Platensimycin-Encapsulated Liposomes or Micelles as Biosafe Nanoantibiotics Exhibited Strong Antibacterial Activities against Methicillin-Resistant Staphylococcus aureus Infection in Mice.,Molecular Pharmaceutics

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Platensimycin-Encapsulated Liposomes or Micelles as Biosafe Nanoantibiotics Exhibited Strong Antibacterial Activities against Methicillin-Resistant Staphylococcus aureus Infection in Mice.
Molecular Pharmaceutics ( IF 4.5 ) Pub Date : 2020-06-10 , DOI: 10.1021/acs.molpharmaceut.0c00194
Zhe Wang ₁ , Xingyun Liu ₁ , Ying Peng ₂ , Meng Su ₁ , Saibin Zhu ₁ , Jian Pan ₁ , Ben Shen , Yanwen Duan _{1,

3,

4} , Yong Huang _{1,

4}

Affiliation

Platensimycin (PTM) is a promising natural product drug lead against Gram-positive bacteria, including methicillin-resistant Staphylococcus aureus (MRSA), while the clinical development was hampered by problems related to its poor solubility and pharmacokinetic properties. In this study, we used liposomes and micelles as carriers of PTM to prepare PTM nanoformulations for the treatment of MRSA infection in mice. PTM-loaded nanoparticles could effectively reduce residual bacteria in the MRSA-infected macrophage cell model, comparing to free PTM. More importantly, in vivo studies showed that encapsulation of PTM by liposomes or micelles effectively improved the pharmacokinetic properties of PTM in Sprague–Dawley rats and the survival rate of MRSA-infected C57BL/6J mice. Our study has thus suggested that the clinically used nanocarriers, such as liposome and micelle, might also be useful to improve the efficacy of other natural product drug leads to accelerate their in vivo evaluation and preclinical development.

中文翻译：

作为生物安全的纳米抗生素，用铂霉素包裹的脂质体或胶束对小鼠的耐甲氧西林金黄色葡萄球菌感染表现出强大的抗菌活性。

Platensimycin（PTM）是对抗革兰氏阳性细菌（包括耐甲氧西林的金黄色葡萄球菌（MRSA））的有前途的天然产物药物，同时其溶解性和药代动力学性质较差的问题也阻碍了临床发展。在这项研究中，我们使用脂质体和胶束作为PTM的载体来制备PTM纳米制剂，以治疗小鼠的MRSA感染。与游离PTM相比，装载PTM的纳米颗粒可以有效减少MRSA感染的巨噬细胞模型中的残留细菌。更重要的是，体内研究表明，脂质体或胶束包裹PTM可有效改善Sprague-Dawley大鼠体内PTM的药代动力学特性，并改善MRSA感染的C57BL / 6J小鼠的存活率。因此，我们的研究表明，临床上使用的纳米载体，例如脂质体和胶束，也可能有助于提高其他天然产物药物的功效，从而加速其体内评估和临床前开发。

更新日期：2020-07-06

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