Li Yanjun, Yang Jingbo, Zheng Ying, Ye Rui, Liu Bin, Huang Yong, Zhou Wei, Jiang Lelun
Guangdong Provincial Key Laboratory of Sensor Technology and Biomedical Instrument, School of Biomedical Engineering, Sun Yat-sen University, Guangzhou, PR China.
Guangdong Medical Devices Quality Surveillance and Test Institute, Guangzhou, PR China.
Acta Biomater. 2021 Feb;121:349-358. doi: 10.1016/j.actbio.2020.12.023. Epub 2020 Dec 16.
A transdermal patch that combines microneedle array (MA) with iontophoresis can achieve synergistic and remarkable enhancement of drug delivery with precise electronic control. However, the development of an MA patch combined with iontophoresis that can enable in situ treatment, easy self-administration, and controllable delivery of liquid macromolecular drugs is still a challenge. Here, we presented an iontophoresis-driven porous MA patch (IDPMAP) for in situ, patient-friendly, and active delivery of charged macromolecular drugs. IDPMAP integrates porous MA with iontophoresis into a single transdermal patch, thus realizing the one-step drug administration strategy of "Penetration, Diffusion, and Iontophoresis." Moreover, a matching portable iontophoresis-driven device was developed for drug self-administration of IDPMAP. In vitro and in vivo studies showed that IDPMAP had approximately 99% skin penetration rate, negligible cytotoxicity, and good biocompatibility without skin irritation and hypersensitivity. In vivo transdermal delivery of insulin in type 1 diabetic rats demonstrated that IDPMAP could effectively deliver insulin nanovesicles and produce a robust hypoglycemic effect on the rats (maintain normal blood glucose for approximately 5.4 h), with more advanced controllability and efficiency than that achieved by pristine MA or iontophoresis. IDPMAP and its portable iontophoresis-driven device are user-friendly and thus show a promising potential for drug self-administration at home.
一种将微针阵列(MA)与离子电渗疗法相结合的透皮贴剂,通过精确的电子控制,可实现协同且显著增强的药物递送。然而,开发一种能实现原位治疗、易于自我给药且能可控递送液体大分子药物的MA与离子电渗疗法相结合的贴剂仍是一项挑战。在此,我们展示了一种用于原位、对患者友好且主动递送带电大分子药物的离子电渗驱动多孔微针阵列贴剂(IDPMAP)。IDPMAP将多孔微针阵列与离子电渗疗法集成到单个透皮贴剂中,从而实现了“渗透、扩散和离子电渗”的一步式给药策略。此外,还开发了一种配套的便携式离子电渗驱动装置,用于IDPMAP的药物自我给药。体外和体内研究表明,IDPMAP的皮肤渗透率约为99%,细胞毒性可忽略不计,且具有良好的生物相容性,无皮肤刺激和过敏反应。在1型糖尿病大鼠体内进行的胰岛素透皮递送实验表明,IDPMAP能够有效递送胰岛素纳米囊泡,并对大鼠产生显著的降血糖作用(使血糖维持正常约5.4小时),其可控性和效率比单纯的微针阵列或离子电渗疗法更高。IDPMAP及其便携式离子电渗驱动装置对用户友好,因此在家中进行药物自我给药方面显示出有前景的潜力。