Harris T L, Wenthur C J, Diego-Taboada A, Mackenzie G, Corbitt T S, Janda K D
Department of Chemistry, The Scripps Research Institute, 10550 North Torrey Pines Road, La Jolla, California 92037, USA.
Department of Chemistry, University of Hull, Cottingham Road, Hull HU6 7RX, England and Sporomex Limited, Medina House, 2 Station Avenue, Bridlington, East Yorkshire Y016 4LZ, England.
Chem Commun (Camb). 2016 Mar 18;52(22):4187-90. doi: 10.1039/c6cc00615a.
3,4-Diaminopyridine has shown promise in reversing botulinum intoxication, but poor pharmacokinetics and a narrow therapeutic window limit its clinical utility. Thus, we developed a pH-dependent oral delivery platform using club moss spore exines. These exine microcapsules slowed 3,4-diaminopyridine absorption, limited its seizure activity, and enabled delivery of doses which prolonged mouse survival after botulism neurotoxin A intoxication.
3,4-二氨基吡啶已显示出在逆转肉毒杆菌中毒方面的前景，但较差的药代动力学和狭窄的治疗窗限制了其临床应用。因此，我们利用石松孢子外壁开发了一种pH依赖性口服给药平台。这些外壁微胶囊减缓了3,4-二氨基吡啶的吸收，限制了其惊厥活性，并能够递送延长肉毒杆菌神经毒素A中毒小鼠存活时间的剂量。
