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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 in vitro release, transdermal penetration and skin retention of the main drug when Vitamin C palmitate vesicle is used as Vitamin A acid carrier. Methods Franz diffusion cell was used to determine the release rate of retinoic acid from the carrier. The diffusion membrane was a cellulose membrane (molecular weight cut-off of 8000-14000) between the diffusion cell and the donor cell. The diffusion cell area was 2.92cm2. In vitro transdermal testing Semi-permeable membranes were replaced with mouse, rat or rabbit back skin. At the end of the in vitro transdermal test, the skin was removed, the homogenate was sheared and homogenized and extracted with 50% isopropanol-normal saline. After the extract was treated, the drug concentration was determined by HPLC. Results The results showed that the release rate of retinoic acid and cumulative transdermal permeation were greater than the commercially available cream with high skin retention. Conclusions Vitamin C palmitate vesicles help to increase the local drug concentration as a retinoic acid carrier.