维A酸维生素C棕榈酸酯泡囊的体外释放、经皮渗透和皮肤贮留研究

Study on the Release Rate,in Vitro Skin Penetration and Retention of Tretinoin Ascorbyl Palmitate Vesicles

目的研究维生素C棕榈酸酯泡囊作为维A酸载体时,主药的体外释放、经皮渗透和皮肤贮留情况。方法采用Franz扩散池测定维A酸从载体中的释放速度,扩散池与供给池之间为纤维素膜(截留分子量8000～14000),扩散池面积为2.92cm2。体外透皮试验用小鼠、大鼠或兔子背部皮肤替代半透膜。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。结果结果表明维A酸释放速率和累积经皮渗透量大于市售乳膏,同时具有较高的皮肤贮留量。结论维生素C棕榈酸酯泡囊作为维A酸载体有助于增加局部药物浓度。

OBJECTIVE To study the release rate,in vitro skin penetration and retention of tretinoin when use ascorbyl palmitate vesicles as its carrier.METHODS The in vitro release rate of tretinoin from carrier was determined by Franz diffusion cell.Between donor compartment and receptor compartment was cellulose membrane（cut-off molecules 8 000-14 000）,the avaiable diffusion area of cell was 2.92 cm^2.In the in vitro skin penetration experiment,the back skin of mouse,rats or rabbits was used instead of cellulose membrane.After in vitro skin penetration experiment,the skin were taken down from cells,cut and homogenated,and then extracted by 50% isopropanol-normal saline.The extracting solution was analyzed by HPLC after treatment.RESULTS The result indicated higher levels of in vitro drug release rate,in vitro tretinoin cumulative penetration quantity and skin retention quantity in ascorbyl palmitate vesicles than cream on sale.CONCLUSION Ascorbyl palmitate vesicles as transdermal administration carrier for tretinoin could increase local concentration of drug.