Currently,
glioblastoma (glioma) is described as the deadliest brain tumor for
its invasive natural with exceeding difficulty in surgical excision.
Blood-brain barrier (BBB) can restrict the penetration of most therapeutic
reagents including platinum (Pt)-based drugs-the most widely used
reagents in clinical trials for their revolutionized cancer chemotherapy
against a broad range of tumors. Nanomedicine represents a promising
strategy for the intravenous delivery of Pt-based drugs into the brain.
In this research, with the aim of malignant glioma treatment by Pt-based
drugs, a novel nano drug carrier was developed: dendrigraft poly-L-lysines (DGLs) was PEGylated, linked with diethylenetriaminpentaacetic
acid (DTPA) to complex (1,2-diaminocyclohexane)platinum(II) (DACHPt),
and modified with Substance P (SP) as a BBB/glioma dual-targeting
moiety. The preparation and characterization of the platform were
exhibited in detail. The increased targeting capability and antitumor
effect was found both in vitro and in vivo. The well-defined chemical
composition, rigorously nanoscaled size and the first attempt of using
SP as a BBB/glioma dual-targeting group were highlighted. The combined
results suggest this strategy may serve as novel formulation for Pt-based
drugs with the aim of clinical glioma treatment.