Trackable Water-Soluble Prodrug Micelles Capable of Rapid Mitochondrial-Targeting and Alkaline pH-Responsive Drug Release for Highly Improved Anticancer Efficacy.

A trackable water-soluble prodrug conjugate possessing high contents of chlorambucil () and triphenylphosphonium cation () was designed and developed after TPP modification on the "branch" of amphipathic prodrugs based on convenient synthesis of heterobifunctional clickable poly(ethylene glycol) (). The aqueous self-assembly of fluorescent polymeric micelles along precise composition can be easily prepared after directly dissolved () in aqueous solution, and exhibit superior cytotoxicity to cancer cells along with highly improved selectivity and sensitivity because of their rapid mitochondrial-targeting and alkaline pH-responsive drug release capabilities. Notably, efficient codelivery of doxorubicin () for synergistic targeted drug delivery and cancer therapy was achieved.

Chemoenzymatic synthesis of dual-responsive graft copolymers for drug delivery: long-term stability, high loading and cell selectivity.

A series of amphiphilic graft copolymers, poly(N-propargyldiethanolamine 4,4'-dithiodibutyionate)-graft-monomethoxy poly(ethylene glycol) (PPD-g-mPEG), were designed via a chemoenzymatic method for pH and reduced glutathione (GSH) dual-responsive drug delivery. The effects of percent grafting and molecular weights of mPEG on critical micelle concentration (CMC) values, size of micelles, drug loading and dual-response were tested. The graft copolymers could easily form homogeneous spherical micelles with appropriate sizes and zeta-potentials.

Lipase-catalyzed synthesis of azido-functionalized aliphatic polyesters towards acid-degradable amphiphilic graft copolymers.

A series of novel aliphatic polyesters with azido functional groups were synthesized via the direct lipase-catalyzed polycondensation of dialkyl diester, diol and 2-azido-1,3-propanediol (azido glycerol) using immobilized lipase B from Candida antarctica (CALB). The effects of polymerization conditions including reaction time, temperature, enzyme amount, substrates and monomer feed ratio on the molecular weights of the products were studied. The polyesters with pendant azido groups were characterized by (1)H NMR, (13)C NMR, 2D NMR, FTIR, GPC and DSC.

Two birds with one stone: multifunctional and highly selective fluorescent probe for distinguishing Zn2+ from Cd2+ and selective recognition of sulfide anion.

A coumarin-based multifunctional fluorescent sensor containing a di-2-picolylamine (DPA) moiety (1) was presented. Interestingly, this probe could similarly act as ON-OFF type fluorescent sensor for Co(2+) and Cu(2+), then in situ generated 1-Co(II) and 1-Cu(II) ensembles could further serve as OFF-ON type fluorescent sensors to achieve the discrimination of Zn(2+) from Cd(2+) and selective recognition of sulfide anion in aqueous solution via displacement approach, respectively. Specially, 1-Cu(II) could permeate the cell membrane and could be used in fluorescence imaging of S(2-) in living biological samples.