炔雌醇醇质体凝胶的经皮渗透研究

 目的考察醇质体凝胶作为炔雌醇透皮给药载体的可行性。方法采用注入法制备炔雌醇醇质体,进而用卡波姆制备成凝胶,采用TK-6H型透皮扩散试验仪用人皮进行体外经皮渗透实验;以HPLC测定药物含量求算累积渗透量及稳态透皮速率,并测定药物在皮肤表皮和真皮中的滞留量。结果炔雌醇醇质体凝胶的经皮渗透速率(3.59μg·cm^-2·h^-1)是其水溶液的9.97倍,是体积分数为30%乙醇溶液的1.69倍,是凝胶制剂(含醇量30%)的1.45倍。24 h后皮肤中药物滞留量大小顺序为:醇质体凝胶>体积分数为30%乙醇溶液>凝胶>饱和水溶液。结论醇质体凝胶能提高炔雌醇的透皮速率,增加药物在皮肤内的滞留量。

Study on Transdermal Penetration of Ethinyl Estradiol Ethosome Gel

OBJECTIVE To investigate the feasibility of ethosome gel as transdermal carries of ethinyl estradiol(EE).METHODS EE was encapsulated in ethosomes composed of phospholipid and ethanol,then ethosomes were incorporated in carbopol gel.Percutaneous permeation of EE was observed using human skin and TK-6H transdermal diffusion device in vitro.The concentrations of EE in receptor compartment at specified time points were determined by HPLC. The steady flux and the accumulation quantity of ethinyl estradiol in skin were calculated.RESULTS The flux of EE from ethosome gel was 3.59 μg·cm^-2·h^-1,which were 9.97,1.69 and 1.45 times higher than that from saturated aqueous solution,30% ethanol solution,gel preparation (contain ethanol 30%),respectively.The subsequence of retention amount in the skin after 24 h was: ethosome gel > 30% ethanol solution > gel> drug-saturated aqueous solution.CONCLUSION Ethosome gel is effective for transdermal delivery and increased the EE amount retained in the skin.