College of Pharmacy and Institute of Drug Research and Development, Chungnam National University, 99 Daehak-Ro, Yuseong-Gu, Daejeon 34134, Republic of Korea.
Division of Pharmaceutical Sciences, Faculty of Pharmacy, Thammasat University, Rangsit Center, Pathumthani 12120, Thailand.
Carbohydr Polym. 2017 Mar 1;159:39-47. doi: 10.1016/j.carbpol.2016.12.009. Epub 2016 Dec 7.
To improve the solubility and anticancer activity of albendazole (ABZ), chitosan (CS)-coated poly-dl-lactic-co-glycolic acid (PLGA) nanoparticles were developed. CS was used to coat ABZ-loaded PLGA nanoparticles to enhance both mucoadhesiveness and colloidal stability. CS-coated PLGA nanoparticles were prepared by suspending the nanoparticles in CS solution after solvent diffusion. The CS-coated PLGA nanoparticles were characterized, and ABZ release was studied in vitro from various formulations. The mucoadhesive properties and in vitro anticancer activities of CS-coated PLGA nanoparticles were investigated by measurement of zeta potentials and the MTT assay, respectively. Spherical nanoparticles below 500nm in diameter were successfully prepared; the particle size distribution was narrow. Complete encapsulation of ABZ in CS-coated PLGA nanoparticles was confirmed by SEM, FTIR, DSC, and XRD. The particle sizes of CS-coated PLGA nanoparticles were in the range of 260-480nm; the encapsulation efficiency was 43.4-54.6%; and the yield 58.5-67.8%. The zeta potential of CS-coated nanoparticles was above +27mV and stability was maintained for 4 weeks. At pH 7.4, the in vitro release of ABZ from nanoparticles (P188-5) was 200-fold higher than that from untreated ABZ; this persisted for 12h. Moreover, ABZ release from CS-coated PLGA nanoparticles (P188-CS0.5) was 1.5-fold higher than that from untreated ABZ at pH 1.2. Additionally, the ABZ-loaded CS-coated nanoparticles exhibited superior mucoadhesion and improved cytotoxicity. The results show that CS coating of PLGA nanoparticles may improve the anticancer effect and the mucoadhesive properties of ABZ-loaded nanoparticles.
为了提高阿苯达唑(ABZ)的溶解度和抗癌活性,开发了壳聚糖(CS)包覆的聚(DL-丙交酯-共-乙交酯)(PLGA)纳米粒。CS 用于包覆 ABZ 载 PLGA 纳米粒,以增强粘膜粘附性和胶体稳定性。CS 包覆的 PLGA 纳米粒是通过将纳米粒悬浮在 CS 溶液中后进行溶剂扩散而制备的。对 CS 包覆的 PLGA 纳米粒进行了表征,并研究了不同制剂中 ABZ 的体外释放情况。通过测量 Zeta 电位和 MTT 测定法,研究了 CS 包覆的 PLGA 纳米粒的粘膜粘附性能和体外抗癌活性。成功制备了直径小于 500nm 的球形纳米粒,粒径分布较窄。SEM、FTIR、DSC 和 XRD 证实了 ABZ 完全包封在 CS 包覆的 PLGA 纳米粒中。CS 包覆的 PLGA 纳米粒的粒径在 260-480nm 之间;包封效率为 43.4-54.6%;产率为 58.5-67.8%。CS 包覆纳米粒的 Zeta 电位高于+27mV,且在 4 周内保持稳定。在 pH7.4 时,纳米粒(P188-5)中 ABZ 的体外释放量是未处理 ABZ 的 200 倍,持续 12h。此外,在 pH1.2 时,CS 包覆的 PLGA 纳米粒(P188-CS0.5)中 ABZ 的释放量比未处理的 ABZ 高 1.5 倍。此外,载 ABZ 的 CS 包覆纳米粒表现出更好的粘膜粘附性和提高的细胞毒性。结果表明,PLGA 纳米粒的 CS 包覆可能提高 ABZ 载纳米粒的抗癌效果和粘膜粘附性。