Liu Gan, Tsai Hsiang-I, Zeng Xiaowei, Zuo Yixiong, Tao Wei, Han Jun, Mei Lin
The Shenzhen Key Lab of Gene and Antibody Therapy and Division of Life and Health Sciences, Graduate School at Shenzhen, Tsinghua University, Shenzhen 518055, P. R. China.
School of Life Sciences, Tsinghua University, Beijing 100084, PR China.
Theranostics. 2017 Mar 5;7(5):1192-1203. doi: 10.7150/thno.17881. eCollection 2017.
The efficient delivery of anticancer drugs into tumor tissues to improve therapeutic efficacy remains an urgent demand. To satisfy this demand, a drug delivery system based on a stealthy nanocapsule was developed. This nanocapsule was fabricated by encapsulating stealthy cross-linked poly(2-methacryloyloxyethyl phosphorylcholine) (PMPC) and benzaldehyde groups around the protein bovine serum albumin (BSA) followed by conjugation of doxorubicin (Dox) through a pH-responsive benzoic-imine bond. The results show that the Dox-conjugated nanocapsule (nBSA-Dox) released the drug under an acidic tumor microenvironment (pH ~6.5) and killed HepG2 human liver cancer cells. The half-life of Dox conjugated to nBSA in mice was significantly prolonged, and the area-under-curve of plasma Dox of the mice treated with nBSA-Dox was as much as 242 fold of free Dox. The results confirmed that this nanocapsule efficiently accumulated in tumor tissue and significantly suppressed the tumor growth.
将抗癌药物有效递送至肿瘤组织以提高治疗效果仍然是一项迫切需求。为满足这一需求，开发了一种基于隐形纳米胶囊的药物递送系统。这种纳米胶囊是通过在蛋白质牛血清白蛋白（BSA）周围包裹隐形交联聚（2-甲基丙烯酰氧基乙基磷酰胆碱）（PMPC）和苯甲醛基团，然后通过pH响应性苯甲酰亚胺键偶联阿霉素（Dox）来制备的。结果表明，偶联阿霉素的纳米胶囊（nBSA-Dox）在酸性肿瘤微环境（pH约6.5）下释放药物并杀死HepG2人肝癌细胞。与nBSA偶联的阿霉素在小鼠体内的半衰期显著延长，用nBSA-Dox处理的小鼠血浆阿霉素的曲线下面积是游离阿霉素的242倍。结果证实，这种纳米胶囊在肿瘤组织中有效蓄积并显著抑制肿瘤生长。
