College of Pharmacy, Liaoning Medical University, Jinzhou 121000, China.
Biomed Res Int. 2013;2013:236469. doi: 10.1155/2013/236469. Epub 2013 Mar 18.
To prepare biocompatible ciprofloxacin-loaded carboxymethyl chitosan nanoparticles (CCC NPs) and evaluate their cell specificity as well as antibacterial activity against Escherichia coli in vitro.
CCC NPs were prepared by ionic cross-linking method and optimized by using Box-Behnken response surface method (BBRSM). Zeta potential, drug encapsulation, and release of the obtained nanoparticles in vitro were thoroughly investigated. Minimum inhibitory concentration (MIC) and killing profiles of free or ciprofloxacin-loaded nanoparticles against Escherichia coli were documented. The cytotocity of blank nanoparticles and cellular uptake of CCC NPs were also investigated.
The obtained particles were monodisperse nanospheres with an average hydrated diameter of 151 ± 5.67 nm and surface of charge -22.9 ± 2.21 mV. The MICs of free ciprofloxacin and CCC NPs were 0.16 and 0.08 μg/mL, respectively. Blank nanoparticles showed no obvious cell inhibition within 24 h, and noticeable phagocytosis effect was observed in the presence of CCC NPs.
This study shows that CCC NPs have stronger antibacterial activity against Escherichia coli than the free ciprofloxacin because they can easily be uptaken by cells. The obtained CCC NPs have promising prospect in drug delivery field.
制备具有生物相容性的载环丙沙星羧甲基壳聚糖纳米粒(CCC NPs),并评价其体外对大肠杆菌的细胞特异性和抗菌活性。
采用离子交联法制备 CCC NPs,并采用 Box-Behnken 响应面法(BBRSM)进行优化。体外研究了所得纳米粒的 Zeta 电位、药物包封率和释放情况。记录游离或载环丙沙星纳米粒对大肠杆菌的最小抑菌浓度(MIC)和杀菌曲线。还研究了空白纳米粒的细胞毒性和 CCC NPs 的细胞摄取情况。
所得颗粒为单分散纳米球,平均水合粒径为 151±5.67nm,表面电荷为-22.9±2.21mV。游离环丙沙星和 CCC NPs 的 MIC 分别为 0.16 和 0.08μg/ml。空白纳米粒在 24 小时内对细胞无明显抑制作用,而在 CCC NPs 存在下观察到明显的吞噬作用。
本研究表明,与游离环丙沙星相比,载环丙沙星的 CCC NPs 对大肠杆菌具有更强的抗菌活性,因为它们容易被细胞摄取。所得到的 CCC NPs 在药物传递领域具有广阔的应用前景。