Department of Drug Sciences, University of Pavia, Via Taramelli 12, 27100 Pavia, Italy.
Int J Mol Sci. 2021 Jan 17;22(2):891. doi: 10.3390/ijms22020891.
The aim of this work was the development of microstructured lipid carriers (MLC) based on chitosan (CH) and containing N-acetylcysteine (NAC), a mucolytic and antioxidant agent, to inhibit the formation of biofilm. MLC were prepared using the high shear homogenization technique. The MLC were characterized for morphology, particle size, Z potential, encapsulation efficiency and drug release. The antioxidant properties of NAC-loaded microstructured carriers were evaluated through an in vitro spectrophotometer assay. Finally, the activity of NAC-CH-MLC on biofilm production by was also evaluated. Results obtained from this study highlighted that the use of chitosan into the inner aqueous phase permitted to obtain microstructured particles with a narrow size range and with good encapsulation efficiency. NAC-loaded MLC showed higher antioxidant activity than the free molecule, demonstrating how encapsulation increases the antioxidant effect of the molecule. Furthermore, the reduction of biofilm growth resulted extremely high with MLC being 64.74% ± 6.2% and 83.74% ± 9.95%, respectively, at 0.5 mg/mL and 2 mg/mL. In conclusion, this work represents a favorable technological strategy against diseases in which bacterial biofilm is relevant, such as cystic fibrosis.
本工作的目的是开发基于壳聚糖（CH）的结构化脂质载体（MLC），并包含粘蛋白溶解剂和抗氧化剂 N-乙酰半胱氨酸（NAC），以抑制生物膜的形成。MLC 是使用高剪切匀浆技术制备的。对 MLC 的形态、粒径、Z 电位、包封效率和药物释放进行了表征。通过体外分光光度计测定法评估了负载 NAC 的结构化载体的抗氧化特性。最后，还评估了 NAC-CH-MLC 对生物膜生成的活性。本研究结果表明，在水相内部使用壳聚糖可以获得具有较窄粒径范围和良好包封效率的结构化颗粒。负载 NAC 的 MLC 表现出比游离分子更高的抗氧化活性，表明包封增加了分子的抗氧化作用。此外，当浓度分别为 0.5mg/mL 和 2mg/mL 时，MLC 对生物膜生长的抑制率极高，分别为 64.74%±6.2%和 83.74%±9.95%。总之，这项工作代表了一种针对与细菌生物膜相关的疾病（如囊性纤维化）的有利技术策略。
