隐形顺铂聚乳酸纳米微粒对口腔鳞癌原发灶的靶向性研究

Objective To investigate the target deliver of Cisplatin to oral carcinoma tissues by intravenous injection of Cispla- tin loaded polylactic acid- polyethylene glycol nanoparticles(CDDP-PLA-PEG-NP).Methods CDDP-PLA-PEG-NP was pre- pared by the emulsion-solvent evaporation method. The buccal cancer model was established in 64 golden hamsters, which were divided randomly into two groups for 32 animals in each group, CDDP-PLA-PEG-NP(6·6 mg/kg ) and CDDP(1 mg/kg)were re- spectively injected into mice tail vein. At 0·083、0·5、1、2、4、6、12、24 h after drug administration. 4 animals in each group were sacrificed and CDDP concentration in the plasma and tumorwere determined by high performance liquid chromatography. Targeting ability was evaluated by targeting index(TI), selectivity index(SI) and relative extraction efficiency(re).Results The average diameter of CDDP-PLA-PEG-NPwas (143·2±1·8)nm. The diameter distributionwas from 103·5 nmto 175·8 nm. Drug loading and embedding ratio were (15·2±0·9)%,(89.0±0·8)% respectively. Values of TI and SI are more than 1 at 8 time points. The area under CDDP concentration-time curve of oral carcinoma tissues in CDDP-PLA-PEG-NP group was 10.36 times as many as that in CDDP group.Conclusion CDDP-PLA-PEG-NP can specifically deliver CDDP to oral carcinoma tissues by vein injec- tion. Stealth anticancer nano-particle system can be regarded as a valuable drug deliver system to treat oral carcinoma.