Fu Ya-Nan, Li Yongsan, Li Guofeng, Yang Lei, Yuan Qipeng, Tao Lei, Wang Xing
Beijing Laboratory of Biomedical Materials, Beijing University of Chemical Technology , Beijing 100029, People's Republic of China.
The Key Laboratory of Bioorganic Phosphorus Chemistry and Chemical Biology (Ministry of Education), Department of Chemistry, Tsinghua University , Beijing 100084, People's Republic of China.
Biomacromolecules. 2017 Jul 10;18(7):2195-2204. doi: 10.1021/acs.biomac.7b00592. Epub 2017 Jun 7.
Smart drug carrier with function-oriented adaptations is highly desired due to its unique properties in medical applications. Herein, adaptive chitosan hollow microspheres (CHM) are fabricated by employing interfacial Schiff-base bonding reaction. Hydrophilic macromolecules of glycol chitosan are fixed at the oil/water interface through numerous hydrophobic small molecules of borneol 4-formylbenzoate, forming the CHM with a positively charged surface and lipophilic cavity. These CHM have an average size of 400-1000 nm after passing through the 0.22 μm apertures of filter paper. This phenomenon combined with SEM measurements demonstrates its remarkable shape-adaptive behavior. Furthermore, the CHM present a pH-dependence of structural stability. When pH value reduces from 7.06 to 5.01, the CHM begin to lose their integrity. All those characteristics make the CHM an intelligent drug carrier, especially for water-insoluble anticancer drugs, paclitaxel (PTX) in particular. Both cell uptake and cell cytotoxicity assays suggest that the PTX-loaded CHM are highly efficient on HepG2 and A549 cells. Therefore, rather than most of the traditional materials, these adaptive CHM show great potential as a novel drug carrier.
具有功能导向适应性的智能药物载体因其在医学应用中的独特性质而备受青睐。在此,通过界面席夫碱键合反应制备了适应性壳聚糖中空微球(CHM)。壳聚糖二醇的亲水性大分子通过大量的冰片4-甲酰基苯甲酸疏水小分子固定在油/水界面,形成表面带正电荷且具有亲脂性空腔的CHM。通过0.22μm孔径的滤纸后,这些CHM的平均尺寸为400 - 1000nm。这一现象与扫描电子显微镜测量结果相结合,证明了其显著的形状适应性行为。此外,CHM呈现出结构稳定性的pH依赖性。当pH值从7.06降至5.01时,CHM开始失去其完整性。所有这些特性使CHM成为一种智能药物载体,尤其适用于水不溶性抗癌药物,特别是紫杉醇(PTX)。细胞摄取和细胞毒性试验均表明,负载PTX的CHM对HepG2和A549细胞具有高效性。因此,与大多数传统材料不同,这些适应性CHM作为新型药物载体具有巨大潜力。