Chongqing Key Laboratory of Biochemistry and Molecular Pharmacology, Medicine Engineering Research Center, School of Pharmacy, Chongqing Medical University, Chongqing 400016, PR China.
School of Pharmaceutical Sciences and Yunnan Key Laboratory of Pharmacology for Natural Products, Kunming Medical University, Kunming 650500, PR China.
Carbohydr Polym. 2015 Nov 20;133:31-8. doi: 10.1016/j.carbpol.2015.06.102. Epub 2015 Jul 11.
Self-assembled pectin nanoparticles was prepared and evaluated for delivering the hydrophobic drug, honokiol (HK), to HepG2 cells. These hydrophobic drug-loaded nanoparticles were developed without using any surfactant and organic solvent. Hydroxypropyl-β-cyclodextrin (HCD) was used to fabricate an inclusion complex with HK (HKHCD) to increase the solubility of the drug and thus facilitate its encapsulation and dispersion in the pectin nanoparticles. Investigation of the in vitro release indicated that the drug-loaded nanoparticles exhibited a higher drug release rate than free honokiol and an effective sustained-release. Cytotoxicity, cell apoptosis and cellular uptake studies further confirmed that the pectin nanoparticles with galactose residues generated higher cytotoxicity than free honokiol on HepG2 cells which highly expressed asialoglycoprotein receptors (ASGR). Nevertheless, these findings were not observed in ASGR-negative A549 cells under similar condition. Therefore, pectin nanoparticles demonstrated a specific active targeting ability to ASGR-positive HepG2 cells and could be used as a potential drug carrier for treatment of liver-related tumors.
自组装的果胶纳米粒子被制备并评估用于将疏水性药物，厚朴酚（HK）递送到 HepG2 细胞。这些疏水性药物负载的纳米粒子是在不使用任何表面活性剂和有机溶剂的情况下开发的。羟丙基-β-环糊精（HCD）被用于与 HK 形成包合物（HKHCD）以增加药物的溶解度，从而便于其包封和分散在果胶纳米粒子中。体外释放研究表明，载药纳米粒子表现出比游离厚朴酚更高的药物释放速率和有效的持续释放。细胞毒性、细胞凋亡和细胞摄取研究进一步证实，带有半乳糖残基的果胶纳米粒子在高表达去唾液酸糖蛋白受体（ASGR）的 HepG2 细胞上产生的细胞毒性高于游离厚朴酚。然而，在类似条件下，ASGR 阴性的 A549 细胞中没有观察到这些发现。因此，果胶纳米粒子对 ASGR 阳性 HepG2 细胞表现出特异性的主动靶向能力，可作为治疗肝相关肿瘤的潜在药物载体。
