Multifunctional nanocomposite based on graphene oxide for in vitro hepatocarcinoma diagnosis and treatment.

Because of its unique chemical and physical properties, graphene oxide (GO) has attracted a large number of researchers to explore its biomedical applications in the past few years. Here, we synthesized a novel multifunctional nanocomposite based on GO and systemically investigated its applications for in vitro hepatocarcinoma diagnosis and treatment. This multifunctional nanocomposite named GO-PEG-FA/Gd/DOX was obtained as the following procedures: gadolinium-diethylenetriamine-pentaacetic acid-poly(diallyl dimethylammonium) chloride (Gd-DTPA-PDDA) as magnetic resonance imaging (MRI) probe was applied to modify GO by simple physical sorption with a loading efficiency of Gd(3+) up to 0.314 mg mg(-1). In order to improve its tumor targeting imaging and treatment efficiency, the obtained intermediate product was further modified with folic acid (FA). Finally, the nanocomposite was allowed to load anticancer drug doxorubicin hydrochloride via π-π stacking and hydrophobic interaction with the loading capacity reaching 1.38 mg mg(-1). MRI test revealed that GO-PEG-FA/Gd/DOX exhibit superior tumor targeting imaging efficiency over free Gd(3+). The in vitro release of DOX from the nanocomposite under tumor relevant condition (pH 5.5) was fast at the initial 10 h and then become relatively slow afterward. Moreover, we experimentally demonstrated that the multifunctional nanocomposite exhibited obviously cytotoxic effect upon cancer cells. Above results are promising for the next in vivo experiment and make it possible to be a potential candidate for malignancy early detection and specific treatment.

Self-assembling nanomicelles of a novel camptothecin prodrug engineered with a redox-responsive release mechanism.

A novel amphiphilic camptothecin prodrug that spontaneously arranges into nanomicelles which preferentially release the cytotoxic drug under tumor-relevant reductive conditions is designed.

Rapidly disassembling nanomicelles with disulfide-linked PEG shells for glutathione-mediated intracellular drug delivery.

The synthesis and biological efficacy of novel nanomicelles that rapidly disassemble and release their encapsulated payload intracellularly under tumor-relevant glutathione (GSH) levels are reported. The unique design includes a PEG-sheddable shell and poly(ε-benzyloxycarbonyl-l-lysine) core with a redox-sensitive disulfide linkage.

Novel vesicles self-assembled from amphiphilic star-armed PEG/polypeptide hybrid copolymers for drug delivery.

A novel amphiphilic four-armed [poly(ε-benzyloxycarbonyl-L-lysine)]2-block-poly(ethylene glycol)-block-[poly(ε-benzyloxycarbonyl-L-lysine)]2 hybrid copolymer has been prepared. The cytotoxicity study shows that the copolymer has good biocompatibility with no obvious inhibition effect on cell growth. The amphiphilic copolymers could self-assemble to form vesicles in aqueous solution. DOX · HCl, as a hydrophilic drug, can be loaded into the vesicles, and then successfully internalized by human breast cancer MCF-7 cells. Importantly, the DOX-loaded vesicles show a greatly improved drug release behavior with a zero-order release at the initial stage, suggesting a great potential as the carrier of hydrophilic drugs for controlled drug delivery.