Self-Assembled Nanoparticles Based on Amphiphilic Anticancer Drug–Phospholipid Complex for Targeted Drug Delivery and Intracellular Dual-Controlled Release

Integrating advantages of mitomycin C (MMC)–phospholipid complex for increased drug encapsulation efficiency and reduced premature drug release, DSPE-PEG-folate (DSPE-PEG-FA) for specific tumor targeting, we reported a simple one-pot self-assembly route to prepare the MMC–phospholipid complex-loaded DSPE-PEG-based nanoparticles (MP-PEG-FA NPs). Both confocal imaging and flow cytometry demonstrated that MMC was distributed into nuclei after cellular uptake and intracellular drug delivery. More importantly, the systemically administered MP-PEG-FA NPs led to increased blood persistence and enhanced tumor accumulation in HeLa tumor-bearing nude mice. This study introduces a simple and effective strategy to design the anticancer drug–phospholipid complex-based targeted drug delivery system for sustained/controlled drug release.