Ye Rui, Yang Jingbo, Li Yanjun, Zheng Ying, Yang Jian, Li Yuanyuan, Liu Bin, Jiang Lelun
Guangdong Provincial Key Laboratory of Sensor Technology and Biomedical Instrument, School of Biomedical Engineering, Sun Yat-Sen University, No. 135, Xingang Xi Road, Guangzhou 510275, P. R. China.
ACS Biomater Sci Eng. 2020 Apr 13;6(4):2487-2494. doi: 10.1021/acsbiomaterials.0c00120. Epub 2020 Mar 20.
We developed a modified micromolding method for the mass production of a novel tip-hollow microneedle array (MA). The tip-hollow MA was fabricated by tuning of the vacuum degree at -80 kPa for 60 s during the micromolding process. Subsequently, a tip-dissolvable MA encapsulated with drugs in the microcraters was fabricated from tip-hollow MA using repeated dipping and the freeze-drying process. Both the tip-hollow and tip-dissolvable MAs could easily penetrate in the rabbit skin without breakage, while the tip-hollow MA can just create a shallow loop hole in the skin. The drug-loaded tip-dissolvable MA can rapidly dissolve, releasing and diffusing the drug in the skin. The tip-dissolvable MA exhibited the best drug permeation ability in that the corresponding flux through the punctured skin using tip-dissolvable MA loaded with Rhodamine B is about 1.7- and 5.8-fold of that through the punctured skin using solid MA and the intact skin, respectively. The tip-dissolvable MA loaded with 5 IU insulin was fabricated to treat the type 1 diabetic SD rats. The tip-dissolvable MA had a good hypoglycemic effect and exhibited longer normoglycemic period in comparison with subcutaneous injection (5 IU). Therefore, our tip-dissolve MA is a promising medical device for transdermal drug delivery.
我们开发了一种改进的微成型方法,用于大规模生产新型尖端中空微针阵列(MA)。在微成型过程中,通过将真空度调节至-80 kPa并保持60秒来制造尖端中空MA。随后,使用反复浸渍和冷冻干燥工艺,由尖端中空MA制备了在微凹坑中封装有药物的尖端可溶解MA。尖端中空MA和尖端可溶解MA都能轻松穿透兔皮而不破损,而尖端中空MA只会在皮肤中形成一个浅环形孔。载药的尖端可溶解MA能迅速溶解,使药物在皮肤中释放和扩散。尖端可溶解MA表现出最佳的药物渗透能力,因为使用负载罗丹明B的尖端可溶解MA穿过刺破皮肤的相应通量分别约为使用实心MA穿过刺破皮肤和完整皮肤通量的1.7倍和5.8倍。制备了负载5 IU胰岛素的尖端可溶解MA来治疗1型糖尿病SD大鼠。与皮下注射(5 IU)相比,尖端可溶解MA具有良好的降血糖效果,且血糖正常期更长。因此,我们的尖端可溶解MA是一种很有前景的经皮给药医疗装置。
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