Tian Baocheng, Yan Qi, Wang Juan, Ding Chen, Sai Sixiang
School of Pharmacy, Binzhou Medical University, Yantai.
College of Life and Health Science, Northeastern University, Shenyang, People's Republic of China.
Int J Nanomedicine. 2017 Sep 26;12:7131-7141. doi: 10.2147/IJN.S145695. eCollection 2017.
commonly adheres to implanted medical devices and forms biofilms. Due to the minimal activity of current antifungals against biofilms, new drugs or drug-delivery systems to treat these persistent infections are urgently needed. In the present investigation, voriconazole-loaded nanostructured lipid carriers (Vrc-NLCs) were formulated for enhanced drug-delivery efficiency to to increase the antifungal activity of Vrc and to improve the treatment of infectious diseases. Vrc-NLCs were prepared by a hot-melt, high-pressure homogenization method, and size distribution, ζ-potential, morphology, drug-encapsulation efficiency, drug loading, and physical stability were characterized. The antifungal activity of Vrc-NLCs in vitro was tested during planktonic and biofilm growth in . The mean particle size of the Vrc-NLCs was 45.62±0.53 nm, and they exhibited spheroid-like morphology, smooth surfaces, and ζ-potential of -0.69±0.03 mV. Encapsulation efficiency and drug loading of Vrc-NLCs were 75.37%±2.65% and 3.77%±0.13%, respectively. Physical stability results revealed that despite the low measured ζ-potential, the dispersion of the Vrc-NLCs was stable during their 3-week storage at 4°C. The minimum inhibitory concentration of Vrc-NLCs was identical to that of Vrc. However, the inhibition rate of Vrc-NLCs at lower concentrations was significantly higher than that of Vrc during planktonic growth in in yeast-extract peptone dextrose medium. Surprisingly, Vrc-NLCs treatment reduced cell density in biofilm growth in and induced more switches form hyphal cells to yeast cells compared with Vrc treatment. In conclusion, Vrc-NLCs maintain antifungal activity of Vrc and increase antifungal drug-delivery efficiency to . Therefore, Vrc-NLCs will greatly contribute to the treatment of infectious diseases caused by .
通常会附着在植入式医疗设备上并形成生物膜。由于目前的抗真菌药物对生物膜的活性极小，因此迫切需要新的药物或药物递送系统来治疗这些持续性感染。在本研究中，制备了载伏立康唑的纳米结构脂质载体（Vrc-NLCs），以提高药物递送效率，增强伏立康唑的抗真菌活性并改善传染病的治疗效果。通过热熔高压均质法制备Vrc-NLCs，并对其粒径分布、ζ电位、形态、药物包封率、载药量和物理稳定性进行了表征。在浮游生长和生物膜生长过程中测试了Vrc-NLCs的体外抗真菌活性。Vrc-NLCs的平均粒径为45.62±0.53 nm，呈现类球状形态，表面光滑，ζ电位为-0.69±0.03 mV。Vrc-NLCs的包封率和载药量分别为75.37%±2.65%和3.77%±0.13%。物理稳定性结果表明，尽管测得的ζ电位较低，但Vrc-NLCs在4°C下储存3周期间分散稳定。Vrc-NLCs的最低抑菌浓度与伏立康唑相同。然而，在酵母提取物蛋白胨葡萄糖培养基中浮游生长期间，较低浓度下Vrc-NLCs的抑菌率明显高于伏立康唑。令人惊讶的是，与伏立康唑治疗相比，Vrc-NLCs治疗降低了生物膜生长中的细胞密度，并诱导更多的菌丝细胞转变为酵母细胞。总之，Vrc-NLCs保持了伏立康唑的抗真菌活性并提高了抗真菌药物递送效率。因此，Vrc-NLCs将对由……引起的传染病的治疗做出巨大贡献。
