University Institute of Pharmacy, Pt. Ravishankar Shukla University, Raipur, Chhattisgarh, India 492010.
Curr Drug Deliv. 2013 Aug;10(4):466-76. doi: 10.2174/1567201811310040011.
Long term tamoxifen citrate therapy is imperative to treat several dermatological and hormonal sensitive disorders. Successful oral and parenteral administration of tamoxifen citrate has been challenging since it undergoes enzymatic degradation and has poor aqueous solubility issues. In the present work, tamoxifen citrate loaded ethosomes were prepared and characterized for transdermal applications. The prepared formulations were characterized for morphological features, particle size distribution, calorimetric attributes, zeta potential and drug entrapment. Permeation profile of prepared ethosomes was compared with liposomes and hydroethonalic solution across cellophane membrane and human cadaver skin. Results of the permeation studies indicate that ethosomes were able to deliver >90% drug within 24 hours of application, while liposomes and hydroethanolic solution delivered only 39.04% and 36.55% respectively. Skin deposition and stability studies are also reported.
长期使用他莫昔芬柠檬酸盐治疗是治疗几种皮肤和激素敏感疾病的必要手段。由于他莫昔芬柠檬酸盐会发生酶降解，且水溶性差，因此成功地进行口服和肠胃外给药具有挑战性。在本工作中，制备了他莫昔芬柠檬酸盐负载的醇质体并对其经皮应用进行了表征。对制备的制剂进行了形态特征、粒径分布、量热属性、ζ 电位和药物包封率的表征。通过在玻璃纸膜和人体尸体皮肤上比较制备的醇质体、脂质体和水醇溶液的渗透情况。渗透研究结果表明，醇质体在应用 24 小时内能够输送超过 90%的药物，而脂质体和水醇溶液分别仅输送 39.04%和 36.55%。还报告了皮肤沉积和稳定性研究。
