Development and characterization of paclitaxel and embelin loaded solid lipid nanoparticles for breast cancer

摘要

In an effort to develop an alternative formulation of combination of paclitaxel (PTX) and embelin (EMB) suitable for parenteral administration, PTX-EMB loaded sterically stabilized solid lipid nanoparticles (SLNs) were prepared, characterized and examined for in vitro cytotoxicity. The SLNs, comprising glycerol mono stearate (GMS) as a solid lipid core, Brij 35 used as surfactant and PEGylated phospholipid used as stabilizer, were prepared using a hot homogenization method. Optimized PTX-EMB loaded formulation, the particle sizes of the prepared SLNs were around 300 nm, suggesting that they would be suitable as a parenteral formulation. Transmission electron microscopy showed that the SLNs were homogeneous and spherical in shape. Entrapment efficiency of paclitaxel and embelin was 92.83 ± 2.2%, 83.25 ± 2.4% respectively. An in vitro drug release study were performed in PBS (pH 7.4) for 80 hrs and observed that paclitaxel and embelin released from the PEGylated SLNs was 93.91 ± 4.1 % and 75.63 ± 4.37 % respectively. Furthermore, treatment of the MCF-7 breast cancer cell line with PTX-EMB loaded SLNs yielded cytotoxicities comparable to PTX solution, PTX-EMB mixture solution and PTX loaded PEGylated SLNs. These results collectively suggest that our optimized SLN formulation may have a potential as alternative delivery system for parenteral administration of paclitaxel and embelin.