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混合普朗尼克-聚氧乙烯蓖麻油聚合物胶束作为难溶性抗生素的纳米载体——对抗菌活性的影响

Mixed Pluronic-Cremophor Polymeric Micelles as Nanocarriers for Poorly Soluble Antibiotics-The Influence on the Antibacterial Activity.

作者信息

Tănase Maria Antonia, Raducan Adina, Oancea Petruţa, Diţu Lia Mara, Stan Miruna, Petcu Cristian, Scomoroşcenco Cristina, Ninciuleanu Claudia Mihaela, Nistor Cristina Lavinia, Cinteza Ludmila Otilia

机构信息

Physical Chemistry Department, University of Bucharest, 030018 Bucharest, Romania.

Microbiology Department, Faculty of Biology, University of Bucharest, 60101 Bucharest, Romania.

出版信息

Pharmaceutics. 2021 Mar 24;13(4):435. doi: 10.3390/pharmaceutics13040435.

DOI:10.3390/pharmaceutics13040435
PMID:33804932
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC8063824/
Abstract

In this work, novel polymeric mixed micelles from Pluronic F127 and Cremophor EL were investigated as drug delivery systems for Norfloxacin as model antibiotic drug. The optimal molar ratio of surfactants was determined, in order to decrease critical micellar concentration (CMC) and prepare carriers with minimal surfactant concentrations. The particle size, zeta potential, and encapsulation efficiency were determined for both pure and mixed micelles with selected composition. In vitro release kinetics of Norfloxacin from micelles show that the composition of surfactant mixture generates tunable extended release. The mixed micelles exhibit good biocompatibility against normal fibroblasts MRC-5 cells, while some cytotoxicity was found in all micellar systems at high concentrations. The influence of the surfactant components in the carrier on the antibacterial properties of Norfloxacin was investigated. The drug loaded mixed micellar formulation exhibit good activity against clinical isolated strains, compared with the CLSI recommended standard strains ( ATCC 25923, ATCC 29213, ATCC 27853, ATCC 25922). 5399 clinical strain shows low sensitivity to Norfloxacin in all tested micelle systems. The results suggest that Cremophor EL-Pluronic F127 mixed micelles can be considered as novel controlled release delivery systems for hydrophobic antimicrobial drugs.

摘要

在本研究中，对由普朗尼克F127和聚氧乙烯蓖麻油EL形成的新型聚合物混合胶束作为诺氟沙星（一种模型抗生素药物）的药物递送系统进行了研究。确定了表面活性剂的最佳摩尔比，以降低临界胶束浓度（CMC）并制备具有最低表面活性剂浓度的载体。测定了具有选定组成的纯胶束和混合胶束的粒径、zeta电位和包封率。诺氟沙星从胶束中的体外释放动力学表明，表面活性剂混合物的组成可产生可调节的缓释效果。混合胶束对正常成纤维细胞MRC - 5细胞表现出良好的生物相容性，而在高浓度下，所有胶束系统均发现有一定的细胞毒性。研究了载体中表面活性剂成分对诺氟沙星抗菌性能的影响。与CLSI推荐的标准菌株（ATCC 25923、ATCC 29213、ATCC 2,7853、ATCC 25922）相比，载药混合胶束制剂对临床分离菌株表现出良好的活性。5399临床菌株在所有测试的胶束系统中对诺氟沙星表现出低敏感性。结果表明，聚氧乙烯蓖麻油EL -普朗尼克F127混合胶束可被视为疏水性抗菌药物的新型控释递送系统。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/6532/8063824/b1fb9a45e461/pharmaceutics-13-00435-g010.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/6532/8063824/70e5343c6722/pharmaceutics-13-00435-g001.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/6532/8063824/8829c261d17e/pharmaceutics-13-00435-g002.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/6532/8063824/92add4a37098/pharmaceutics-13-00435-g003.jpg
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https://cdn.ncbi.nlm.nih.gov/pmc/blobs/6532/8063824/37088bf73011/pharmaceutics-13-00435-g005.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/6532/8063824/9aa3fa02971d/pharmaceutics-13-00435-g006a.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/6532/8063824/edd272ea3c1a/pharmaceutics-13-00435-g007a.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/6532/8063824/67b238ba1d1b/pharmaceutics-13-00435-g008.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/6532/8063824/fe9323161e9b/pharmaceutics-13-00435-g009.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/6532/8063824/b1fb9a45e461/pharmaceutics-13-00435-g010.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/6532/8063824/70e5343c6722/pharmaceutics-13-00435-g001.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/6532/8063824/8829c261d17e/pharmaceutics-13-00435-g002.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/6532/8063824/92add4a37098/pharmaceutics-13-00435-g003.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/6532/8063824/4fe2158a2109/pharmaceutics-13-00435-g004.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/6532/8063824/37088bf73011/pharmaceutics-13-00435-g005.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/6532/8063824/9aa3fa02971d/pharmaceutics-13-00435-g006a.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/6532/8063824/edd272ea3c1a/pharmaceutics-13-00435-g007a.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/6532/8063824/67b238ba1d1b/pharmaceutics-13-00435-g008.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/6532/8063824/fe9323161e9b/pharmaceutics-13-00435-g009.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/6532/8063824/b1fb9a45e461/pharmaceutics-13-00435-g010.jpg

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