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 |