鬼臼毒素固体脂质纳米粒经皮渗透和皮肤贮留研究

Study on the in vitro transdermal penetration and retention of podophyllotoxin solid lipid nanoparticles

目的研究鬼臼毒素固体脂质纳米粒经皮渗透和皮肤贮留情况。方法采用Franz扩散池测定鬼臼毒素固体脂质纳米粒的经皮渗透速率,扩散池与供给池之间为大鼠或家兔腹部皮肤,扩散池面积为2.92 cm^2。在体外透皮试验完结后,取下皮肤,剪碎匀浆,用50%异丙醇-生理盐水提取,提取液处理后用HPLC测定药物浓度。结果制得的鬼臼毒素固体脂质纳米粒包封率平均为95.28%,RSD为2.53%（n=5）,粒径在50-200 nm之间。固体脂质纳米粒作为载体时,鬼臼毒素经大鼠和家兔离体腹部皮肤的平均渗透速率和累积透过量较市售酊剂明显降低,同时药物贮留量较市售酊剂明显提高。结论鬼臼毒素固体脂质纳米粒具有较强的皮肤靶向性。

Objective To study in vitro transdermal penetration and retention of podophyllotoxin solid lipid nanoparticles（SLN）.Methods The in vitro transdermal penetration of podophyllotoxin from SLN was determined by Franz diffusion cells.Between donor compartment and receptor compartment was abdominal skin of rats or rabbits,the avaiable diffusion area of cells was 2.92 cm2.The sample was analyzed by HPLC after treatment.After in vitro transdermal penetration experiment completed,the skin were taken down from cells,cut and homogenated,then extracted with 50% isopropanol-normal saline.The extracting solution was analyzed by HPLC.Results The encapsulation efficiency of obtained podophyllotoxin solid lipid nanoparticles were 95.28% on average,with RSD was 2.53%（n=5） and diameter between 50200 nm.When solid lipid nanoparticles as deliverer,the average transdermal rate and cumulative transdermal quantity of podophyllotoxin through rat and rabbit abdominal skin in vitro were significantly lower than marketed tincture,while skin retention quantity of podophyllotoxin in rat and rabbit abdominal skin were significantly higher than marketed tincture.Conclusion Podophyllotoxin SLN had higher local concentration of drug in skin.