Abstract: Objective To design arginine-glycine-aspartate-phenylalanine-dodecyl alcohols mediated docetaxel lipid emulsion[RGDFOC₁₂-DTX-LE] and investigate its anti-tumor activity. Methods DTX a broadly used anti-cancer drug, was tested as the model drug. The RGDFOC₁₂-DTX-LE was made of seal oil, lecithin, RGDFOC₁₂ and glycerol. The formulation was obtained by high pressured homogenization. Results The physicochemical property of RGDFOC₁₂-DTX-LE was evaluated by measuring mean particle size(190 nm~250 nm), Zeta potential(-30 mV to -40 mV), eccentricity constants(Ke<0.7), pH(6.5~8.0). Drug entrapment efficiency was greater than 90%. Transmission electron microscopy(TEM) and scanning electron microscopy(SEM) indicated that RGDFOC₁₂-DTX-LEs appeared to be homogeneous and spherical particles. The result of dynamic dialysis method demonstrated that the drug was released from the emulsion slowly. Cytotoxicity studies in HepG2, A375, SH-sy5y, HeLa, MCF-7 cell lines were explored and DTX mixed suspension is the positive control. RGDFOC₁₂-DTX-LE for each cell line had obvious time-dependent effect and presents the characteristics of slow releasing. The in vivo anti-tumor activity experiments showed that RGDFOC₁₂-DTX-LE exhibited better anti-tumor activity. Conclusion In this work RGDF-mediated docetaxel lipid emulsion preparation, had a good in vitro stability, lower injection irritation, enhanced compliance, sustained release property and better anti-tumor effect.

Key words: arginine-glycine-aspartate-phenylalanine-dodecyl alcohols, docetaxel, lipid emulsion, seal oil, anti-tumor