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立体光固化成型技术制备的 3D 打印中空微针阵列用于高效透皮传递利福平。

3D printed hollow microneedles array using stereolithography for efficient transdermal delivery of rifampicin.

机构信息

Department of Pharmaceutics, National Institute of Pharmaceutical Education & Research (NIPER)-Guwahati, Changsari, Assam, India.

Department of Pharmaceutics, National Institute of Pharmaceutical Education & Research (NIPER)-Guwahati, Changsari, Assam, India; National Centre for Pharmacoengineering, NIPER-Guwahati, Changsari, Assam, India.

出版信息

Int J Pharm. 2021 Aug 10;605:120815. doi: 10.1016/j.ijpharm.2021.120815. Epub 2021 Jun 19.

DOI:10.1016/j.ijpharm.2021.120815
PMID:34153441
Abstract

A 3D printed assembly of hollow microneedles (HMNs) array, conjoined with a reservoir void, was designed and additively manufactured using stereolithography (SLA) technology utilizing a proprietary class-I resin. The HMNs array was utilized for transdermal delivery of high molecular weight antibiotics, i.e., rifampicin (M 822.94 g/mol), which suffers from gastric chemical instability, low bioavailability, and severe hepatotoxicity. HMNs morphology was designed with sub-apical holes present in a quarter of the needle tip to improve its mechanical strength and integrity of the HMNs array. The HMNs array was characterized by optical microscopy and electron microscopy to ascertain the print quality and uniformity across the array. The system was also subjected to mechanical characterization for failure and penetration analyses. The ex vivo permeation and consequent transport of rifampicin across porcine skin were systematically evaluated. Finally, in vivo examinations of rifampicin administration through the microneedle reservoir system in SD rats revealed efficient penetration and desired bioavailability.

摘要

设计并采用立体光固化(SLA)技术,利用专有的 I 类树脂添加剂制造了一种带有储腔的中空微针(HMN)阵列的 3D 打印组件。该 HMN 阵列用于经皮输送高分子量抗生素,例如利福平(M 822.94 g/mol),它易受胃酸化学不稳定性、生物利用度低和严重肝毒性的影响。HMN 针尖的四分之一处设计有亚顶点孔,以提高其机械强度和 HMN 阵列的完整性。通过光学显微镜和电子显微镜对 HMN 阵列进行了表征,以确定打印质量和阵列的均匀性。还对该系统进行了机械特性测试,以进行失效和穿透分析。系统地评估了利福平在猪皮上的体外渗透和随后的转运。最后,在 SD 大鼠中通过微针储库系统给予利福平的体内研究表明,其具有高效的穿透性和理想的生物利用度。

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