卡培他滨-层状双金属氢氧化物纳米杂化物的制备及其性能分析  

Preparation and properties analysis of Capecitabine-LDHs nanocomplexes

作　　者：于红卫[1] 孙枫林 杨超[1] YU Hong-wei;SUN Feng-lin;YANG Chao(Physical and chemical laboratory,Qingdao Municipal Center for Disease Control and Prevention,Shandong 266033,China)

机构地区：[1]青岛市疾病预防控制中心理化检验所,山东266033

出　　处：《预防医学论坛》2024年第8期620-623,629,共5页Preventive Medicine Tribune

摘　　要：目的 制备海藻酸钠(SA)包覆卡培他滨-层状双金属氢氧化物(LDHs)纳米杂化物形成微球,并分析其性能。方法 采用共沉淀法制备卡培他滨-LDHs的纳米杂合物,采用紫外-分光光度计测定卡培他滨-LDHs/SA中卡培他滨的含量,用X射线衍射仪分析LDHs和卡培他滨-LDHs纳米杂化物的晶体结构,测定卡培他滨释放速率。结果 SA微球呈透明胶状;而SA/LDHs微球呈乳白色球状。30倍扫描电子显微镜(SEM)观察的微球表面形态,微球整体呈椭圆球状;1 000倍SEM观察的微球表面形态,加入LDHs后微球的结构发生了变化,可明显看出LDHs的片状结构。卡培他滨-SA/LDHs纳米杂化物微球、SA/LDHs微球具备LDHs、SA微球的特征。LDHs/SA在003峰(11.59°)处有明显的峰,SA的特征峰(31.38°、45.57°)比较明显。在37℃下pH=7.2缓冲溶液中卡培他滨的释放情况:在微球释放的前100 min为卡培他滨在卡培他滨-SA/LDHs纳米杂化物微球中的快速释放阶段,释放率达到了80%;在之后的200 min内卡培他滨释放完成了缓慢释放阶段,释放率达到了95%;而未包覆SA的纳米杂化物的快速释放时间为50 min,释放率为67%,在100 min内完成缓慢释放,释放率为80%,释放不完全。在37℃下pH=2.2缓冲溶液中卡培他滨的释放情况:对比卡培他滨-LDHs纳米杂化物在30 min内卡培他滨的释放率达到98%,50 min内完全释放,药物在卡培他滨-SA/LDHs纳米杂化物微球中缓释性能与物理混合LDHs和卡培他滨相比更好。卡培他滨在微球内释放的前100 min是快速释放阶段,释放率达到90%,在之后的230 min内完成了缓慢释放阶段,释放率达到98%,随后达到平衡,卡培他滨完全释放。结论 在一定条件下,卡培他滨-海藻酸钠/LDHs微球可以控制卡培他滨在酸性条件下的缓释速率。Objective To prepare sodium alginate(SA)coated capecitabine-layered bimetallic hydroxide(LDHs)nanocomposites to form microspheres,and to analyze their properties.Methods Capecitabine-LDH nanocomplexes were synthesized via the co-precipitation method.The content of capecitabine in the capecitabine-LDH/SA nanocomposites was determined using a UV-spectrophotometer.The crystal structures of LDHs and capecitabine-LDHs nanocomplexes were analyzed by X-ray diffractometer,and the release rate of capecitabine was determined.Results The SA microspheres were transparent adhesive.The SA/LDHs microspheres were milky white spheres.The surface morphology of the microsphere was observed by 30-fold scanning electron microscope(SEM).The surface morphology of microspheres observed by 1000-fold SEM showed that the structure of microspheres changed after LDHs was added,and the lamellar structure of LDHs could be clearly seen.Capecitabine-SA/LDHs nanohybrid microspheres and SA/LDHs microspheres had the characterwastics of LDHs and SA microspheres.LDHs/SA had an obvious peak at peak 003(11.59°),and the characterwastic peaks of SA(31.38°,45.57°)were more obvious.Release of capecitabine in buffer solution with pH=7.2 at 37℃.the first 100 min of release of the microspheres was the rapid release stage of capecitabine in capecitabine-SA/LDHs nanohybrid microspheres,and the release rate reached 80%.In the following 200 minutes,capecitabine release completed the slow release phase,and the release rate reached 95%.The fast release time of the nano-hybrid without SA coating was 50 min,the release rate was 67%,and the release rate was 80%within 100 min,and the release was incomplete.Release of capecitabine in a pH=2.2 buffer solution at 37℃:the release rate of capecitabine-LDHS nanohybrid reached 98%within 30 min and was completely released within 50 min.The sustained release performance of the drug in capecitabine-SA/LDHs nanohybrid microspheres was better than that of physical mixture of LDHs and capecitabine.The first 100 min of capeci

关 键 词：共沉淀法 海藻酸钠 卡培他滨-层状双金属氢氧化物纳米杂化物 释放率 

分 类 号：R914.2[医药卫生—药物化学] R979.1[医药卫生—药学]