摘要
目的制备丹酚酸B-蜗牛黏液纳米凝胶(salvianolic acid B-snail mucus nanogel,SAB-SM/Gel),进行相关表征及体外透皮性能研究。方法采用高压均质法制备丹酚酸B-蜗牛黏液纳米粒(salvianolic acid B-snail mucus nanoparticles,SABSM),再用搅拌法将其与凝胶基质制成SAB-SM/Gel。对纳米粒的形状、粒径、多分散指数(polydispersity index,PDI)、ζ电位等进行表征;用Franz扩散池法考察SAB-SM/Gel体外透皮吸收及真皮层滞留性能。结果SAB-SM纳米粒为透明均一的液体,具有丁达尔效应,透射电子显微镜(transmission electron microscope,TEM)下呈球状或类球状结构,大小均一,粒子间无黏连现象,平均粒径为(155.55±2.95)nm,PDI为0.31±0.01,平均ζ电位为(-15.45±1.67)mV,pH值为6.11±0.12,SAB-SM纳米粒中SAB的包封率为(37.70±1.16)%,载药量(1.78±0.06)mg/mL;SAB-SM/Gel在常温下为无色透明液体,TEM下呈圆形或类圆形,pH值为6.24±0.13,包封率为(42.42±1.02)%,SAB载药量(1.44±0.04)mg/mL,平均黏度为0.02 Pa·s,质地均匀细腻,涂抹至皮肤能快速胶凝,可涂布性能良好。体外透皮试验表明,SAB-SM/Gel中SAB在48 h内单位面积累透过量为(188.39±2.89)μg/cm^(2),真皮滞留量为(17.58±0.04)μg/cm^(2),透皮释放过程符合Hixson-Crowell方程。结论SAB-SM/Gel处方工艺合理,具有良好的透皮吸收性能和真皮滞留性能。
Objective To prepare salvianolic acid B-snail mucus nanogel(SAB-SM/Gel)and study its related characterization and the osmotic dynamics of ex vivo skin.Methods Salvianolic acid B-snail mucus nanoparticles(SAB-SM nanoparticles)were prepared by high-pressure homogenization method,and then SAB-SM/Gel was prepared with the gel matrix by stirring.The shape,size,polydispersity index(PDI),ζ potential,etc.of nanoparticles were characterize;The Franz diffusion pool method was used to investigate the transdermal absorption and dermal retention performance of SAB-SM/Gel in vitro.Results SAB-SM nanoparticles are transparent and homogeneous liquid,with Tyndall effect,spherical or spheroid structure under transmission electron microscope(TEM),uniform size,no adhesion between particles,average particle size of(155.55±2.95)nm,PDI of 0.31±0.01,average ζ potential of(-15.45±1.67)mV,pH of 6.11±0.12,encapsulation rate of SAB in SAB-SM nanoparticles is(37.70±1.16)%,and drug load is(1.78±0.06)mg/mL;SAB-SM/Gel is a colorless transparent liquid at room temperature,round or quasi-circular under TEM,pH of 6.24±0.13,encapsulation rate of(42.42±1.02)%,SAB loading capacity of(1.44±0.04)mg/mL,average viscosity of 0.02 Pa·s,uniform and delicate texture,which can be quickly gelled applied to the skin,and has good coating performance.The in vitro transdermal test showed that the cumulative permeability of SAB in SAB-SM/Gel within 48 h was(188.39±2.89)μg/cm^(2),the dermal retention amount was(17.58±0.04)μg/cm^(2),and the transdermal release process conformed to the Hixson-Crowell equation.Conclusion SAB-SM/Gel prescription process is reasonable,with good transdermal absorption and dermal retention performance.
作者
姚碧金
罗玺
张俏菊
郑俊侨
徐万帮
时军
YAO Bi-jin;LUO Xi;ZHANG Qiao-ju;ZHENG Jun-qiao;XU Wan-bang;SHI Jun(School of Traditional Chinese Medicine,Guangdong Pharmaceutical University,Guangzhou 510006,China;Guangdong Institute for Drug Control,Guangzhou 510663,China;Guangdong Engineering&Technology Research Center of Topical Precise Drug Delivery Preparation,Guangzhou 510006,China)
出处
《中草药》
CAS
CSCD
北大核心
2023年第21期6988-6996,共9页
Chinese Traditional and Herbal Drugs
基金
国家自然科学基金资助项目(82173982)
广东省自然科学基金资助项目(2022A1515011382)。
关键词
药辅合一
蜗牛
黏液
丹酚酸B
高压均质法
纳米粒
凝胶
透皮吸收
unification of drugs and excipients
snail
mucus
salvianolic acid B
high pressure homogenization method
nanoparticles
gel
transdermal absorption