Jinzhou Medical University, Jinzhou, 121001, People's Republic of China.
Jinzhou Medical University, Jinzhou, 121001, People's Republic of China.
Colloids Surf B Biointerfaces. 2018 May 1;165:278-285. doi: 10.1016/j.colsurfb.2018.02.052. Epub 2018 Feb 24.
N-(2-(3-fluorobenzyl)-2H-indazol-5-yl)-2-phenyl-2H-pyrazolo[4,3-c]qui- nolin-4-amine (LZC-2b) with a quinoline structure was synthesized as an anticancer prodrug. The pH sensitive anticancer drugs obtained by a simple hydrothermal method. The interaction of chitosan (Cts) and LZC-2b is used to complete the encapsulation without any cross-linking. The obtained micromedicine (LZC-2b@Cts-MSs) has an average size of ∼980 nm. The drug loading efficiency (DLE) of LZC-2b@Cts-MSs was about 79%. In addition, drug release from LZC-2b@Cts-MSs was pH depended. At pH = 7.4, only 5.1% of loaded LZC-2b was released, while 90.3% of loaded LZC-2b was released at pH = 5.0. Cell culture results indicate that LZC-2b@Cts-MSs can be easily uptaken by KB cells. Cell viability results show that KB cells can be effectively killed by LZC-2b@Cts-MSs. Our strategy of synthesis and preparation of pH responsive LZC-2b@Cts-MSs has promising prospect in chemotherapy of oral cancer.
N-(2-(3-氟苄基)-2H-吲唑-5-基)-2-苯基-2H-吡唑并[4,3-c]喹啉-4-胺（LZC-2b）具有喹啉结构，被合成作为一种抗癌前药。通过简单的水热法获得了 pH 敏感的抗癌药物。壳聚糖（Cts）与 LZC-2b 的相互作用用于完成封装，而无需任何交联。所得的微药物（LZC-2b@Cts-MSs）的平均尺寸约为 980nm。LZC-2b@Cts-MSs 的载药效率（DLE）约为 79%。此外，LZC-2b@Cts-MSs 的药物释放呈 pH 依赖性。在 pH=7.4 时，仅释放了 5.1%的负载 LZC-2b，而在 pH=5.0 时，释放了 90.3%的负载 LZC-2b。细胞培养结果表明，LZC-2b@Cts-MSs 可以被 KB 细胞轻易摄取。细胞活力结果表明，LZC-2b@Cts-MSs 可以有效杀死 KB 细胞。我们合成和制备 pH 响应性 LZC-2b@Cts-MSs 的策略在口腔癌的化学疗法中具有广阔的前景。
