserved, unless otherwise indicated. Previously published items are made available in accordance with the copyright policy of the publisher. en
dc.rights.uri https://researchspace.auckland.ac.nz/docs/uoa-docs/rights.htm en
dc.subject Animals en
dc.subject Humans en
dc.subject Rats en
dc.subject Rats, Sprague-Dawley en
dc.subject Polyethylene Glycols en
dc.subject Vitamin E en
dc.subject Amsacrine en
dc.subject Phosphatidylethanolamines en
dc.subject Antineoplastic Agents en
dc.subject Delayed-Action Preparations en
dc.subject Drug Carriers en
dc.subject Cell Culture Techniques en
dc.subject Drug Stability en
dc.subject Cell Survival en
dc.subject Micelles en
dc.subject Particle Size en
dc.subject Permeability en
dc.subject Surface Properties en
dc.subject Half-Life en
dc.subject Male en
dc.subject Nanoparticles en
dc.subject MCF-7 Cells en
dc.subject Drug Liberation en
dc.title Optimization of Weight Ratio for DSPE-PEG/TPGS Hybrid Micelles to Improve Drug Retention and Tumor Penetration. en
dc.type Journal Article en
dc.identifier.doi 10.1007/s11095-017-2340-y en
pubs.issue 1 en
pubs.begin-page 13 en
pubs.volume 35 en
dc.rights.holder Copyright: The author en
dc.identifier.pmid 29302821 en
pubs.publication-status Published en
dc.rights.accessrights http://purl.org/eprint/accessRights/RestrictedAccess en
pubs.subtype Research Support, Non-U.S. Gov't en
pubs.subtype Journal Article en
pubs.elements-id 720354 en
pubs.org-id Medical and Health Sciences en
pubs.org-id Pharmacy en
pubs.org-id Science en
pubs.org-id Science Research en
pubs.org-id Maurice Wilkins Centre (2010-2014) en
dc.identifier.eissn 1573-904X en
pubs.record-created-at-source-date 2018-01-06 en
pubs.dimensions-id 29302821 en


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