Novel versatile self-assembled nanoparticles were developed from biocompatible, biodegradable lithocholic acid derivatives. These nanoparticles can incorporate different cytotoxic drugs (paclitaxel and doxorubicin) and PI3K signalling inhibitor (PI103). Drugs were released from the nanoparticles in a slow, sustained manner at acidic pH. The drug loaded nanoparticles were internalized through lysosomal compartments and induced cell death in HeLa cervical cancer cells.