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第119篇论文被International Journal Pharmaceutics接受发表!

Zhi Wang, Longbing Ling, Yawei Du, Chen Yao, Xinsong Li*, Reduction responsive liposomes based on paclitaxel-ss-lysophospholipid with high drug loading for intracellular delivery

International Journal of Pharmaceutics 564 (2019) 244–255

Abstract: In this report, a novel redox-responsive liposomes based on disulfide derivative paclitaxel-ss-lysophosphatidylcholine prodrug (PTX-ss-PC) with high PTX loading was developed for triggering drug release. First of all, PTX-ss-PC was synthesized by a facile esterification and verified by MS, 1H NMR and HPLC. After that, PTXss-PC derived liposomes (PTX-ss-PC liposomes) containing EPC:Chol:mPEG2000-DSPE components were prepared

by the conventional film method。 Moreover, physicochemical characterizations of the PTX-ss-PC liposomes were carried out by using transmission electron microscope (TEM), dynamic light scattering (DLS) and release test。 It was demonstrated that the PTX-ss-PC liposomes possessed average diameter of 234。9 nm and zeta potential of ?29。1 mV with highest PTX loading 7。97%。 The PTX-ss-PC liposomes dissociated rapidly in a reduction medium, as confirmed by their triggered aggregation/disruption and rapid release of PTX in the presence of glutathione (GSH)。 Finally, in vitro cytotoxicity of the liposomes was checked against MCF-7 and A549 cells。 It was found that the PTX-ss-PC liposomes exhibited favorable GSH-mediated anti-proliferative activity in comparison with the nonresponsive counterpart。 Taken together, the novel PTX-ss-PC based liposomes possess improved loading capacity, reduction triggered release of PTX and efficient anti-proliferative activity, which should be valuable for further preclinical evaluation。


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