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一种用于增强抗生素口服递送的聚乙二醇化纳米结构脂质载体。

A PEGylated Nanostructured Lipid Carrier for Enhanced Oral Delivery of Antibiotics.

作者信息

Alavi Seyed Ebrahim, Bakht Urooj, Koohi Moftakhari Esfahani Maedeh, Adelnia Hossein, Abdollahi Seyed Hossein, Ebrahimi Shahmabadi Hasan, Raza Aun

机构信息

Immunology of Infectious Diseases Research Center, Research Institute of Basic Medical Sciences, Rafsanjan University of Medical Sciences, Rafsanjan 7717933777, Iran.

School of Food and Agricultural Sciences, University of Management and Technology, Lahore 54770, Pakistan.

出版信息

Pharmaceutics. 2022 Aug 11;14(8):1668. doi: 10.3390/pharmaceutics14081668.

DOI:10.3390/pharmaceutics14081668
PMID:36015294
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC9415149/
Abstract

Antimicrobial resistance is a major concern for public health throughout the world that severely restricts available treatments. In this context, methicillin-resistant (MRSA) is responsible for a high percentage of infections and mortality. To overcome this challenge, nanoparticles are appropriate tools as drug carriers to improve the therapeutic efficacy and decrease the toxicity of drugs. In this study, a polyethylene glycol (PEG)ylated nanostructured lipid carrier (PEG-NLC) was synthesized to improve the oral delivery of trimethoprim/sulfamethoxazole (TMP/SMZ) for the treatment of MRSA skin infection in vitro and in vivo. The nanoformulation (PEG-TMP/SMZ-NLC) was synthesized with size and drug encapsulation efficiencies of 187 ± 9 nm and 93.3%, respectively, which could release the drugs in a controlled manner at intestinal pH. PEG-TMP/SMZ-NLC was found efficient in decreasing the drugs' toxicity by 2.4-fold in vitro. In addition, the intestinal permeability of TMP/SMZ was enhanced by 54%, and the antibacterial effects of the drugs were enhanced by 8-fold in vitro. The results of the stability study demonstrated that PEG-TMP/SMZ-NLC was stable for three months. In addition, the results demonstrated that PEG-TMP/SMZ-NLC after oral administration could decrease the drugs' side-effects such as renal and hepatic toxicity by ~5-fold in MRSA skin infection in Balb/c mice, while it could improve the antibacterial effects of TMP/SMZ by 3 orders of magnitude. Overall, the results of this study suggest that the application of PEGylated NLC nanoparticles is a promising approach to improving the oral delivery of TMP/SMZ for the treatment of MRSA skin infection.

摘要

抗菌耐药性是全球公共卫生领域的一个主要问题，它严重限制了可用的治疗方法。在这种背景下，耐甲氧西林金黄色葡萄球菌（MRSA）导致了高比例的感染和死亡。为了克服这一挑战，纳米颗粒作为药物载体是合适的工具，可提高治疗效果并降低药物毒性。在本研究中，合成了一种聚乙二醇（PEG）化的纳米结构脂质载体（PEG-NLC），以改善甲氧苄啶/磺胺甲恶唑（TMP/SMZ）的口服给药，用于体外和体内治疗MRSA皮肤感染。该纳米制剂（PEG-TMP/SMZ-NLC）的合成尺寸和药物包封率分别为187±9 nm和93.3%，可在肠道pH值下以可控方式释放药物。发现PEG-TMP/SMZ-NLC在体外可将药物毒性降低2.4倍。此外，TMP/SMZ的肠道通透性提高了54%，药物的抗菌效果在体外提高了8倍。稳定性研究结果表明PEG-TMP/SMZ-NLC在三个月内是稳定的。此外，结果表明，口服PEG-TMP/SMZ-NLC可使Balb/c小鼠MRSA皮肤感染中药物的肾毒性和肝毒性等副作用降低约5倍，同时可将TMP/SMZ的抗菌效果提高3个数量级。总体而言，本研究结果表明，PEG化NLC纳米颗粒的应用是一种有前景的方法，可改善TMP/SMZ的口服给药以治疗MRSA皮肤感染。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/a987/9415149/d0bf03bc529f/pharmaceutics-14-01668-g007.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/a987/9415149/d8e235b4eff8/pharmaceutics-14-01668-g001.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/a987/9415149/f69961992d9f/pharmaceutics-14-01668-g002.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/a987/9415149/c2d10a244315/pharmaceutics-14-01668-g003.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/a987/9415149/8f7274e2e587/pharmaceutics-14-01668-g004.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/a987/9415149/5e492548ecbf/pharmaceutics-14-01668-g005.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/a987/9415149/24c4ee498811/pharmaceutics-14-01668-g006.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/a987/9415149/d0bf03bc529f/pharmaceutics-14-01668-g007.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/a987/9415149/d8e235b4eff8/pharmaceutics-14-01668-g001.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/a987/9415149/f69961992d9f/pharmaceutics-14-01668-g002.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/a987/9415149/c2d10a244315/pharmaceutics-14-01668-g003.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/a987/9415149/8f7274e2e587/pharmaceutics-14-01668-g004.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/a987/9415149/5e492548ecbf/pharmaceutics-14-01668-g005.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/a987/9415149/24c4ee498811/pharmaceutics-14-01668-g006.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/a987/9415149/d0bf03bc529f/pharmaceutics-14-01668-g007.jpg

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