【摘要】 目的设计制备氨甲环酸纳米乳膏(TA-NC),并观察其体外透皮效果。方法采用高压均质法制备氨甲环酸纳米乳,并进一步制得TA-NC,检测TA-NC粒径、微观结构及包封率。以裸鼠皮肤为模型,通过体外透皮吸收实验、离体皮肤组织滞留实验考察TA-NC的体外透皮效果;以尼罗红为荧光探针制备荧光标记TA-NC,共聚焦显微镜观察其促透进入真皮层的效果。并考察TA-NC的6个月加速稳定性。结果制备的TA-NC粒径为(109.9±7.4)nm,形态圆整,分布均匀;包封率为(90.13±2.90)%。体外透皮吸收实验中,TA-NC组给药6 h药物皮肤中的累积滞留量达饱和状态,24 h累积透过量达(163.9±7.4)μg·cm-2;TA水溶液组皮肤的滞留量在20μg·cm-2以下,24 h累积透过量为(15.9±0.8)μg·cm-2,组间差异非常显著(P<0.01)。共聚焦显微镜下,荧光素TA水溶液组仅表皮角质层有荧光,荧光标记的TA-NC经皮吸收后可透过角质层和表皮层到达真皮层,且TA-NC粒径越小透皮能力越强。6个月内TA-NC制剂外观性状、有关物质、含量、粒度等均未发生明显改变。结论 TA-NC制备简单,透皮效果显著,稳定性好。更多还原

【Abstract】 AIM To prepare tranexamic acid nano-cream(TA-NC) and evaluate the transdermal effect of TA-NC in vitro.METHODS TA-NC was prepared by further process from TA nano-emulsion which was got through high pressure homogenizing method.TA-NC was characterized for the particle size,morphology and encapsulation efficiency.The transdermal effect of the nano-cream was evaluated by in vitro transdermal delivery/permeation experiments by using skin of nude mice as model.And the TA-NC labeled with Nile red was prepared to study the improved absorption behavior into the dermis of TA by confocal assay in skin of nude mice,too.Accelerated stability test was also carried out for 6 months.RESULTS The prepared TA-NC was(109.9 ± 7.4) nm and presented a regular spherical surface with homogeneous distribution.The encapsulation efficiency was(90.13 ± 2.90) %.In vitro transdermal absorption experiment showed that the retention of TA in skin was saturated after 6 h administration in the TA-NC group,and the total permeated amount of TA was( 163.9 ± 7.4) μg·cm-2,whereas the amount of TA solution group was( 15.9 ± 0.8) μg·cm-2,with a significant difference( P < 0.01).Comparing with Nile red-TA solution which observed fluorescent only in cuticle,the Nile red labeled TA-NC was observed to permeate the cuticle and epidermis and reach the dermis by confocal assay,and the smaller the particle size of TA-NC,the stronger the ability of transdermal ability.The samples showed no significant differences in external properties,related substance,contents and particle size after accelerated stability test.CONCLUSION The TA-NC preparation technology is simple,and the TANC is good stability and can improve the transdermal absorption of TA significantly.更多还原