Kyzioł Agnieszka, Mazgała Aleksandra, Michna Justyna, Regiel-Futyra Anna, Sebastian Victor
1 Faculty of Chemistry, Jagiellonian University, Kraków, Ingardena, Poland.
2 Department of Chemical Engineering, Nanoscience Institute of Aragon (INA), Zaragoza, Spain.
J Biomater Appl. 2017 Aug;32(2):162-174. doi: 10.1177/0885328217714352. Epub 2017 Jun 26.
In this work, alginate beads loaded with ciprofloxacin (AL_CP) and alginate beads loaded with ciprofloxacin and covered by chitosan (AL_CP_CS) were prepared by emulsification technique in combination with internal gelation method. Physicochemical characterization of the resulting formulations revealed the hydrodynamic diameter and Zeta potential ca. 160 nm and ca. -32 mV in the case of AL_CP and ca. 240 nm and ca. +14 mV in the case of AL_CP_CS (pH = 6.0), respectively. Kinetics of ciprofloxacin release from alginate/chitosan formulations was studied in different media (pH = 1.2, 6.8, and 7.4). Covering alginate core with a polycation such as chitosan moderates the drug release, resulting in a pH-sensitive hybrid controlled-release system. Herein, alginate beads with encapsulated ciprofloxacin covered with chitosan are proposed as an effective oral delivery system since the drug release from alginate core is limited in low pH solution (gastric conditions).
在本研究中,采用乳化技术结合内部凝胶法制备了负载环丙沙星的海藻酸钠珠(AL_CP)以及负载环丙沙星且表面覆盖壳聚糖的海藻酸钠珠(AL_CP_CS)。对所得制剂的理化特性进行表征发现,在pH = 6.0的条件下,AL_CP的流体动力学直径约为160 nm,Zeta电位约为 -32 mV;AL_CP_CS的流体动力学直径约为240 nm,Zeta电位约为 +14 mV。研究了海藻酸钠/壳聚糖制剂中,环丙沙星在不同介质(pH = 1.2、6.8和7.4)中的释放动力学。用壳聚糖等聚阳离子覆盖海藻酸钠核心可减缓药物释放,从而形成一种pH敏感的混合控释系统。在此,提出用壳聚糖覆盖的包裹有环丙沙星的海藻酸钠珠作为一种有效的口服给药系统,因为在低pH溶液(胃部环境)中,药物从海藻酸钠核心的释放受到限制。