Nanovex Biotechnologies S.L., Parque Tecnológico de Asturias Edificio CEEI, 33428 Llanera, Spain.
Departamento de Química Orgánica e Inorgánica, Instituto Universitario de Química Organometálica "Enrique Moles", Universidad de Oviedo, Julián Clavería 8, 33006 Oviedo, Spain.
Dalton Trans. 2024 Sep 18;53(36):15205-15214. doi: 10.1039/d4dt01867b.
A novel lipoformulation was developed by encapsulating cationic (S^C)-cyclometallated gold(III) complex [Au(dppta)(NPy-PZ-dtc)] (AuPyPZ) in liposomes. The liposomal form of compound AuPyPZ has a bactericidal action similar to that of the free drug without any appreciable effect on the viability of mammalian cells. Furthermore, the nanoformulation reduces metalloantibiotic-induced inhibition of hERG and the inhibition of cytochromes, significantly decreasing the potential liabilities of the metallodrug. The obtained metalloantibiotic liposomal formulation shows high stability and suitable properties for drug delivery, representing an effective strategy to fight against drug-resistant bacteria.
一种新型的脂质体制剂通过将阳离子（S^C）-环金属化金（III）配合物 [Au(dppta)(NPy-PZ-dtc)]（AuPyPZ）包封在脂质体中来制备。化合物 AuPyPZ 的脂质体形式具有类似于游离药物的杀菌作用，而对哺乳动物细胞的活力没有任何明显影响。此外，纳米制剂减少了金属抗生素诱导的 hERG 抑制和细胞色素抑制，显著降低了金属药物的潜在毒性。所得的金属抗生素脂质体制剂表现出高稳定性和适合药物传递的特性，代表了对抗耐药菌的有效策略。
