Study on the Preparation and Transdermal Permeability of Soluble Microneedles Loaded with Gastrodin in vitro
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摘要:
目的 制备天麻素全载药可溶性微针, 并考察其理化性质及体外透皮性能。 方法 采用两步离心法制备天麻素全载药可溶性微针, HPLC法测定其载药量, 并进行形态学、机械性能、皮肤穿刺性能和恢复性能考察; 采用Franz扩散池考察其体外透皮性能。 结果 所制微针阵列完整, 柔韧性好, 每片载药量达(5.45±0.14)mg, 机械性能良好, 能成功刺穿大鼠皮肤, 微针处理后皮肤在2 h内即可恢复到原来的状态。离体皮肤渗透结果显示, 12 h后全载药微针中天麻素的累积渗透量可达87%, 而天麻素溶液中天麻素的累积渗透量为12%, 说明可溶性微针对天麻素具有良好的透皮递送促进作用。 结论 制备的天麻素全载药可溶性微针机械强度及柔韧性好, 实现了水溶性药物的透皮递送。 Abstract:OBJECTIVE To prepare soluble microneedles loaded with gastrodin, and to investigate their physical and chemical properties and transdermal properties in vitro. METHODS The soluble microneedles loaded with gastrodin were prepared by two-step centrifugation method, and the drug loading was determined by HPLC. Morphology, mechanical properties, skin puncture performance and recovery performance were investigated. The in vitro transdermal properties were investigated by Franz diffusion cell. RESULTS The prepared microneedles had complete array, good flexibility and good mechanical properties. The drug loading of each tablet was up to (5.45±0.14)mg, and the skin could be successfully penetrated. The skin could be restored to its original state within 2 h after the treatment. In vitro skin infiltration results showed that the cumulative osmotic amount of gastrodin in the fully loaded microneedles reached 87% after 12 h, while the cumulative osmotic amount of gastrodin in the gastrodin solution was 12%, indicating that the soluble micro-target gastrodin had a good promoting effect on transdermal delivery of gastrodin. CONCLUSION The soluble microneedles prepared in this study have good mechanical strength and flexibility, and can realize transdermal delivery of water-soluble drugs. -
图 1 空白可溶性微针(A)、天麻素对照品(B)、全载药天麻素可溶性微针(C)HPLC图
Figure 1. HPLC images of blank soluble microneedles (A), gastrodin reference substance (B), and soluble microneedles loaded with gastrodin (C)
图 2 天麻素可溶性微针扫描电镜图
Figure 2. Apparent morphology of soluble microneedles under polarized light microscope
图 3 天麻素全载药可溶性微针压变-应力曲线(n=3)
Figure 3. Pressure variable-stress curve of soluble microneedles loaded with gastrodin (n=3)
图 4 经微针扎过后皮肤台盼蓝染色结果
Figure 4. Images of skin after microneedling and trypan blue staining
图 5 微针刺入大鼠皮肤后的组织切片图(×100)
Figure 5. Tissue section diagram of rat skin after microacupuncture (×100)
图 7 天麻素全载药可溶性微针及其溶液对照的透皮累积渗透曲线(x±s, n=6)
Figure 7. Transdermal accumulative permeation curve of soluble microneedles loaded with gastrodin and their solutions (x±s, n=6)
表 1 天麻素体外透皮数据(n=6)
Table 1. Transdermal data of gastrodin in vitro (n=6)
组别 Q-t方程 r Q12/(μg·cm-2·h-1) Jss/(μg·cm-2·h-1) 天麻素溶液组 Q=1.104 4t+0.195 3 0.966 9 12.10±5.88 1.10 天麻素全载药
可溶性微针组Q=25.493 4t1/2+11.822 0 0.903 1 87.98±9.84 25.49 
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