透皮
曲普瑞林
丝绸
生物医学工程
化学
材料科学
增塑剂
丝素
化学工程
生物相容性
复合材料
药理学
生物化学
医学
促性腺激素释放激素
有机化学
激素
促黄体激素
工程类
作者
Xiaoyan Lu,Yiying Sun,Meishan Han,Daoyuan Chen,Aiping Wang,Kaoxiang Sun
标识
DOI:10.1016/j.ijpharm.2021.121433
摘要
A double-layer silk fibroin microneedles (SF-MNs) was proposed for the transdermal delivery of triptorelin. Two-step pouring and centrifugation were employed to prepare SF-MNs. Triptorelin was wrapped in MNs in the form of microcrystals with a size of ∼1 μm. β-sheet nanocrystals (the secondary structure of silk fibroin) were adjusted in content by methanol-vapor treatment to manipulate the characteristics of SF-MNs prepared with two concentrations of silk fibroin. The mechanical strength of MNs was measured and analyzed in proportion to the β-sheet content. The triptorelin in MNs could be released sustainedly in phosphate-buffered saline for 168 h, and the release amount decreased with increasing β-sheet content. The Ritger–Peppas equation was employed to fit the release data. A linear decreasing relationship was observed between the diffusion coefficient and increased β-sheet content. After administration to rats, SF-MNs exhibited long-term testosterone inhibition and maintained castration levels for ≥7 d. Manipulable mechanical properties and release behavior combined with biocompatibility and biodegradability render SF-MNs as viable long-term transdermal delivery devices for triptorelin.
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