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Triclosan-loaded pH-responsive copolymer to target bacteria and to have long bacteriostatic efficacy.
European Journal of Pharmaceutical Sciences ( IF 4.3 ) Pub Date : 2020-03-31 , DOI: 10.1016/j.ejps.2020.105320
Dongqin Lei 1 , Quan Wang 1 , Yue Kong 1 , Yuanwei Chen 1 , Xianglin Luo 2
Affiliation  

It is important to reduce side effects and to explore novel usage for hydrophobic broad-spectrum antibacterial agent triclosan (TCS). In this study, a new amphiphilic copolymer with tertiary amine groups, monomethyl ether poly(ethylene glycol)-b-poly{α-[4-(diethylamino)methyl-1,2,3-triazol]-caprolactone-co-caprolactone} (mPEG-PDCL) was designed and synthesized, and its micelles were applied as carries of TCS to enhance antimicrobial and bacteriostatic action. mPEG-PDCL and its contrastive copolymer mPEG-PCL could form uniform spherical micelles with sizes 50-110 nm. The zeta potential of mPEG-PDCL micelles was positive and changed from 7.00 ± 0.67 mV at pH 7.5 to 24.67 ± 1.23 mV at pH 5.5. Both TCS-loaded micelles displayed quite high drug loading content (approx. 15%) and drug loading efficiency (more than 85%). In comparison with pH 7.4, TCS released faster in acidic environment which was induced by bacteria metabolism. MIC values of both TCS-loaded micelles against S. aureus and E. coli were as low as free TCS. TCS-loaded micelles showed much better antibacterial activity than free TCS, especially, mPEG-PDCL/TCS micelles displayed long bacteriostatic efficacy in 60 h against S. aureus and in 54 h against E. coli. mPEG-PDCL micelles preferred targeting to both S. aureus and E. coli due to positive zeta potential. In in vivo experiment, the purulence of the infected wound almost disappeared for SD rats treated with mPEG-PDCL/TCS micelles. Therefore, mPEG-PDCL micelles may be used as good carriers for antimicrobial agents, and the TCS-loaded micelles possess long antimicrobial/bacteriostatic efficacy.

中文翻译:

三氯生负载的pH响应共聚物可靶向细菌并具有长期抑菌效果。

重要的是减少副作用并探索疏水性广谱抗菌剂三氯生(TCS)的新用途。在这项研究中,一种新型的具有叔胺基的两亲共聚物,单甲醚聚(乙二醇)-b-聚{α-[4-(二乙氨基)甲基-1,2,3-三唑]-己内酯-共己内酯}设计并合成了mPEG-PDCL(mPEG-PDCL),并以其胶束作为TCS的载体,以增强抗菌和抑菌作用。mPEG-PDCL及其对比共聚物mPEG-PCL可以形成大小为50-110 nm的均匀球形胶束。mPEG-PDCL胶束的ζ电位为正,从pH 7.5的7.00±0.67 mV变为pH 5.5的24.67±1.23 mV。两种TCS负载的胶束均显示出很高的载药量(约15%)和载药效率(超过85%)。与pH 7.4相比,TCS在酸性环境中释放较快,这是细菌代谢引起的。TCS负载的胶束对金黄色葡萄球菌和大肠杆菌的MIC值都与游离TCS一样低。载有TCS的胶束比游离的TCS表现出更好的抗菌活性,尤其是mPEG-PDCL / TCS胶束在60小时内对金黄色葡萄球菌和54小时内对大肠杆菌具有很长的抑菌效力。由于正的ζ电势,mPEG-PDCL胶束优选同时靶向金黄色葡萄球菌和大肠杆菌。在体内实验中,对于用mPEG-PDCL / TCS胶束处理的SD大鼠,感染伤口的脓性几乎消失了。因此,mPEG-PDCL胶束可以用作抗菌剂的良好载体,而载有TCS的胶束具有长的抗菌/抑菌功效。TCS负载的胶束对金黄色葡萄球菌和大肠杆菌的MIC值都与游离TCS一样低。载有TCS的胶束比游离的TCS表现出更好的抗菌活性,尤其是mPEG-PDCL / TCS胶束在60小时内对金黄色葡萄球菌和54小时内对大肠杆菌具有很长的抑菌效力。由于正电动势,mPEG-PDCL胶束优选同时靶向金黄色葡萄球菌和大肠杆菌。在体内实验中,对于用mPEG-PDCL / TCS胶束处理的SD大鼠,感染伤口的脓性几乎消失了。因此,mPEG-PDCL胶束可以用作抗菌剂的良好载体,而载有TCS的胶束具有长的抗菌/抑菌功效。TCS负载的胶束对金黄色葡萄球菌和大肠杆菌的MIC值都与游离TCS一样低。载有TCS的胶束比游离的TCS表现出更好的抗菌活性,尤其是mPEG-PDCL / TCS胶束在60小时内对金黄色葡萄球菌和54小时内对大肠杆菌具有很长的抑菌效力。由于正的ζ电势,mPEG-PDCL胶束优选同时靶向金黄色葡萄球菌和大肠杆菌。在体内实验中,对于用mPEG-PDCL / TCS胶束处理的SD大鼠,感染伤口的脓性几乎消失了。因此,mPEG-PDCL胶束可以用作抗菌剂的良好载体,而载有TCS的胶束具有长的抗菌/抑菌功效。特别是,mPEG-PDCL / TCS胶束在60小时内对金黄色葡萄球菌和54小时内对大肠杆菌表现出长抑菌功效。由于正的ζ电势,mPEG-PDCL胶束优选同时靶向金黄色葡萄球菌和大肠杆菌。在体内实验中,对于用mPEG-PDCL / TCS胶束处理的SD大鼠,感染伤口的脓性几乎消失了。因此,mPEG-PDCL胶束可以用作抗菌剂的良好载体,而载有TCS的胶束具有长的抗菌/抑菌功效。特别是,mPEG-PDCL / TCS胶束在60小时内对金黄色葡萄球菌和54小时内对大肠杆菌表现出长抑菌功效。由于正的ζ电势,mPEG-PDCL胶束优选同时靶向金黄色葡萄球菌和大肠杆菌。在体内实验中,对于用mPEG-PDCL / TCS胶束处理的SD大鼠,感染伤口的脓性几乎消失了。因此,mPEG-PDCL胶束可以用作抗菌剂的良好载体,而载有TCS的胶束具有长的抗菌/抑菌功效。对于用mPEG-PDCL / TCS胶束处理的SD大鼠,感染伤口的脓性几乎消失了。因此,mPEG-PDCL胶束可以用作抗菌剂的良好载体,而载有TCS的胶束具有长的抗菌/抑菌功效。对于用mPEG-PDCL / TCS胶束处理的SD大鼠,感染伤口的脓性几乎消失了。因此,mPEG-PDCL胶束可以用作抗菌剂的良好载体,而载有TCS的胶束具有长的抗菌/抑菌功效。
更新日期:2020-03-31
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