The Indonesian Food and Drug Authority, Jakarta 10560, Indonesia.
Department of Chemistry, Faculty of Mathematics and Natural Science, Universitas Indonesia, Depok 16424, Indonesia; The Indonesian Food and Drug Authority, Jakarta 10560, Indonesia.
J Pharm Sci. 2023 Dec;112(12):3164-3174. doi: 10.1016/j.xphs.2023.07.021. Epub 2023 Jul 27.
The encapsulation efficiency and the loading capacity of azithromycin (AZI) were succesfully enhanced by modifying chitosan nanoparticle (NCh) with Anredera cordifolia leaf extract (ACLE), as demonstrated in this study. The prominent secondary metabolites in ACLE could establish a new chemical bonds with NCh's amino groups and partly improved the hydrophobicity of NCh, which leads to excellent AZI encapsulation efficiency and loading capacity of 95.24 ± 1.30% and 55.74 ± 1.03%, respectively. TEM characterization demonstrated that the AZI-loaded ACLE-NCh nanoparticles were uniformly distributed with a particle size of 24.6 ± 2.9 nm. According to the result of in vitro drug release studies, AZI-loaded ACLE-NCh releases 1.12 ± 0.33% at a pH of 1.6 for 2 h, 82.05 ± 2.26% at a pH of 6.8 for 6 h, and 93.44 ± 1.94% at a pH of 7.4 for 24 h. It is remarkable that the encapsulation activityu of AZI-loaded ACLE-NCh is more effective due to the better interaction between NCh and AZI resulting from the increased hydrophobicity of modified NCh. Moreover, this work provides novel findings on the significant contribution of NCh modified by plant extracts, which has the potential as a carrier for azithromycin.
本研究成功地通过修饰壳聚糖纳米颗粒（NCh）用安德列德叶提取物（ACLE）来提高阿奇霉素（AZI）的包封效率和载药量。ACLE 中的突出次生代谢物可以与 NCh 的氨基建立新的化学键，并在一定程度上提高 NCh 的疏水性，从而使 AZI 的包封效率和载药量分别达到 95.24 ± 1.30%和 55.74 ± 1.03%。TEM 表征表明，载有 AZI 的 ACLE-NCh 纳米粒子均匀分布，粒径为 24.6 ± 2.9nm。根据体外药物释放研究的结果，载有 AZI 的 ACLE-NCh 在 pH 值为 1.6 时在 2 小时内释放 1.12 ± 0.33%，在 pH 值为 6.8 时在 6 小时内释放 82.05 ± 2.26%，在 pH 值为 7.4 时在 24 小时内释放 93.44 ± 1.94%。值得注意的是，由于修饰后的 NCh 疏水性增加，NCh 和 AZI 之间的相互作用增强，载有 AZI 的 ACLE-NCh 的包封活性更加有效。此外，这项工作为植物提取物修饰的 NCh 的重要贡献提供了新的发现，为阿奇霉素的载体提供了新的思路。
