Folate-PEG Conjugates of a Far-Red Light-Activatable Paclitaxel Prodrug to Improve Selectivity toward Folate Receptor-Positive Cancer Cells.

ABSTRACT: We recently demonstrated the far-red light-activatable prodrug of paclitaxel (PTX), Pc-(L-PTX)₂. Upon illumination with a 690 nm laser, Pc-(L-PTX)₂ showed combinational cell killing from rapid photodynamic therapy damage by singlet oxygen, followed by sustained chemotherapy effects from locally released PTX. However, its high lipophilicity (log D_7.4 > 3.1) caused aggregation in aqueous solutions and has nonselectivity toward cancer cells. To solve these important problems, we prepared folic acid (FA)-conjugated and photoactivatable prodrugs of PTX with a polyethylene glycol (PEG) spacer of various chain lengths: FA-PEG _n -Pc-L-PTX [n = 0 (0k, 5), ∼23 (1k, 7a), ∼45 (2k, 7b), ∼80 (3.5k, 7c), or ∼114

SUBMITTER: Thapa P 

PROVIDER: S-EPMC5664141 | biostudies-literature | 2017 Oct

REPOSITORIES: biostudies-literature