Lipid-coated nanoscale coordination polymers for targeted cisplatin delivery

Nanoscale coordination polymers (NCPs) containing a Pt(IV) cisplatin prodrug, disuccinatocisplatin, were formed by a surfactant-templated synthesis and were shown to have a prodrug loading of 8.2 wt% and a diameter of similar to 133 nm by dynamic light scattering. These NCPs were stabilized by coating with a DOPC/cholesterol/DSPE-Peg(2) (kappa) lipid layer; a release profile in phosphate buffered saline showed an initial drug release of similar to 25% within the first hour and no more release observed up to 192 h. The NCP was rendered target-specific for sigma receptors by addition of a DSPE-Peg(2) (kappa)-AA conjugate (AA = anisamide) in the lipid formulation. The AA-containing NCP showed a statistically significant decrease in IC50 (inhibitory concentration, 50%) compared to the non-targeted NCP. Enhanced uptake of the AA-containing NCP was further supported by confocal microscopy and competitive binding assays.