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火箭启发的泡腾型马达用于口服大分子递药。

Rocket-Inspired Effervescent Motors for Oral Macromolecule Delivery.

机构信息

Department of Rheumatology and Immunology, Nanjing Drum Tower Hospital, School of Biological Science and Medical Engineering, Southeast University, Nanjing, 210096, China.

Shanghai Xuhui Central Hospital, Zhongshan-Xuhui Hospital, and the Shanghai Key Laboratory of Medical Epigenetics, International Co-laboratory of Medical Epigenetics and Metabolism (Ministry of Science and Technology), Institutes of Biomedical Sciences, Fudan University, Shanghai, 200032, China.

出版信息

Adv Mater. 2023 Aug;35(33):e2210679. doi: 10.1002/adma.202210679. Epub 2023 Jul 2.

Abstract

Oral administration is among the most convenient ways with good patient compliance for drug delivery; while it remains a challenge to achieve desirable bioavailability of most macromolecules due to the complex gastrointestinal barriers. Here, inspired by the structure and function of rocket, a novel micromotor delivery system is presented with scaled-down rocket-like architecture and effervescent-tablets-derived fuel for efficient oral macromolecule delivery by penetrating intestinal barrier. These rocket-inspired effervescent motors (RIEMs) are composed of sharp needle tips for both loading cargoes and efficient penetrating, and tail wings for loading effervescent powders and avoiding perforation. When exposed to a water environment, the effervescent fuel generates intensive CO bubbles to propel the RIEMs to move at high speed. Thus, the RIEMs with their sharp tip can inject into the surrounding mucosa for effective drug release. Furthermore, benefiting from their tail-wing design, perforation can be effectively avoided during the injection process, ensuring the safety of the RIEMs in gastrointestinal active delivery. Based on these advantages, it is demonstrated that the RIEMs can efficiently move and stab into the intestinal mucosa for insulin delivery, exhibiting efficacy in regulating blood sugar glucose in a diabetic rabbit model. These features indicate that these RIEMs are versatile and valuable for clinical oral delivery of macromolecules.

摘要

口服给药是最方便的给药方式之一,患者顺应性好;但由于复杂的胃肠道屏障,大多数大分子药物的理想生物利用度仍然难以实现。受火箭结构和功能的启发,本研究提出了一种新型的微马达输送系统,其具有缩小版的火箭样结构和由泡腾片衍生的燃料,可通过穿透肠道屏障来高效递送达药物。这些受火箭启发的泡腾马达(RIEMs)由用于装载货物和高效穿透的锋利针尖以及用于装载泡腾粉末和避免穿孔的尾翼组成。当暴露于水环境时,泡腾燃料会产生密集的 CO 气泡,从而推动 RIEM 以高速移动。因此,RIEMs 可以利用其锋利的尖端注入周围的黏膜,实现有效药物释放。此外,得益于其尾翼设计,在注射过程中可以有效地避免穿孔,确保了 RIEMs 在胃肠道主动递药中的安全性。基于这些优势,研究表明 RIEMs 可有效地移动并刺穿肠道黏膜进行胰岛素递药,在糖尿病兔模型中有效调节血糖。这些特点表明,这些 RIEMs 在大分子的临床口服递送上具有多功能性和应用价值。

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