Abstract：
:Cardiac glycosides (CGs) have been used to treat cancer for hundreds of years. However, the narrow therapeutic window and system toxicity have hindered their wide clinical applications. Herein, the small molecule prodrug strategy and nanotechnology were integrated into one drug delivery system with enhanced therapeutic effect. Using periplocymarin (PPM) as a target agent, we designed a novel redox-responsive prodrug conjugated with linoleic acid (PPM-ss-LA), which was capable of self-assembling independent of exogenous excipients. This prodrug could co-assemble with DSPE2k to form PEGylated prodrug nanoparticles (PPM-ss-LA/DSPE2k-NPs) with enhanced colloidal stability and blood circulation. Compared with free PPM, PPM-ss-LA/DSPE2k-NPs retained high anti-proliferative activity and showed increased cell uptake and therapeutic efficacy. Furthermore, the PPM-ss-LA/DSPE2k-NPs acquired a greatly enhancement of 50% lethal dose (LD50) in mice and reduced system toxicity compared with the free drug. Overall, the on-demand release of nanoprodrug delivery system could improve the therapeutic window and anticancer efficacy of CGs.
journal_name
Int J Pharmjournal_title
International journal of pharmaceuticsauthors
Zhang H,Zhu Y,Sun C,Xie Y,Adu-Frimpong M,Deng W,Yu J,Xu X,Han Z,Qi Gdoi
10.1016/j.ijpharm.2019.118980subject
Has Abstractpub_date
2020-02-15 00:00:00pages
118980eissn
0378-5173issn
1873-3476pii
S0378-5173(19)31041-5journal_volume
575pub_type
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