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锌微火箭药丸:用于活性口服递送的制备与表征

Zinc Microrocket Pills: Fabrication and Characterization toward Active Oral Delivery.

作者信息

Mundaca-Uribe Rodolfo, Esteban-Fernández de Ávila Berta, Holay Maya, Lekshmy Venugopalan Pooyath, Nguyen Bryan, Zhou Jiarong, Abbas Amal, Fang Ronnie H, Zhang Liangfang, Wang Joseph

机构信息

Department of Nanoengineering, Chemical Engineering Program, University of California San Diego, La Jolla, CA, 92093, USA.

出版信息

Adv Healthc Mater. 2020 Sep;9(18):e2000900. doi: 10.1002/adhm.202000900. Epub 2020 Aug 2.

Abstract

Here the fabrication of a zinc (Zn) microrocket pill is reported, and its unique features toward active and enhanced oral delivery application are demonstrated. By loading Zn-based tubular microrockets into an orally administrable pill formulation, the resulting Zn microrocket pill can rapidly dissolve in the stomach, releasing numerous encapsulated Zn microrockets that are instantaneously activated and then propel in the gastric fluid. The released Zn microrockets display efficient propulsion without being affected by the presence of the inactive excipient materials of the pill. An in vivo retention study performed in mice clearly shows that the active pill dissolution and powerful acid-driven Zn microrocket propulsion greatly enhance the microrocket retention within the gastric tissue without causing toxic effects. By combining the active delivery feature of Zn microrockets with the oral administration of a pill, the Zn microrocket pill holds considerable potential for active oral delivery of various therapeutics for diverse medical applications.

摘要

本文报道了一种锌(Zn)微火箭药丸的制备,并展示了其在主动和增强口服给药应用方面的独特特性。通过将锌基管状微火箭装载到可口服的药丸制剂中,所得的锌微火箭药丸可在胃中迅速溶解,释放出大量封装的锌微火箭,这些微火箭会立即被激活,然后在胃液中推进。释放出的锌微火箭显示出高效的推进能力,不受药丸中惰性辅料的影响。在小鼠身上进行的体内滞留研究清楚地表明,药丸的主动溶解和强大的酸驱动锌微火箭推进极大地增强了微火箭在胃组织中的滞留,且不会产生毒性作用。通过将锌微火箭的主动递送特性与药丸的口服给药相结合,锌微火箭药丸在为各种医学应用主动口服递送多种治疗药物方面具有巨大潜力。

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