斑蝥素脂质体凝胶剂的研制与质量评价

目的 :研究斑蝥素脂质体凝胶的制备工艺 ,并初步评价其质量。方法 :用均匀设计法优选斑蝥素脂质体 (LC)的最佳处方及制备工艺 ,借助数字显微镜及病理图像分析系统 (MoticB5 professionalseries)观测其外观、大小及分布 ;用离心法结合GC法测定其包封率及渗漏率 ;并进一步将其制成凝胶剂 ,初步观察其稳定性 ,并以家兔为试验对象与对照品 (较膏剂 )比较其皮肤刺激性 ,用大鼠离体皮肤的扩散实验与对照品比较斑蝥素的透皮扩散情况。结果 :所得脂质体外观圆整 ,粒径分布均匀 ,平均包封率为 (79.7± 1 .2 ) %(n =5 ) ,稳定性良好 ;所得凝胶剂为半透明粘稠状胶体 ,与对照品相比皮肤刺激性显著减小 ,2 4h后皮肤内斑蝥素的滞留量显著增加 (为对照组的 2 .6倍 ) ,而透皮扩散的量极微。结论 :该脂质体凝胶制备工艺可行 ,质量稳定 ,检测方法可靠 ,高效、低毒 ,可望成为临床治疗斑秃的新制剂。

The preparation and quality evaluation of liposomal gel of cantharidin

OBJECTIVE To study the preparation method and quality evaluation of cantharidin liposmal gel. METHODS The optimum composition and preparation method of the liposome was selected with uniform design, its appearance and size distribution was detected with digital microscope. High speed centrifuge and GC were used to study the encapsulation and leakage ratio of the liposome. The stability of the formulation was also observed preliminarily. The skin irritating was tested using the rabbits and its transdermal diffusion was tested using the Wistar rice's skin in vitro compared with ointment formulation. RESULTS The liposome had a fine looking outward appearance, narrow size distribution, higher encapsulation ratio and good stability. Compared with the control(ointment),it had significant protective action for the skin of rabbits. It resulted higher accumulation of cantharridin in the Wistar mice's skin(2.6 fold), while lower transdermal diffusion 24 h later. CONCLUSIONS The results strongly suggests that the cantharidin liposomal gel is valuable to be further developed as a new effective therapeutic preparation for alopecia areata.