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用于耐甲氧西林靶向治疗的叶酸功能化脂质纳米颗粒

Folate Functionalized Lipid Nanoparticles for Targeted Therapy of Methicillin-Resistant .

作者信息

Vanamala Kushal, Bhise Ketki, Sanchez Hiram, Kebriaei Razieh, Luong Duy, Sau Samaresh, Abdelhady Hosam, Rybak Michael J, Andes David, Iyer Arun K

机构信息

Use-Inspired Biomaterials & Integrated Nano Delivery (U-BiND) Systems Laboratory, Department of Pharmaceutical Sciences, Eugene Applebaum College of Pharmacy and Health Sciences, Wayne State University, Detroit, MI 48201, USA.

Division of Infectious Disease, Department of Medicine, University of Wisconsin-Madison, Madison, WI 53706, USA.

出版信息

Pharmaceutics. 2021 Oct 26;13(11):1791. doi: 10.3390/pharmaceutics13111791.

Abstract

Methicillin-resistant (MRSA), commonly called a superbug, is a highly alarming antibiotic-resistant population of bacteria. Vancomycin (VAN) was first approved by the FDA in 1988, and it is still regarded as the treatment of choice for MRSA. The efficacy of VAN treatment has become less effective due to the development of VAN resistance in MRSA and the potential for nephrotoxicity. This study aims to improve the efficacy of VAN treatment by identifying the folate receptor for MRSA infected tissues and developing folate decorated lipid nanoparticles containing VAN (LVAN). In comparison to conventional VAN, LVAN showed a higher bactericidal effect and a superior ability to inhibit biofilm in MRSA with an enhanced accumulation in MRSA infected thigh tissues and a reduced accumulation in kidney. The results suggested that LVAN is a promising candidate to overcome the current limitations of bacterial resistance and adverse side effects in kidneys found in VAN.

摘要

耐甲氧西林金黄色葡萄球菌(MRSA),通常被称为超级细菌,是一种极具警示性的耐抗生素细菌群体。万古霉素(VAN)于1988年首次获得美国食品药品监督管理局(FDA)批准,至今仍被视为治疗MRSA的首选药物。由于MRSA中出现了对万古霉素的耐药性以及存在肾毒性的可能性,万古霉素治疗的疗效已有所下降。本研究旨在通过鉴定MRSA感染组织的叶酸受体并开发含有万古霉素的叶酸修饰脂质纳米颗粒(LVAN)来提高万古霉素治疗的疗效。与传统万古霉素相比,LVAN在MRSA中表现出更高的杀菌效果和更强的抑制生物膜能力,在MRSA感染的大腿组织中积累增加,而在肾脏中的积累减少。结果表明,LVAN有望克服目前万古霉素存在的细菌耐药性和肾脏不良副作用的局限性。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/57c7/8617750/814a3d8442ab/pharmaceutics-13-01791-g001.jpg

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