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Mol Pharm：新型抗菌素纳米悬浮液可同时增强药物的溶解度和抗菌活性

2018-06-30 MedSci MedSci原创

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https://www.ncbi.nlm.nih.gov/pubmed/29953362

本研究旨在配制夫西地酸（FA）的纳米混悬剂（FA-NS）以增强其水溶性和抗菌活性。使用各种体外、计算机和体内技术表征纳米悬浮液。

结果显示，所制备的FA-NS的尺寸、PI和ZP分别为265±2.25nm、0.158±0.026和-16.9±0.794mV。FA和泊洛沙姆188的分子动力学模拟显示，相互作用和结合能分别为-74.42 kJ/mol和-49.764±1.298 kJ/mol，范德华相互作用在自发结合中起主要作用。与裸药相比，纳米混悬剂中FA的溶解度提高了8倍。MTT分析显示细胞活力为75％-100％，证实FA-NS的无毒性。体外抗菌活性显示，与裸FA相比，纳米混悬剂对金黄色葡萄球菌（SA）和耐甲氧西林SA（MRSA）的抗菌活性分别增加16倍和18倍。流式细胞术显示，FA-NS处理的MRSA细胞死亡细菌百分比约为裸药的两倍，尽管MIC降低8倍。皮肤感染的小鼠模型中显示，与裸FA相比，FA-NS处理组的MRSA负荷降低76倍。

综上所述，这些结果表明，抗生素的纳米混悬剂可同时增强药物的溶解度和抗菌活性。

原始出处：

Omolo CA, Kalhapure RS, et al., Formulation and Molecular Dynamics Simulations of a Fusidic Acid Nanosuspension for Simultaneously Enhancing Solubility and Antibacterial activity. Mol Pharm. 2018 Jun 28. doi: 10.1021/acs.molpharmaceut.8b00505.

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    2019-03-27 jj000001

    #Pharm#

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    2018-07-27 xiongke023

    #抗菌素#

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    2018-07-02 ms7899726347904398

    #抗菌#

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    2018-07-01 1201e5c5m39暂无昵称

    学习了

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