Qiu Li, Zhang Weirui, Wang Shuyun, Zhang Xu, Zhao Yanbao, Cao Liuqin, Sun Lei
Engineering Research Center for Nanomaterials, Henan University, Kaifeng 475004, China.
Department of Pharmaceutics, Henan University, Kaifeng 475004, China.
Mater Sci Eng C Mater Biol Appl. 2017 Dec 1;81:485-491. doi: 10.1016/j.msec.2017.08.029. Epub 2017 Aug 12.
pH/enzyme-responsive nanocarriers based on porous silica (pSiO) nanospheres (NSs) were developed for controlled release of drug. The pSiO NSs present uniform spheres and have an average diameter of 100nm. The pSiO NSs with high specific surface area (835m·g) and the pore volume (1.24cm·g) are suitable for drug loading and the loading capacity reaches to 29% for amoxicillin (AMX) model drug. In this system, protocatechuic acid (PCA) and L-glutamic acid (Glu) as linkers were grafting onto the surface of pSiO NSs to conjugate the capping lids. Acid-decomposable ZnO quantum dots (QDs) were introduced to block the partial pores of pSiO via amido bonds, which could act as gates and fluorescence probes. To minimize the premature release, hyaluronic acid (HA) was further coating on the outer surface of pSiO, which would be degraded by over-expressed hyaluronidase (Hyal-1) in the tumor microenvironment. The controlled release of the drug from the ZnO/HA-gated delivery system was realized by the acidic dissolution of ZnO QDs and enzymatic hydrolysis of HA. The obtained ZnO/HA-gated pSiO delivery system would achieve minimized premature release and responsive release under a physiological environment.
基于多孔二氧化硅（pSiO）纳米球（NSs）开发了pH/酶响应性纳米载体用于药物控释。pSiO NSs呈均匀球形，平均直径为100nm。具有高比表面积（835m·g）和孔体积（1.24cm·g）的pSiO NSs适合药物负载，阿莫西林（AMX）模型药物的负载量达到29%。在该体系中，原儿茶酸（PCA）和L-谷氨酸（Glu）作为连接剂接枝到pSiO NSs表面以连接封端盖。引入酸可分解的氧化锌量子点（QDs）通过酰胺键封堵pSiO的部分孔，其可作为门控和荧光探针。为了使过早释放最小化，在pSiO的外表面进一步包覆透明质酸（HA），其会被肿瘤微环境中过表达的透明质酸酶（Hyal-1）降解。通过ZnO QDs的酸溶解和HA的酶水解实现了药物从ZnO/HA门控递送系统的控释。所获得的ZnO/HA门控pSiO递送系统在生理环境下将实现最小化的过早释放和响应性释放。
