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Star‐Shape Redox‐Responsive PEG‐Sheddable Copolymer of Disulfide‐Linked Polyethylene Glycol‐Lysine‐di‐Tocopherol Succinate for Tumor‐Triggering Intracellular Doxorubicin Rapid Release: Head‐to‐Head Comparison
Author(s) -
Ai Xiaoyu,
Sun Jin,
Zhong Lu,
Wu Chunnuan,
Niu Handong,
Xu Tao,
Lian He,
Han Xiaopeng,
Ren Guolian,
Ding Wenya,
Wang Jia,
Pu Xiaohui,
He Zhonggui
Publication year - 2014
Publication title -
macromolecular bioscience
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.924
H-Index - 105
eISSN - 1616-5195
pISSN - 1616-5187
DOI - 10.1002/mabi.201400149
Subject(s) - doxorubicin , chemistry , peg ratio , polyethylene glycol , intracellular , copolymer , cytotoxicity , biophysics , redox , in vivo , biochemistry , in vitro , polymer chemistry , organic chemistry , chemotherapy , medicine , biology , surgery , economics , microbiology and biotechnology , polymer , finance
A redox‐responsive poly(ethylene glycol) (PEG)‐sheddable copolymer of disulfide‐linked PEG 5000‐lysine‐di‐tocopherol succinate (P 5k SSLV) is developed which can self‐assemble into nanomicelles in aqueous condition and trigger the rapid release of encapsulated drugs within tumor cells. The reduction‐insensitive doxorubicin (DOX)‐loaded P 5k LV (P 5k LV‐DOX) nanomicelles are further prepared. Then head‐to‐head comparison of P 5k SSLV‐DOX, P 5k LV‐DOX and DOX‐Sol is performed concerning in vitro release, cytotoxicity, cellular uptake and apoptosis. Results show that P 5k SSLV‐DOX nanomicelles have a faster DOX release, a higher anti‐tumor activity and more DOX concentrating in the nucleus than P 5k LV‐DOX nanomicelles. In conclusion, the redox‐responsive P 5k SSLV nanomicelles might hold a great potential to improve chemotherapy by tumor‐triggering intracellular rapid release. The outcomes of this study also address the significance of such head‐to‐head comparison studies in translational research of nanomedicine.