Ligand conjugated tumor targeted nanoparticle drug delivery system of vincristine: 32 Full factorial design and in vitro evaluation.

[摘要] An active targeting system is more preferred to enhance intracellular uptake of drug within tumor tissues, while it is highly restricted in normal tissues. Various targeting moieties or ligands against tumor cell-specific receptors have been immobilized on the surface of nano-particulate carriers to deliver them within cells via receptor-mediated endocytosis. This study investigated the preparation and characterization of a targeted system represented by folateconjugated vincristine sulfate-loaded polymeric nanoparticles for breast cancer. Conjugation of folic acid to PLGA was achieved by coupling di-block copolymer with folic acid. The vincristine sulfate loaded nanoparticles, prepared by solvent evaporation method were characterized by particle size analysis, entrapment efficiency and in-vitro drug release. The optimization of formulation was done by three square full factorial design. Phase ratio and sonication time were the independent variables, while particle size and entrapment efficiency were responses. The optimized nanoparticles showed a particle size of 200.3 nm and an entrapment efficiency of 54.33%. The ANOVA results of particle size showed a Model F-value of 104.45, implies the model is significant. And for entrapment efficiency, the Model F-value of 59.55 implies the model is significant. By in-vitro drug release studies, the optimized formulation showed sustained release characteristics following Non-Fickian type of diffusion controlled release.

[学科分类] 药理学